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Investigating Allosteric Activation of the M1 Muscarinic Acetylcholine Receptor

By Rachel Thomas


Allosteric ligands of G protein-coupled receptors (GPCRs) bind to sites that are topographically distinct from the orthosteric site. AC-42 and 77-LH-28-1 are functionally selective M1 muscarinic acetylcholine (mACh) receptor allosteric agonists that are able to activate the M1 mACh receptor in the absence of an orthosteric ligand.\ud In the present study, a variety of signalling pathways activated by AC-42 and 77-LH-28-1 have been investigated and compared with those activated by orthosteric agonists in Chinese hamster ovary (CHO) cells recombinantly expressing human M1 mACh receptors. Both orthosteric and allosteric agonists are able to activate Gαq/11-dependent signalling as demonstrated by concentration-dependent increases in [35S]-GTPγS binding to Gαq/11 subunits, [³H]-inositol phosphate accumulation and Ca²+ mobilisation.\ud Both AC-42 and 77-LH-28-1 are also able to activate extracellular signal-regulated kinase 1/2 and cyclic AMP response-element binding protein (CREB). However, while all agonists enhance forskolin-stimulated cyclic AMP accumulation, only orthosteric agonists cause significant increases in [35S]-GTPγS binding to Gαi-proteins, suggesting that subtle differences may exist in the receptor conformations stabilised by orthosteric versus allosteric ligands.\ud The effects of orthosteric and allosteric agonists on the regulation of the M1 mACh receptor expressed in CHO cells revealed that in contrast to orthosteric agonists, which cause significant internalisation and down-regulation, prolonged exposure to AC-42 does not significantly alter either cell-surface or total cellular M1 mACh receptor expression. 77-LH-28-1 does cause receptor internalisation, but not down-regulation.\ud The apparent inability of AC-42 to cause M1 mACh receptor desensitisation is supported by the observation that arecoline was still able to stimulate a similar phosphoinositide hydrolysis response in CHO-hM1 cells incubated for 24 h with AC-42.\ud These data indicate that AC -42 binding causes functional signalling in the absence of receptor regulatory mechanisms. These distinct pharmacological properties of allosteric agonists may provide therapeutic advantages additional to receptor subtype selectivity of action

Publisher: University of Leicester
Year: 2010
OAI identifier: oai:lra.le.ac.uk:2381/9298

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  2. (1996). A heterotrimeric G protein complex couples the muscarinic ml receptor to phospholipase C-beta.
  3. (1994). A novel mechanism for coupling ofm4 muscarinic acetylcholine receptors to calmodulin-sensitive adenylyl cyclases: Crossover from G protein-coupled inhibition to stimulation.
  4. (2008). A novel mechanism of G proteincoupled receptor functional selectivity. muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand.
  5. (2002). A novel pathway for adrenergic stimulation of cAMP-response-element-binding protein (CREB) phosphorylation: Mediation via alphal-adrenoceptors and protein kinase C activation.
  6. (1999). A role for rho-kinase in rho-controlled phospholipase D stimulation by the m3 muscarinic acetylcholine receptor.
  7. (2007). A select set of opioid ligands induce up-regulation by promoting the maturation and stability of the rat kappa-opioid receptor in human embryonic kidney 293 cells.
  8. (2005). A selective metabotropic glutamate receptor 7 agonist: Activation of receptor signaling via an allosteric site modulates stress parameters in vivo.
  9. (1994). Acetylcholine mustard labels the binding site aspartate in muscarinic acetylcholine receptors.
  10. (1999). Activation of adenylate cyclase by human recombinant sst5 receptors expressed in CHO-K1 cells and involvement of galphas proteins.
  11. (2003). Activation of Ml muscarinic receptors triggers transmitter release from rat sympathetic neurons through an inhibition ofM-type K+ channels.
  12. (1996). Activation of muscarinic acetylcholine receptors via their allosteric binding sites.
  13. (1997). Activation of p38 mitogen-activated protein kinase by signaling through G protein-coupled receptors. involvement of gbetagamma and Galphaql11 subunits.
  14. (1991). Activation of the beta 1 isozyme of phospholipase C by alpha subunits of the gq class of G proteins.
  15. (1995). Activation of the STAT pathway by angiotensin II in T3CHOIATIA cells. cross-talk between angiotensin II and interleukin-6 nuclear signaling.
  16. (1995). Adenylyl cyclases and the interaction between calcium and cAMP signalling.
  17. (2003). ADP-ribosylation factor-dependent phospholipase D activation by the M3 muscarinic receptor.
  18. (1992). Agents that stimulate phosphoinositide turnover also elevate cAMP in SK-N-SH human neuroblastoma cells.
  19. (1995). Agonist-dependent phosphorylation of human muscarinic receptors in spodoptera frugiperda insect cell membranes by G protein-coupled receptor kinases.
  20. (1990). Agonist-independent phosphorylation of purified cardiac muscarinic cholinergic receptors by protein kinase
  21. (1999). Agonist-induced desensitization and phosphorylation of m I-muscarinic receptors.
  22. (1994). Agonist-induced muscarinic cholinergic receptor internalization, recycling and degradation in cultured neuronal cells. cellular mechanisms and role in desensitization.
  23. (1994). Agonist-mediated destabilization of ml muscarinic acetylcholine receptor mRNA. elements involved in mRNA stability are localized in the 3'-untranslated region.
  24. (2008). Agonist-selective mechanisms of GPCR desensitization.
  25. (2006). Agonist-selective mechanisms of mu-opioid receptor desensitization in human embryonic kidney 293 cells.
  26. (1997). Agonist-specific receptor conformations.
  27. (1999). Alanine-scanning mutagenesis of transmembrane domain 6 of the M(1) muscarinic acetylcholine receptor suggests that Tyr381 plays key roles in receptor function.
  28. (2006). Allosteric agonists of 7TM receptors: Expanding the pharmacological toolbox. Trends Pharmacal.
  29. (1991). Allosteric antagonists of the muscarinic acetylcholine receptor.
  30. (2002). Allosteric binding sites on cell-surface receptors: Novel targets for drug discovery.
  31. (2007). Allosteric GPCR modulators: Taking advantage of permissive receptor pharmacology.
  32. (1998). Allosteric interactions at muscarinic cholinoceptors.
  33. (1991). Allosteric interactions at the ml, m2 and m3 muscarinic receptor subtypes.
  34. (2000). Allosteric interactions between the antagonist prazosin and amiloride analogs at the human alpha(1A)-adrenergic receptor.
  35. (2000). Allosteric interactions of staurosporine and other indolocarbazoles with N-[methyl-(3)H]scopolamine and acetylcholine at muscarinic receptor subtypes: Identification of a second allosteric site.
  36. (2006). Allosteric interactions with muscarinic acetylcholine receptors: Complex role of the conserved tryptophan M2422Trp in a critical cluster of amino acids for baseline affinity, subtype selectivity, and cooperativity.
  37. (2007). Allosteric modulation of G protein-coupled receptors.
  38. (2002). Allosteric modulation of muscarinic receptor signaling: Alcuronium-induced conversion of pilocarpine from an agonist into an antagonist.
  39. (2005). Allosteric modulation of the cannabinoid CBI receptor.
  40. (2008). Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia.
  41. Allosteric modulation ofG protein-coupled receptors.
  42. (2009). Allosteric modulators of GPCRs: A novel approach for the treatment of CNS disorders.
  43. (1963). Allosteric proteins and cellular control systems.
  44. (1991). Allosteric regulation of cloned m1-m5 muscarinic receptor subtypes.
  45. (2005). Allosterism at muscannlC receptors: Ligands and mechanisms.
  46. (1997). Altered activity of palmitoylation-deficient and isoprenylated forms of the G protein-coupled receptor kinase GRK6.
  47. (1999). Altered airway and cardiac responses in mice lacking G protein-coupled receptor kinase 3.
  48. (2009). Altered M(1) muscarinic acetylcholine receptor (CHRMl)-galpha(qlll) coupling in a schizophrenia endophenotype.
  49. (2001). Alzheimer's disease: Genes, proteins, and therapy.
  50. (1994). An arginine residue conserved in most G protein-coupled receptors is essential for the function of the m 1 muscarinic receptor.
  51. (1995). An english translation of alzheimer's
  52. (2005). An investigation of whether agonist-selective receptor conformations occur with respect to M2 and M4 muscarinic acetylcholine receptor signalling via Gilo and gs proteins.
  53. (1987). An M2 muscarinic receptor subtype coupled to both adenylyl cyclase and phosphoinositide turnover.
  54. (1961). An unusual type of sympathetic ganglionic stimulant.
  55. (2002). Analogs of WIN 62,577 define a second allosteric site on muscarinic receptors.
  56. and charactenzatlOn of the G protein-coupled receptor kinase GRK5.
  57. (1988). Animal models of alzheimer's disease: Experimental cholinergic denervation.
  58. (1991). Antagonism by 8-hydroxy2( di-n-propylamino )tetraline and other serotonin agonists of muscarinic M I-type receptors coupled to inositol phospholipid breakdown in human IMR-32 and SK-N-MC neuroblastoma cells.
  59. (1995). Arrestin interactions with G protein-coupled receptors. direct binding studies of wild type and mutant arrestins with rhodopsin, beta 2-adrenergic, and m2 muscarinic cholinergic receptors.
  60. (1998). Arrestin-independent internalization of the ml, m3, and m4 subtypes of muscarinic cholinergic receptors.
  61. (2002). Arresting developments in heptahelical receptor signaling and regulation.
  62. (2003). Association of muscarinic ml receptor genetic polymorphisms with psychiatric symptoms and cognitive function in schizophrenic patients.
  63. (2006). Beneficial metabolic effects of M3 muscarinic acetylcholine receptor deficiency.
  64. (2000). Beta-arrestin 2: A receptorregulated MAPK scaffold for the activation of JNK3.
  65. (2007). Beta-arrestin-biased ligands at seventransmembrane receptors.
  66. (1999). Beta-arrestin-dependent formation of beta2 adrenergic receptor-src protein kinase complexes.
  67. (1990). Beta-arrestin: A protein that regulates beta-adrenergic receptor function.
  68. (2002). Bioinformatics and type II Gprotein-coupled receptors.
  69. (2000). Brain-stimulation reward thresholds raised by an antisense oligonucleotide for the M5 muscarinic receptor infused near dopamine cells.
  70. (1991). Carbachol and bradykinin elevate cyclic AMP and rapidly deplete A TP in cultured rat sympathetic neurons.
  71. (1991). Cell cycle-dependent coupling of the calcitonin receptor to different G proteins.
  72. (2007). Cell typespecific upregulation of parkin in response to ER stress.
  73. (1990). Cellular responses to stimulation of the M5 muscarinic acetylcholine receptor as seen in murine L cells.
  74. (2003). Cellular signaling mechanisms for muscarinic acetylcholine receptors. Receptors Channels.
  75. (1988). Characteristics ofphorbol esterand agonist-induced down-regulation of astrocyte receptors coupled to inositol phospholipid metabolism.
  76. (2008). Characterization of a CNS penetrant,
  77. (2002). Characterization of central inhibitory muscarinic autoreceptors by the use of muscarinic acetylcholine receptor knock-out mice.
  78. (1996). Characterization of the G protein-coupled receptor kinase GRK4. identification of four splice variants.
  79. (1999). Characterization of the subtype selectivity of the allosteric modulator heptane1,7-bis-(dimethyl-3'-phthalimidopropyl) ammonium bromide (C7/3-phth) at cloned muscarinic acetylcholine receptors.
  80. (1988). Chemical modification of rat cerebral cortex M 1 muscarinic receptors: Role of histidyl residues in antagonist and agonist binding.
  81. (1992). Cholinergic agonists and interleukin 1 regulate processing and secretion of the alzheimer beta/ A4 amyloid protein precursor.
  82. (2001). Cholinergic dilation of cerebral blood vessels is abolished in M(5) muscarinic acetylcholine receptor knockout mice.
  83. (1988). Clinical, pathological, and neurochemical changes in dementia: A subgroup with preserved mental status and numerous neocortical plaques.
  84. (1988). Cloned Ml muscarinic receptors mediate both adenylate cyclase inhibition and phosphoinositide turnover.
  85. (1992). Cloning and functional expression of a human neuropeptide Y/peptide YY receptor of the Yl type.
  86. (1986). Cloning, sequencing and expression of complementary DNA encoding the muscarinic acetylcholine receptor.
  87. (2007). Common structural requirements for heptahelical domain function in class A and class C G protein-coupled receptors.
  88. (1995). Competition between positive and negative allosteric effectors on muscarinic receptors.
  89. (2008). Conformational thermostabilization of the beta1-adrenergic receptor in a detergentresistant form.
  90. (2006). Constitutive activity and inverse agonism at the M2 muscarinic acetylcholine receptor.
  91. (2000). Coupling of M(2) muscarinic receptors to ERK MAP kinases and caldesmon phosphorylation in colonic smooth muscle.
  92. (1991). Coupling of transfected muscarinic acetylcholine receptor subtypes to phospholipase D.
  93. (1999). CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding.
  94. (2000). Crystal structure of rhodopsin: A G protein-coupled receptor.
  95. (2007). Crystal structure of the human beta2 adrenergic G-protein-coupled receptor.
  96. (2006). Cyclic AMP-dependent and epac-mediated activation of R-ras by G protein-coupled receptors leads to phospholipase D stimulation.
  97. (2008). Cysteine pairs in the third intracellular loop of the muscarinic ml acetylcholine receptor playa role in agonistinduced internalization.
  98. (1997). Cytosolic phospholipase A2 is coupled to muscarinic receptors in the human astrocytoma cell line 1321NI: Characterization of the transducing mechanism.
  99. Decreased muscarinic 1 receptors in the dorsolateral prefrontal cortex of subjects with schizophrenia.
  100. Definition of a continuous human cell line derived from neuroblastoma.
  101. (1994). Deletion analysis of the m4 muscarinic acetylcholine receptor. molecular detenninants for activation of but not coupling to the gi guanine-nucleotide-binding regulatory protein regulate receptor internalization.
  102. (1989). Deletion analysis of the mouse ml muscarinic acetylcholine receptor: Effects on phosphoinositide metabolism and downregulation.
  103. (2002). Deletion of the M5 muscarinic acetylcholine receptor attenuates morphine reinforcement and withdrawal but not morphine analgesia.
  104. (1995). Desensitization and internalization of the m2 muscarinic acetylcholine receptor are directed by independent mechanisms.
  105. (2007). Desensitization and re-sensitization of CGRP receptor function in human neuroblastoma SK-N-MC cells.
  106. (1995). Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: Interactions of strychnine and acetylcholine at muscarinic receptors.
  107. (2002). Determinants of metabotropic glutamate receptor-5-mediated Ca2+ and inositol 1,4,5-trisphosphate oscillation frequency. receptor density versus agonist concentration.
  108. (1993). Development of antisera selective for m4 and m5 muscarinic cholinergic receptors: Distribution of m4 and m5 receptors in rat brain.
  109. (1995). Development of selective antisera for muscarinic cholinergic receptor subtypes.
  110. (1997). Differences between natural and recombinant G proteincoupled receptor systems with varying receptor/G protein stoichiometry.
  111. (1995). Differential calcium signalling by m2 and m3 muscarinic acetylcholine receptors in a single cell type.
  112. (1995). Differential coupling of m2 and m4 muscarinic receptors to inhibition of adenylyl cyclase by gi alpha and G( 0 )alpha subunits.
  113. (1994). Differential regulation of cAMPmediated. gene t~anscription by m 1 and m4 muscarinic acetylcholine receptors. preferentIal couplIng ofm4 receptors to gi alpha-2.
  114. (1999). Differential regulation of muscarinic MI and M3 receptors by a putative phosphorylation domain.
  115. (1993). Differential regulation of muscarinic receptor mRNA levels in neuroblastoma cells by chronic agonist exposure: A comparative polymerase chain reaction study.
  116. (1988). Differential regulation of PI hydrolysis and adenylyl cyclase by muscarinic receptor subtypes.
  117. (2008). Differential role of beta-arrestin ubiquitination in agonist-promoted downregulation of M 1 vs M2 muscarinic acetylcholine receptors.
  118. (1993). Differential signal transduction by five splice variants of the PACAP receptor.
  119. (1997). Direct stimulation of bruton's tyrosine kinase by G(q)-protein alpha-subunit.
  120. (2009). Discovery and characterization of novel allosteric potentiators of M 1 muscarinic receptors reveals multiple modes of activity.
  121. (2002). Discovery of an ectopic activation site on the M(I) muscarinic receptor.
  122. (1994). Discrete activation of transduction pathways associated with acetylcholine m1 receptor by several muscarinic ligands.
  123. (2008). Distinct pathways of ERK activation by the muscarinic agonists pilocarpine and carbachol in a human salivary cell line.
  124. (1987). Distinct primary structures, ligandbinding properties and tissue-specific expression of four human muscarinic acetylcholine receptors.
  125. (2007). Distinct structural changes in a G protein-coupled receptor caused by different classes of agonist ligands.
  126. (1966). Ditran and its antagonists in a mixed psychiatric population.
  127. (2001). Dual effects of muscarinic M(2) acetylcholine receptors on the synthesis of cyclic AMP in CHO cells: Dependence on time, receptor density and receptor agonists.
  128. (2005). Dynamics of signaling by PKA.
  129. (1998). Effector pathway-dependent relative efficacy at serotonin type 2A and 2C receptors: Evidence for agonist-directed trafficking of receptor stimulus.
  130. (1996). Effects of long-term treatment with the allosteric enhancer, PD81,723, on chinese hamster ovary cells expressing recombinant human Al adenosine receptors.
  131. (1999). Endocytosis and recycling of muscarinic receptors.
  132. (2002). Endogenous G protein-coupled receptor kinase 6 regulates M3 muscarinic acetylcholine receptor phosphorylation and desensitization in human SH-SY5Y neuroblastoma cells.
  133. (2003). Erk1l2- and p38 MAP kinasedependent phosphorylation and activation of cPLA2 by m3 and m2 receptors.
  134. (2000). Essential role of dynamin in internalization of M2 muscarinic acetylcholine and angiotensin ATIA receptors.
  135. (1988). Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods.
  136. Evaluation of muscarinic agonist-induced analgesia in muscarinic acetylcholine receptor knockout mice.
  137. (2003). Evolution, structure, and activation mechanism of family 3/C G-protein-coupled receptors.
  138. (1995). Expression of ml-m4 muscarinic acetylcholine receptor proteins in rat hippocampus and regulation by cholinergic innervation.
  139. (1990). Expression of muscarinic acetylcholine and dopamine receptor mRNAs in rat basal ganglia.
  140. (2005). Fenobam: A clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity.
  141. (1999). Fluorescent muscarinic EGFP-hMI chimeric receptors: Design, ligand binding and functional properties.
  142. (2003). Forskolin as a tool for examining adenylyl cyclase expression, regulation, and G protein signaling.
  143. (1999). Functional characterization and potential applications for enhanced green fluorescent protein- and epitope-fused human Ml muscarinic receptors.
  144. (1999). Functional comparison of muscarinic partial agonists at muscarinic receptor subtypes hMl, hM2, hM3, hM4 and hM5 using microphysiometry.
  145. (1993). Functional role of proline and tryptophan residues highly conserved among G protein-coupled receptors studied by mutational analysis of the m3 muscarinic receptor.
  146. (2007). Functional selectivity and classical concepts of quantitative phannacology.
  147. (2002). G protein-coupled receptor allosterism and complexing.
  148. (1998). G protein-coupled receptor kinases.
  149. (1998). G protein-coupled receptors. II. mechanism of agonist activation.
  150. (1998). G protein-coupled receptors. III. new roles for receptor kinases and beta-arrestins in receptor signaling and desensitization.
  151. (1998). G-protein signaling: Fine-tuning signaling kinetics.
  152. (1997). G-protein-coupled receptors: Molecular mechanisms involved III receptor activation and selectivity of G-protein recognition.
  153. (1998). G-protein-coupled receptors: Tum-ons and turn-offs.
  154. (2003). G-proteins as transducers in transmembrane signalling.
  155. (2001). G(q/11) and G(i/o) activation profiles in CHO cells expressing human muscarinic acetylcholine receptors: Dependence on agonist as well as receptor-subtype.
  156. (2006). Galantamine improves cognition in schizophrenic patients stabilized on risperidone.
  157. (1994). GCRDb: A G-protein-coupled receptor database. Receptors Channels.
  158. (2007). GPCR engineering yields high-resolution structural insights into beta2-adrenergic receptor function.
  159. (2005). Group I metabotropic glutamate receptors, mGlu 1 a and mGlu5a, couple to cyclic A~P ~esponse element binding protein (CREB) through a common Ca2+ - and protem kmase Cdependent pathway.
  160. (2000). GTPase-activating proteins for heterotrimeric G proteins: Regulators of G protein signaling (RGS) and RGS-like proteins.
  161. (1990). Heterogeneity of [3H]inositol 1,4,5-trisphosphate binding sites in adrenal-cortical membranes. characterization and validation of a radioreceptor assay.
  162. (1983). Heterogeneity of binding sites on cardiac muscarinic receptors induced by the neuromuscular blocking agents gallamine and pancuronium.
  163. (2005). Heterotrimeric G proteins precouple with G protein-coupled receptors in living cells.
  164. (2007). High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor.
  165. (1992). Hml muscarinic cholinergic receptor internalization requires a domain in the third cytoplasmic loop.
  166. (1998). Homer binds a novel proline-rich motif and links group 1 metabotropic glutamate receptors with IP3 receptors.
  167. (1998). Homologous desensitization of the D lA dopamine receptor: Efficacy in causing desensitization dissociates from both receptor occupancy and functional potency.
  168. (1992). Hormonal stimulation of adenylyl cyclase through gi-protein beta gamma subunits.
  169. (1996). Human muscarinic cholinergic receptor Hml internalizes via clathrin-coated vesicles.
  170. (2001). Hyperactivity and intact hippocampus-dependent learning in mice lacking the M 1 muscarinic acetylcholine receptor.
  171. (2001). Hyperactivity, elevated dopaminergic transmission, and response to amphetamine in M 1 muscarinic acetylcholine receptor-deficient mice.
  172. (1994). Ident~ficatIon, punficatIon: and characterization of GRK5, a member of the family of G protem-coupled receptor klnases.
  173. (1990). Identification and characterization of functional D I dopamine receptors in a human neuroblastoma cell line.
  174. (1991). Identification and localization of muscarinic acetylcholine receptor proteins in brain with subtype-specific antibodies.
  175. (1998). Identification of a [3H]ligand for the common allosteric site of muscarinic acetylcholine M2 receptors.
  176. (2003). Identification of allosteric peptide agonists of CXCR4.
  177. (1994). Identification of drugs competing with d-tubocurarine for an allosteric site on cardiac muscarinic receptors.
  178. (1991). Identification of multiple phosphoinositidelinked receptors on human SK-N-MC neuroepithelioma cells.
  179. (2004). Imaging of muscarinic acetylcholine receptor signaling in hippocampal neurons: Evidence for phosphorylation-dependent and -independent regulation by G-protein-coupled receptor kinases.
  180. (1997). In vitro and in vivo biochemistry of olanzapine: A novel, atypical antipsychotic drug.
  181. (1999). In vitro characterisation of the muscarinic receptor partial agonist, sabcomeline, in rat cortical and heart membranes.
  182. (2003). In vivo determination of muscarinic acetylcholine receptor availability in schizophrenia.
  183. (1985). Increased agonist affinity is induced in tetranitromethane-modified muscarinic receptors.
  184. (1990). Indications for selective coupling to phosphoinositide hydrolysis or to adenyl ate cyclase inhibition by endogenous muscarinic receptor subtypes M3 and M4 but not by M2 in tumor cell lines.
  185. (1981). Induction of neurite outgrowth in the IMR-32 human neuroblastoma cell line by nerve growth factor.
  186. (1996). Inhibition of receptor signaling to phospholipase D by clostridium difficile toxin B. role of rho proteins.
  187. (1969). Inhibition of the actions of carbachol and DFP on guinea pig isolated atria by alkane-bis-ammonium compounds.
  188. (2001). Initial sequencing and analysis of the human genome.
  189. (2003). Insights into G protein structure, function, and regulation.
  190. (2005). Integration of G protein signals by extracellular signal-regulated protein kinases in SK-N-MC neuroepithelioma cells.
  191. (2001). Interaction between the G alpha subunit of heterotrimeric
  192. (1997). Interaction of arrestins with intracellular domains of muscarinic and alpha2-adrenergic receptors.
  193. (2006). Interaction studies of multiple binding sites on m4 muscarinic acetylcholine receptors.
  194. (2001). Interactions between allosteric modulators and 4-DAMP and other antagonists at muscarinic receptors: Potential significance of the distance between the N and carboxyl C atoms in the molecules of antagonists.
  195. (2000). Interactions of alcuronium, TMB-8, and other allosteric ligands with muscarinic acetylcholine receptors: Studies with chimeric receptors.
  196. (2003). Interactions of orthosteric and allosteric ligands with [3H]dimethyl-W84 at the common allosteric site of muscarinic M2 receptors.
  197. (1998). Internalization and down-regulation of human muscarinic acetylcholine receptor m2 subtypes. role of third intracellular m2 loop and G protein-coupled receptor kinase 2.
  198. (2000). Internalization and down-regulation of muscarinic acetylcholine receptors in cerebellar granule cells of tenascin-gene deficient mice.
  199. (1990). Internalization of the Hm1 muscarinic cholinergic receptor involves the third cytoplasmic loop.
  200. (2001). Internalization of the M2 muscarinic acetylcholine receptor proceeds through an atypical pathway in HEK293 cells that is independent of clathrin and caveolae.
  201. (1998). International union of pharmacology. XVII. classification of muscarinic acetylcholine receptors.
  202. (1997). Inverse agonism and the regulation of receptor number.
  203. (1999). Is the ras-MAPK signalling pathway necessary for long-term memory formation?
  204. (2002). Isoforms of mammalian adenylyl cyclase: MUltiplicities of signaling.
  205. Life Sci.
  206. (2003). Ligand-selective receptor conformations revisited: The promise and the problem.
  207. (1997). Linkage of G protein-coupled receptors to the MAPK signaling pathway through PI 3-kinase gamma.
  208. (1995). Lipid modifications of trimeric G proteins.
  209. (2000). LNB-TM7, a group of seven-transmembrane proteins related to family-B G-protein-coupled receptors.
  210. (1990). Localization of m5 muscarinic receptor mRNA in rat brain examined by in situ hybridization histochemistry.
  211. Location in muscarinic acetylcholine receptors of sites for [3H]propylbenzilylcholine mustard binding and for phosphorylation with protein kinase
  212. (1994). Location of agonist-dependent-phosphorylation sites in the third intracellular loop of muscarinic acetylcholine receptors (m2 subtype).
  213. (2008). Location, location, location ... site-specific GPCR phosphorylation offers a mechanism for cell-type-specific signalling. Trends Pharmacal.
  214. (2003). Lysine 195 and aspartate 196 in the first extracellular loop
  215. (2000). M(2) and M(4) receptor knockout mice: Muscarinic receptor function in cardiac and smooth muscle in vitro.
  216. (1989). Mechanism of agonist-induced down-regulation and subsequent recovery of muscarinic acetylcholine receptors in a clonal neuroblastoma x glioma hybrid cell line.
  217. (2003). Mechanism of toxicity in rotenone models of parkinson's disease.
  218. (2007). mGluR 7 undergoes rapid internalization in response to activation by the allosteric agonist AMN082.
  219. (1999). Milameline (CI-979/RU35926): A muscarinic receptor agonist with cognition-activating properties: Biochemical and in vivo characterization.
  220. (1999). Mitogenactivated protein kinase: Conservation of a three-kinase module from yeast to human.
  221. (2003). Ml muscarinic agonists can modulate some of the hallmarks in alzheimer's disease: Implications in future therapy.
  222. (1987). Modes of attachment of acetylcholinesterase to the surface membrane.
  223. (1983). Modification of the binding properties of muscarinic receptors by gallamine.
  224. (1997). Modulation of the arrestin-clathrin interaction in cells. characterization of betaarrestin dominant-negative mutants.
  225. (2004). Modulation of the M2 muscarinic acetylcholine receptor activity with monoclonal anti-M2 receptor antibody fragments.
  226. (1993). Molecular and functional diversity of mammalian gs-stimulated adenylyl cyclases.
  227. (1996). Molecular biology of muscarinic acetylcholine receptors.
  228. (2004). Molecular mechanisms of ligand binding, signaling, and regulation within the superfamily of G-protein-coupled receptors: Molecular modeling and mutagenesis approaches to receptor structure and function.
  229. (2006). Monitoring ligand-mediated internalization of G protein-coupled receptor as a novel pharmacological approach.
  230. (1996). Morphine activates opioid receptors without causing their rapid internalization.
  231. (1998). Morphine-activated opioid receptors elude desensitization by beta-arrestin.
  232. (1973). Morphology and growth, tumorigenicity, and cytogenetics of human neuroblastoma cells in continuous culture.
  233. (2001). Multiple allosteric sites on muscarinic receptors.
  234. (2000). Multiple endocytic pathways of G protein-coupled receptors delineated by GIT1 sensitivity.
  235. (2002). Multiple new and isolated families within the mouse superfamily of VIr vomeronasal receptors.
  236. (2008). Multiple roles of phosphoinositide-specific phospholipase C isozymes.
  237. (2000). Multiple topological domains mediate subtype-specific internalization of the M2 muscanmc acetylcholine receptor.
  238. (2004). Muscarinic acetylcholine receptor knockout mice: Novel phenotypes and clinical implications.
  239. (1997). Muscarinic acetylcholine receptor subtype, m2: Diverse functional implications of differential synaptic localization.
  240. (2005). muscarinic acetylcholine receptor without inducing adaptive changes.
  241. (1990). Muscarinic acetylcholine receptors. peptide sequencing identifies residues involved in antagonist binding and disulfide bond fonnation.
  242. (2000). Muscarinic activation of mitogen-activated protein kinase in PC12 cells.
  243. (2007). Muscarinic M2 receptors directly activate Gqlll and gs G-proteins.
  244. (1996). Muscarinic ml receptor-stimulated adenylate cyclase activity in chinese hamster ovary cells is mediated by gs alpha and is not a consequence ofphosphoinositidase C activation.
  245. (1989). Muscarinic receptor activation of phosphatidylcholine hydrolysis. relationship to phosphoinositide hydrolysis and diacylglycerol metabolism.
  246. (2005). Muscarinic receptor agonists and antagonists in the treatment of alzheimer's disease.
  247. (1989). Muscarinic receptor binding characteristics of a human neuroblastoma SK-N-SH and its clones SHSY5Yand SH-EPI.
  248. (1999). Muscarinic receptor ligands and their therapeutic potential.
  249. (1983). Muscarinic receptor subclasses.
  250. (1996). Muscarinic receptor subtypes and smooth muscle function.
  251. (1992). Muscarinic receptor subtypes in human neuroblastoma cell lines SH-SY5Y and IMR-32 as determined by receptor binding, ca++ mobilization and northern blotting.
  252. (2006). Muscarinic receptor subtypes in neuronal and non-neuronal cholinergic function.
  253. (1988). Muscarinic receptor-mediated increase in cAMP levels in SK-N-SH human neuroblastoma cells.
  254. (1997). Muscarinic receptor-stimulated cytosol-membrane translocation of RhoA.
  255. (1991). Muscarinic receptorlinked elevation of cAMP in SH-SY5Y neuroblastoma cells is mediated by Ca2+ and protein kinase
  256. (1993). Muscarinic receptors--characterization, coupling and function.
  257. (1999). Muscarinic supersensitivity and impaired receptor desensitization in G protein-coupled receptor kinase 5-deficient mice.
  258. (2009). Mutagenic mapping suggests a novel binding mode for selective agonists of M I muscarinic acetylcholine receptors.
  259. (1995). Mutation of carboxyl-terminal threonine residues in human m3 muscarinic acetylcholine receptor modulates the extent of sequestration and desensitization.
  260. (2003). N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate receptor activity.
  261. (2001). New mechanisms in heptahelical receptor signaling to mitogen activated protein kinase cascades.
  262. (2003). Non-visual GRKs: Are we seeing the whole picture? Trends Pharmacol.
  263. (2008). Novel selective allosteric activator of the M 1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats.
  264. (1992). NPY and carbachol raise Ca2+ in SK-N-MC cells by three different mechanisms. evidence for inositol phosphate-independent Ca2+ mobilization by NPY.
  265. (1996). Opposite effects of alcuronium on agonist and on antagonist binding to muscarinic receptors.
  266. (1999). Organization and regulation of mitogen-activated protein kinase signaling pathways. Curro Opin.
  267. (1989). Palmitoylation of the human beta 2-adrenergic receptor. mutation of Cys341 in the carboxyl tail leads to an uncoupled nonpalmitoylated form of the receptor.
  268. (2005). Pathways modulating neural KCNQ/M (Kv7) potassium channels.
  269. (2008). Pharmacological assessment of m 1 muscarinic acetylcholine receptor-gqlll protein coupling in membranes prepared from postmortem human brain tissue.
  270. (1993). Pharmacological characterization of acetylcholine-stimulated [35S]-GTP gamma S binding mediated by human muscarinic ml-m4 receptors: Antagonist studies.
  271. (1986). Pharmacological characterization of cholinergic receptors in a human neuroblastoma cell line.
  272. (1993). Pharmacological characterization of guanine nucleotide exchange reactions in membranes from CHO cells stably transfected with human muscarinic receptors ml-m4. Life Sci.
  273. (2007). Phenotypic" pharmacology: The influence of cellular environment on G protein-coupled receptor antagonist and inverse agonist pharmacology.
  274. (1985). Phorbol ester inhibits phosphoinositide hydrolysis and calcium mobilization in cultured astrocytoma cells.
  275. (2006). Phospholipase A2 is involved in muscarinic receptor-mediated sAPPalpha release independently of cyclooxygenase or lypoxygenase activity in SH-SY5Y cells.
  276. (2007). Phospholipase D signaling: Orchestration by PIP2 and small GTPases.
  277. (2002). Phospholipase D-structure, regulation and function.
  278. (2000). Phospholipase D: Molecular and cell biology of a novel gene family.
  279. (2004). Phospholipid metabolism is required for M 1 muscarinic inhibition of N -type calcium current in sympathetic neurons.
  280. (1995). Phosphorylation of cyclic AMP response element-binding protein and induction of c-fos gene expression on withdrawal from chronic treatment with carbachol in
  281. (1986). Phosphorylation of the cardiac muscarinic receptor in intact chick heart and its regulation by a muscarinic agonist.
  282. (1996). Phosphorylation-dependent activation of the ras-GRF /CDC25Mm exchange factor by muscarinic receptors and G-protein beta gamma subunits.
  283. (1981). Physostigmine and lithium response in the schizophrenias.
  284. (1995). Plasma membrane localization and functional rescue of truncated forms of a G protein-coupled receptor.
  285. (2001). PLD pathway involved in carbachol-induced cl- secretion: Possible role of TNF-alpha.
  286. (1995). Pleckstrin homology domain-mediated membrane association and activation of the betaadrenergic receptor kinase requires coordinate interaction with G beta gamma subunits and lipid.
  287. (1995). Porcine m2 muscarinic acetylcholine receptor-effector coupling in chinese hamster ovary cells.
  288. (1996). Positive allosteric action of ebumamonine on cardiac muscarinic acetylcholine receptors.
  289. (2001). Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501.
  290. (1990). Positive cooperativity in the binding of alcuronium and Nmethylscopolamine to muscarinic acetylcholine receptors.
  291. (1997). Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
  292. (1995). Potentiation by alcuronium of the antimuscarinic effect of N-methylscopolamine in guinea pig left atria.
  293. (1998). Prevention of PC12 cell death by N-acetylcysteine requires activation of the ras pathway.
  294. (1986). Primary structure of porcine cardiac muscarinic acetylcholine receptor deduced from the cDNA sequence.
  295. (1995). Probing of the location of the allosteric site on ml muscarinic receptors by site-directed mutagenesis.
  296. (2006). Probing the molecular mechanism of interaction between 4-n-butyl-l-[ 4-(2-methylphenyl)-4-oxo-l-butyl]-piperidine (AC-42) and the muscarinic M(l) receptor: Direct pharmacological evidence that AC-42 is an allosteric agonist.
  297. (1990). Protein kinase C is involved in desensitization of muscarinic receptors induced by phorbol esters but not by receptor agonists.
  298. (1981). Purification of phosphatidylinositol-specific phospholipase C from rat liver.
  299. (2005). Quantitative analysis of binding parameters of [3H]Nmethylscopolamine in central nervous system of muscarinic acetylcholine receptor knockout mice. Brain Res.
  300. (1995). Quantitative comparisons of muscarinic and bradykinin receptor-mediated ins (1,4,5)P3 accumulation and Ca2+ signalling in human neuroblastoma cells.
  301. (1993). Rapid agonist-mediated phosphorylation of m3-muscarinic receptors revealed by immunoprecipitation.
  302. (1990). Rapid protein kinase Cdependent activation of phospholipase D leads to delayed 1,2-diglyceride accumulation.
  303. Reactive oxygen species regulate signaling pathways induced by M 1 muscarinic receptors in PC12M1 cells.
  304. (1995). receptor and alterations in receptor binding properties of muscarinic agonists.
  305. (1993). Receptor distribution in the human and animal hippocampus: Focus on muscarinic acetylcholine receptors.
  306. (1998). Receptor subtype-specific regulation of muscarinic acetylcholine receptor sequestration by dynamin. distinct sequestration of m2 receptors.
  307. (1998). Receptor-induced transient reduction in plasma membrane Ptdlns( 4,5)P2 concentration monitored in living cells.
  308. (2007). Receptor-mediated activation of heterotrimeric G-proteins: Current structural insights.
  309. (2006). receptors play a central role in modulating AD-like pathology in transgenic mice.
  310. (1992). Reconstitution of agonist-stimulated phosphatidylinositol 4,5-bisphosphate hydrolysis using purified ml muscarinic receptor, Gq/ll, and phospholipase C-beta 1.
  311. (1991). Reconstitutively active G protein-coupled receptors purified from baculovirus-infected insect cells.
  312. (2005). Reduced cocaine self-administration in muscarinic M5 acetylcholine receptor-deficient mice.
  313. (2004). Regulation of acetylcholine-induced phosphorylation of PLD1 in porcine tracheal smooth muscle.
  314. (1990). Regulation of cAMP metabolism in mouse parotid gland by cGMP and calcium .
  315. (1994). Regulation of cAMPmediated gene transcription by wild type and mutated G-protein alpha subunits. inhibition of adenylyl cyclase activity by muscarinic receptor-activated and constitutively activated G( 0) alpha.
  316. (2008). Regulation of cyclic AMP response-element binding-protein (CREB) by GqIlI-protein-coupled receptors in human SH-SY5Y neuroblastoma cells.
  317. (2005). Regulation of M2 muscarinic acetylcholine receptor expression and signaling by prolonged exposure to allosteric modulators.
  318. (1999). Regulation of muscarinic acetylcholine receptor sequestration and function by beta-arrestin.
  319. (2003). Regulation of muscarinic acetylcholine receptor signaling.
  320. (1996). Regulation of phospholipase C-beta1 by gq and m1 muscarinic cholinergic receptor. steady-state balance of receptor-mediated activation and GTPase-activating protein-promoted deactivation.
  321. (2003). Regulation of phospholipase D by muscarinic receptors in rat submandibular ductal cells.
  322. (1991). Regulation of polyphosphoinositide-specific phospholipase C activity by purified gq.
  323. (2004). Regulation of signal transduction at M2 muscarinic receptor.
  324. (1992). Release of alzheimer amyloid precursor derivatives stimulated by activation of muscarinic acetylcholine receptors.
  325. (1997). Residues specifically involved in down-regulation but not internalization of the ml muscarinic acetylcholine receptor.
  326. (1998). Role for G protein-coupled receptor kinase in agonist-specific regulation of mu-opioid receptor responsiveness.
  327. (1994). Role of acidic amino acids in the allosteric modulation by gallamine of antagonist binding at the m2 muscarinic acetylcholine receptor.
  328. (1992). Role of beta gamma subunits of G proteins in targeting the beta-adrenergic receptor kinase to membrane-bound receptors.
  329. (2008). Role of methionine 35 in the intracellular Ca2+ homeostasis dysregulation and Ca2+-dependent apoptosis induced by amyloid beta-peptide in human neuroblastoma IMR32 cells.
  330. (2003). Roles of amyloid precursor protein and its fragments in regulating neural activity, plasticity and memory.
  331. (2005). Roles of phosphorylation-dependent and -independent mechanisms in the regulation of M 1 muscarinic acetylcholine receptors by G protein-coupled receptor kinase 2 in hippocampal neurons.
  332. (1997). SB 202026: A novel muscarinic partial agonist with functional selectivity for M 1 receptors.
  333. (1998). Secretin and vasoactive intestinal peptide receptors: Members of a unique family of G proteincoupled receptors.
  334. (2009). Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation.
  335. (2003). Selective cognitive dysfunction in acetylcholine M 1 muscarinic receptor mutant mice.
  336. (2004). Sequential binding of agonists to the beta2 adrenoceptor. kinetic evidence for intermediate conformational states.
  337. (1998). Sequestration of human muscarinic acetylcholine receptor hml-hm5 subtypes: Effect of G proteincoupled receptor kinases GRK2, GRK4, GRK5 and GRK6.
  338. (1993). Serine- and threonine-rich domain regulates internalization of muscarinic cholinergic receptors.
  339. (2002). Seven-transmembrane receptors.
  340. (1983). Short-term disappearance of muscarinic cell surface receptors in carbachol-induced desensitization.
  341. (2004). Signal transductton underlYIng carbachol-induced contraction of human urinary bladder.
  342. (2001). Signalling roles of mammalian phospholipase D1 and D2.
  343. (2001). Single-cell imaging of graded ins(I,4,5)P3 production following G-proteincoupled-receptor activation.
  344. (1989). Site-directed mutagenesis of ml muscarinic acetylcholine receptors: Conserved aspartic acids play important roles in receptor function.
  345. (1990). Site-directed mutagenesis of the m2 muscarinic acetylcholine receptor. analysis of the role ofN-glycosylation in receptor expression and function.
  346. (1992). Site-directed mutagenesis of the rat m 1 muscarinic acetylcholine receptor. role of conserved cysteines in receptor function.
  347. SK-N-MC neuroblastoma cells.
  348. (2001). Snake toxins that bind specifically to individual subtypes of muscarinic receptors.
  349. (2000). Snake toxins with high selectivity for subtypes of muscarinic acetylcholine receptors.
  350. (1986). Stabilization of antagonist binding to cardiac muscarinic acetylcholine receptors by gallamine and other neuromuscular blocking drugs.
  351. (1988). Stimulation of arachidonic acid release and inhibition of mitogenesis by cloned genes for muscarinic receptor subtypes stably expressed in A9 L cells.
  352. (1999). Stimulation of cAMP synthesis by gi-coupled receptors upon ablation of distinct galphai protein expression. gi subtype specificity of the 5-HTIA receptor.
  353. (1996). Stimulation of cyclic AMP accumulation and phosphoinositide hydrolysis by M3 muscarinic receptors in the rat peripheral lung.
  354. (2001). Stimulation of endothelin B receptors in astrocytes induces cAMP response element-binding protein phosphorylation and c-fos expression via multiple mitogen-activated protein kinase signaling pathways.
  355. (2002). Stimulation of phospholipase C-epsilon by the M3 muscarinic acetylcholine receptor mediated by cyclic AMP and the GTPase Rap2B.
  356. (1991). Stimulation of phospholipase D activity in human neuroblastoma (LA-N-2) cells by activation of muscarinic acetylcholine receptors or by phorbol esters: Relationship to phosphoinositide turnover.
  357. (1997). Stimulusdependent phosphorylation of G-protein-coupled receptors by casein kinase 1 alpha.
  358. (1999). Structural basis ofG protein-coupled receptor function.
  359. (1997). Structural instability of a constitutively active G protein-coupled receptor. agonist-independent activation due to conformational flexibility.
  360. (2006). Structural requirements of transmembrane domain 3 for activation by the MI muscarinic receptor agonists AC42, AC-260584, clozapine, and N-desmethylclozapine: Evidence for three distinct modes of receptor activation.
  361. (1994). Structure and function of G protein-coupled receptors.
  362. (2007). Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors.
  363. (2009). Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders.
  364. (1999). Subtype-selective positive cooperative interactions between brucine analogs and acetylcholine at muscarinic receptors: Functional studies.
  365. (1998). Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: Radioligand binding studies.
  366. (1992). Subunits beta gamma of heterotrimeric G protein activate beta 2 isoform of phospholipase
  367. (1992). Suppressive effect of carbachol on forskolin-stimulated neurite outgrowth in human neuroblastoma NB-OKI cells.
  368. (2008). The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist.
  369. (1995). The allosteric enhancer, PD 81,723, stabilizes human A 1 adenosine receptor coupling to G proteins.
  370. (1999). The beta2-adrenergic receptorlbetaarrestin complex recruits the clathrin adaptor AP-2 during endocytosis.
  371. (1996). The density of muscarinic
  372. (1978). The effect of stercuronium on cardiac muscarinic receptors.
  373. (1998). The EGF-TM7 family: Unusual structures at the leukocyte surface.
  374. (1995). The function of a highlyconserved arginine residue in activation of the muscarinic M 1 receptor.
  375. (1999). The G protein subunit gene families.
  376. (2004). The heptahe1ical domain of GABA(B2) is activated directly by CGP7930, a positive allosteric modulator of the GABA(B) receptor.
  377. (2001). The human serotonin 5-HT4 receptor regulates secretion of non-amyloidogenic precursor protein.
  378. (1976). The inhibitory effect of gallamine on muscarinic receptors.
  379. (2000). The interaction of beta-arrestin with the AP-2 adaptor is required for the clustering of beta 2-adrenergic receptor into clathrin-coated pits.
  380. (1984). The kinetics of competitive radioligand binding predicted by the law of mass action.
  381. (1993). The ligand-binding domain in metabotropic glutamate receptors is related to bacterial periplasmic binding proteins.
  382. (2001). The M3 muscarinic acetylcholine receptor expressed in HEK-293 cells signals to phospholipase D via G12 but not gq-type G proteins: Regulators ofG proteins as tools to dissect pertussis toxin-resistant G proteins in receptor-effector coupling.
  383. (1995). The muscarinic Ml agonist xanomeline increases soluble amyloid precursor protein release from chinese hamster ovary-ml cells.
  384. (1951). The pharmacology of flaxedil, with observations on certain analogs.
  385. (2000). The proliferative and antiapoptotic effects of substance Pare facilitated by formation of a beta -arrestin-dependent scaffolding complex.
  386. (2007). The regulation of Ml muscarinic acetylcholine receptor desensitization by synaptic activity in cultured hippocampal neurons.
  387. (2000). The regulator of G protein signaling family.
  388. (1998). The relationship between agonist intrinsic activity and the rate of endocytosis of muscarinic receptors in a human neuroblastoma cell line.
  389. (2002). The role of beta-arrestins in the termination and transduction of G-protein-coupled receptor signals.
  390. (1998). The role of receptor kinases and arrestins in G protein-coupled receptor regulation.
  391. (1997). The role of the aspartate-arginine-tyrosine triad in the ml muscarinic receptor: Mutations of aspartate 122 and tyrosine 124 decrease receptor expression but do not abolish signaling.
  392. (2001). The sequence of the human genome.
  393. (1984). The structure of an antigenic determinant in a protein.
  394. (2002). The wnts.
  395. (2001). Therapeutic opportunities from muscarinic receptor research.
  396. (2004). Thiochrome enhances acetylcholine affinity at muscarinic M4 receptors: Receptor subtype selectivity via cooperativity rather than affinity.
  397. (1994). Transfected muscarinic acetylcholine receptors selectively couple to gi-type G proteins and Gqlli.
  398. (2004). trisphosphate, Ca2+, diacylglycerol, and protein kinase C signaling using fluorescent biosensors.
  399. (2003). Tumour necrosis factorrelated apoptosis-inducing ligand sequentially activates pro-survival and pro-apoptotic pathways in SK-N-MC neuronal cells.
  400. (1988). Two adjacent cysteine residues in the C-terminal cytoplasmic fragment of bovine rhodopsin are palmitylated.
  401. (1992). Two allosteric modulators interact at a common site on cardiac muscarinic receptors.
  402. (1997). Two homologous phosphorylation domains differentially contribute to desensitization and internalization of the m2 muscarinic acetylcholine receptor.
  403. (1996). Two-point kinetic experiments to quantify allosteric effects on radioligand dissociation.
  404. (1997). Visualization of G protein-coupled receptor trafficking with the aid of the green fluorescent protein. endocytosis and recycling of cholecystokinin receptor type
  405. (2007). When a G protein-coupled receptor does not couple to a G protein.
  406. (1994). Xanomeline: A novel muscarinic receptor agonist with functional selectivity for Ml receptors.

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