27 research outputs found
2-(5-Bromopentyl)-4-chloro-5-[2-(4-methoxyphenyl)ethylamino]pyridazin-3(2H)-one
The asymmetric unit of the title compound, C18H23BrClN3O2, consists of two molecules which exhibit different conformations of the pentyl chains [C—C—C—C torsion angles of −60.4 (4) and 175.8 (3)°]. The crysal packing exhibits a chain structure, generated through the O atom of the pyridazinone forming a hydrogen bond with the N—H group of an adjacent molecule
Imaging of opioid receptors in the central nervous system
In vivo functional imaging by means of positron emission tomography (PET) is the sole method for providing a quantitative measurement of μ-, κ and δ-opioid receptor-mediated signalling in the central nervous system. During the last two decades, measurements of changes to the regional brain opioidergic neuronal activation—mediated by endogenously produced opioid peptides, or exogenously administered opioid drugs—have been conducted in numerous chronic pain conditions, in epilepsy, as well as by stimulant- and opioidergic drugs. Although several PET-tracers have been used clinically for depiction and quantification of the opioid receptors changes, the underlying mechanisms for regulation of changes to the availability of opioid receptors are still unclear. After a presentation of the general signalling mechanisms of the opioid receptor system relevant for PET, a critical survey of the pharmacological properties of some currently available PET-tracers is presented. Clinical studies performed with different PET ligands are also reviewed and the compound-dependent findings are summarized. An outlook is given concluding with the tailoring of tracer properties, in order to facilitate for a selective addressment of dynamic changes to the availability of a single subclass, in combination with an optimization of the quantification framework are essentials for further progress in the field of in vivo opioid receptor imaging
Report on 8the 7th European Workshop on Molecular and Cellular Endocrinology of the testis.
not applicabl
Simple recipe for blocking ion channels
Original article can be found at: http://www.nature.com/nbt/index.html Copyright Nature Publishing Group. DOI: 10.1038/nbt1005-1234 [Full text of this article is not available in the UHRA]Genome sequencing has provided electrophysiologists with a plethora of new ion channel sequences. Not surprisingly, the supply of pharmacological reagents to probe their functions has lagged behind.Peer reviewe