Is the beta3-adrenoceptor (ADRB3) a potential target for uterorelaxant drugs?-3

<p><b>Copyright information:</b></p><p>Taken from "Is the beta3-adrenoceptor (ADRB3) a potential target for uterorelaxant drugs?"</p><p>http://www.biomedcentral.com/1471-2393/7/S1/S14</p><p>BMC Pregnancy and Childbirth 2007;7(Suppl 1):S14-S14.</p><p>Published online 1 Jun 2007</p><p>PMCID:PMC1892055.</p><p></p>membranes from myometrium of non-pregnant and pregnant women. Expected sizes are 67 kDa for ADRB2 and 68 kDa for ADRB3. These experiments were performed on myometrium from five non-pregnant and five pregnant women. Homogenate of Chinese Hamster Ovary cells transfected with the human ADRB3 (ADRB3-CHO) was used as positive control. Analysis of the expression of ADRB2 and ADRB3 immunoreactive proteins in myometrium of non-pregnant and pregnant women. A.D.U. represents the intensity of the bands evaluated by densitometry. Each bar represents the mean ± s.e.m. from five different non-pregnant and five different pregnant women. Figure reproduced from the paper by Rouget [29]

Is the beta3-adrenoceptor (ADRB3) a potential target for uterorelaxant drugs?-2

<p><b>Copyright information:</b></p><p>Taken from "Is the beta3-adrenoceptor (ADRB3) a potential target for uterorelaxant drugs?"</p><p>http://www.biomedcentral.com/1471-2393/7/S1/S14</p><p>BMC Pregnancy and Childbirth 2007;7(Suppl 1):S14-S14.</p><p>Published online 1 Jun 2007</p><p>PMCID:PMC1892055.</p><p></p>ts, and beta2 microglobulin expression was used as a standard reference

Representative recording of the effect of SR 59119A on spontaneous contractions of human non-pregnant (upper trace) and near-term (lower trace) myometrial strips

<p><b>Copyright information:</b></p><p>Taken from "Is the beta3-adrenoceptor (ADRB3) a potential target for uterorelaxant drugs?"</p><p>http://www.biomedcentral.com/1471-2393/7/S1/S14</p><p>BMC Pregnancy and Childbirth 2007;7(Suppl 1):S14-S14.</p><p>Published online 1 Jun 2007</p><p>PMCID:PMC1892055.</p><p></p

Concentration-response curve for SR59119 and Salbutamol (ADRB3 and ADRB2 agonists respectively) in human near term myometrium

<p><b>Copyright information:</b></p><p>Taken from "Is the beta3-adrenoceptor (ADRB3) a potential target for uterorelaxant drugs?"</p><p>BMC Pregnancy and Childbirth 2007;7(Suppl 1):S14-S14.</p><p>Published online 1 Jun 2007</p><p>PMCID:PMC1892055.</p><p></p

Saturation experiments with ¹²⁵I-HEAT on receptor variants.

<p>Saturation experiments with ¹²⁵I-HEAT on receptor variants.</p

Homology modelling of the ρ-Da1a binding site in the α_1A-AR and the MT7 toxin.

<p>Views from the side of the TM bundle (Panel A), and from the top of the extracellular space (Panel B). F187^5.41, F193^5.47, F281^6.44, M292^6.55, F308^7.35 in green. D106^3.32 and the double S188^5.42/S192^5.46 in orange. F86^2.64, F288^6.51 and F312^7.39 in red. Panel C :3D structure of the three-finger fold MT7 toxin (2vlw) with the four conserved disulfide bridges in red.</p

Inhibition of the binding of a series of concentrations of ³H-prazosin and ¹²⁵I-HEAT to α_1A-AR by ρ-Da1a.

<p>Panel A ³H-prazosin binding (from 0.2 to 16 nM) inhibited by ρ-Da1a. Panel B ¹²⁵I-HEAT binding (from 0.1 to 1.25 nM) inhibited by ρ-Da1a. Panel C and D: Fitting, by the Cheng and Prusoff equation IC₅₀ = Ki+Ki(L/Kd), of IC₅₀ values as a function of the radiotracer concentrations.</p

Effect of human α_1A-AR mutations on receptor expression and affinity for HEAT and ρ-Da1a.

*<p>for p&lt;0.05. Position refers to the Ballesteros-Weinstein numbering scheme for residues within TM domains of G protein-coupled receptors. n = 3–6.</p

Influence of various ligands on ³H-prazosin and ¹²⁵I-HEAT dissociation.

<p>Panel A: Dissociation of ³H-prazosin (2 nM) binding to α_1A-AR (1 µg) in the presence of prazosin (10 µM, black), prazosin plus ρ-Da1a (2.5 µM, blue), prazosin plus adrenaline (2 mM, red) and prazosin plus EPA (150 µM, green). Panel B : dissociation of ¹²⁵I-HEAT (0.4 nM) binding to α_1A-AR (0.2 µg) in the presence of HEAT (5 µM, black), HEAT plus ρ-Da1a (2.5 µM, blue), HEAT plus prazosin (10 µM, red) and HEAT plus EPA (150 µM, green). n = 2.</p

Pharmacological profile of ρ-Da1a binding to various human AR subtypes expressed in eukaryotic cells.

<p>Binding inhibition curves for ³H-prazosin (2 nM), ³H-rauwolscine (2 nM) and ³H-CGP-12177 (6 nM) on hα_1A- (1 µg, ○), hα_1B- (3 µg, •), hα_1D- (29 µg, □), hα_2A- (140 µg, ◊), hα_2B- (100 µg, Δ), hα_2C- (3 µg, x), β₁- (3 µg,▾) and β₂-AR (1.5 µg, ▪) with recombinant ρ-Da1a. n = 4.</p