Role of α-Adrenergic Receptors in the Effect of the β-Adrenergic Receptor Ligands, CGP 12177, Bupranolol, and SR 59230A, on the Contraction of Rat Intrapulmonary Artery

@article{Leblais2004RoleO,
  title={Role of $\alpha$-Adrenergic Receptors in the Effect of the $\beta$-Adrenergic Receptor Ligands, CGP 12177, Bupranolol, and SR 59230A, on the Contraction of Rat Intrapulmonary Artery},
  author={V{\'e}ronique Leblais and Fabrice Pourageaud and María Dolores Ivorra and Christelle Guibert and Roger Marthan and Bernard Muller},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2004},
  volume={309},
  pages={137 - 145}
}
This study investigates the effect of the aryloxypropanolamines 4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-1,3-dihydro-2H-benzimidazol-2-one (CGP 12177), bupranolol, and 3-(2-ethylphenoxy)-1[(1S)-1,2,3,4-tetrahydronaphth-1-ylamino]-(2S)-2-propanol oxalate (SR 59230A) [commonly used as β3- and/or atypical β-adrenergic receptors (β-AR) ligands] on the contractile function of rat intralobar pulmonary artery. Affinities of β-AR ligands for α1-adrenergic receptors (α1-AR) were also evaluated… Expand

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References

SHOWING 1-10 OF 59 REFERENCES
Influence of β-adrenoceptor agonists on the pulmonary circulation. Effects of a β3-adrenoceptor antagonist, SR 59230A
The aims of this study were (a) to compare in the rat isolated perfused lung preparation, the effects of isoprenaline and of three beta3-adrenoceptors agonists, SR 59104A,Expand
Functional studies of the first selective beta 3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes.
TLDR
Evidence is provided that the new selective beta 3-adrenoceptor antagonist can contribute considerably to functional characterization of the beta 2- adrenoceptors as well as in confluent brown fat cells. Expand
Influence of beta-adrenoceptor agonists on the pulmonary circulation. Effects of a beta3-adrenoceptor antagonist, SR 59230A.
TLDR
Results suggest the existence of atypical beta-adrenoceptors in the rat pulmonary vessels and suggest concentration-dependent relaxations during the pulmonary pressure response. Expand
Atypical beta-adrenergic receptor in 3T3-F442A adipocytes. Pharmacological and molecular relationship with the human beta 3-adrenergic receptor.
Expression of ligand binding properties for an atypical beta-adrenergic receptor (beta-AR) subtype was studied during the adipose differentiation of murine 3T3-F442A cells and compared with that ofExpand
Agonistic activity of SR59230A at atypical beta-adrenoceptors in guinea pig gastric fundus and duodenum.
TLDR
The results clearly indicate that SR59230A acts as an atypical beta-adrenoceptor agonist on guinea pig gastric fundus and duodenum. Expand
The role of a low β1-adrenoceptor selectivity of [3H]CGP-12177 for resolving subtype-selectivity of competitive ligands
TLDR
Non-linear fits of competition curves with subtype-selective unlabeled ligands will result in serious distortion in the estimates of affinity of the competing ligands and in the size of subtype populations if [3H]CGP-12177 is considered entirely non- selective. Expand
Aryloxypropanolamine and catecholamine ligand interactions with the beta(1)-adrenergic receptor: evidence for interaction with distinct conformations of beta(1)-adrenergic receptors.
TLDR
Results suggest that catecholamines and aryloxypropanolamines interact with distinct active conformations of the beta(1)-AR: a state that is responsive to catechlamines and is blocked with high affinity by CGP 12177 and LY 362884, and a novel states that is activated by aryLoxypro panolamines but is resistant to blockade by standard beta-AR antagonists. Expand
Evidence against beta 3-adrenoceptors or low affinity state of beta 1-adrenoceptors mediating relaxation in rat isolated aorta.
TLDR
These results provide no evidence for the presence of functional beta(3)-adrenoceptors or the low affinity state of the beta(1)- adrenoceptor in rat aorta. Expand
Comparison of the affinity of beta-blockers for two states of the beta 1-adrenoceptor in ferret ventricular myocardium.
TLDR
In ferret ventricle the effects of (-)-isoprenaline appear to be antagonized by beta-blockers through the state of the beta(1)-adrenoceptor for which (-)-[(125)I]-cyanopindolol and beta- blockers have high affinity. Expand
Atypical beta-adrenoceptors, different from beta 3-adrenoceptors and probably from the low-affinity state of beta 1-adrenoceptors, relax the rat isolated mesenteric artery.
TLDR
It is concluded that beta2- and atypical beta-adrenoceptors (but not beta3- adrenOceptors) relax the rat mesenteric artery, and the atypicals, which is partially located endothelially, may differ from the low-affinity state of the beta1-Adrenoceptor. Expand
...
1
2
3
4
5
...