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The α1D-adrenoceptor antagonist BMY 7378 is also an α2C-adrenoceptor antagonist.
- Source :
- Autonomic & Autacoid Pharmacology; Oct2005, Vol. 25 Issue 4, p135-141, 7p
- Publication Year :
- 2005
-
Abstract
- 1 We have investigated the actions of the α<subscript>1D</subscript>-adrenoceptor selective antagonist BMY 7378 in comparison with yohimbine at α<subscript>1</subscript>- and α<subscript>2</subscript>-adrenoceptors. 2 In rat aorta ( α<subscript>1D</subscript>-adrenoceptor), BMY 7378 (p A<subscript>2</subscript> of 8.67) was about 100 times more potent than yohimbine (p A<subscript>2</subscript> of 6.62) at antagonizing the contractile response to noradrenaline. 3 In human saphenous vein ( α<subscript>2C</subscript>-adrenoceptor), BMY 7378 (p A<subscript>2</subscript> of 6.48) was approximately 10 times less potent than yohimbine (p A<subscript>2</subscript> of 7.56) at antagonizing the contractile response to noradrenaline. 4 In prostatic portions of rat vas deferens, BMY 7378 (10 μ m) did not significantly affect the concentration-dependent inhibition of single pulse nerve stimulation-evoked contractions by xylazine (an action at prejunctional α<subscript>2D</subscript>-adrenoceptors). 5 In ligand-binding studies, BMY 7378 showed 10-fold selectivity for α<subscript>2C</subscript>-adrenoceptors (p K<subscript>i</subscript> of 6.54) over other α<subscript>2</subscript>-adrenoceptors. 6 It is concluded that BMY 7378, in addition to α<subscript>1D</subscript>-adrenoceptor selectivity in terms of α<subscript>1</subscript>-adrenoceptors, shows selectivity for α<subscript>2C</subscript>-adrenoceptors in terms of α<subscript>2</subscript>-adrenoceptors. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 14748665
- Volume :
- 25
- Issue :
- 4
- Database :
- Complementary Index
- Journal :
- Autonomic & Autacoid Pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 18316311
- Full Text :
- https://doi.org/10.1111/j.1474-8673.2005.00342.x