ISSN:
1474-8673
Source:
Blackwell Publishing Journal Backfiles 1879-2005
Topics:
Chemistry and Pharmacology
,
Medicine
Notes:
1 We have investigated the actions of the α1D-adrenoceptor selective antagonist BMY 7378 in comparison with yohimbine at α1- and α2-adrenoceptors. 2 In rat aorta (α1D-adrenoceptor), BMY 7378 (pA2 of 8.67) was about 100 times more potent than yohimbine (pA2 of 6.62) at antagonizing the contractile response to noradrenaline. 3 In human saphenous vein (α2C-adrenoceptor), BMY 7378 (pA2 of 6.48) was approximately 10 times less potent than yohimbine (pA2 of 7.56) at antagonizing the contractile response to noradrenaline. 4 In prostatic portions of rat vas deferens, BMY 7378 (10 μm) did not significantly affect the concentration-dependent inhibition of single pulse nerve stimulation-evoked contractions by xylazine (an action at prejunctional α2D-adrenoceptors). 5 In ligand-binding studies, BMY 7378 showed 10-fold selectivity for α2C-adrenoceptors (pKi of 6.54) over other α2-adrenoceptors. 6 It is concluded that BMY 7378, in addition to α1D-adrenoceptor selectivity in terms of α1-adrenoceptors, shows selectivity for α2C-adrenoceptors in terms of α2-adrenoceptors.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1111/j.1474-8673.2005.00342.x
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