ISSN:
1432-1912
Keywords:
Alpha1/alpha2-adrenoceptor antagonism
;
Wy 27127
;
Idazoxan
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Summary Wy 27127 and idazoxan were approximately equipotent as antagonists atα 2-adrenoceptors as estimated by their ability to block clonidine-induced inhibition of electrically-evoked contractions of the rat isolated vas deferens. Idazoxan was seven times as potent as Wy 27127, as an antagonist atα 1-adrenoceptors as indicated by blockade of methoxamine-induced contractions of the rat isolated anococcygeus muscle. Thus, theα 2:α 1 selectivity ratio, as calculated from these tests was 407 for Wy 27127 and 76 for idazoxan. Wy 27127 and idazoxan were equipotent in enhancing stimulation-evoked overflow of tritium from rabbit isolated pulmonary arteries preloaded with [3H]-noradrenaline as expected forα 2-adrenoceptor antagonists. At higher concentrations both compounds reduced the stimulation-evoked contraction of the pulmonary artery but idazoxan was 15 times as potent as Wy 27127 in this respect. Neither compound had marked antagonist actions at 5-hydroxytryptamine (D), muscarinic, presynaptic dopamine or histamine (H1) receptors or atβ 1-adrenoceptors. Thus, idazoxan and Wy 27127 were equipotentα 2-adrenoceptor antagonists in vitro, however, theα 2:α 1 selectivity of Wy 27127 was considerably greater than that of idazoxan by virtue of weakerα 1-adrenoceptor antagonism.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00569380
Permalink