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  • Title: Influence of alpha 1-adrenoceptor antagonism of ketanserin on the nature of its 5-HT2 receptor antagonism.
    Author: Marwood JF.
    Journal: Clin Exp Pharmacol Physiol; 1994 Dec; 21(12):955-61. PubMed ID: 7736654.
    Abstract:
    1. In order to investigate alpha 1-adrenoceptor interactions with 5-HT2 receptors, the effect of ketanserin (which antagonizes both types of the above receptors) on responses to 5-hydroxytryptamine (5-HT) and phenylephrine (PE) was measured in isolated perfused rat tail arteries. 2. Ketanserin was found to be a competitive antagonist at 5-HT2 receptors (pA2 = 9.19) and alpha 1-adrenoceptors (pA2 = 7.52). 3. Ritanserin, an analogue of ketanserin with very weak alpha 1-adrenoceptor antagonist activity, was found to be a potent non-competitive 5-HT2 receptor antagonist. 4. In the presence of the potent alpha 1-adrenoceptor antagonist prazosin, ketanserin was a non-competitive 5-HT2 receptor antagonist. 5. Thus, for ketanserin to exhibit competitive 5-HT2 receptor antagonism, its coexisting alpha 1-adrenoceptor antagonist property appears mandatory.
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