Evidence that the hypotensive effect of WAY 100635, a 5-HT1A receptor antagonist, is related to vascular α1-adrenoceptor blockade in the adult rat

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1 The effect of WAY100635 (N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl) cyclohexanecarboxamide trihydrochloride), a 5-HT1A receptor antagonist, on cardiovascular function was studied.

2 The i.v. injection of WAY100635 dose-dependently decreased blood pressure in anaesthetized rats; while in pithed rats WAY100635 (1 mg  kg−1) displaced the phenylephrine pressor effect.

3 WAY100635 antagonized phenylephrine-induced contraction in rabbit and rat aorta (pA2 of 6.88 and 7.93 and Schild slopes of −0.83 and −1.21, respectively); while in rat caudal artery pK B was 7.45 and the Schild slope of −0.56, suggesting a complex interaction in this vessel.

4 The results show that WAY100635 induced hypotension in the anaesthetized rat and suggest that this effect could be partially explained by antagonism of vascular α1-adrenoceptors.

Document Type: Research Article

DOI: http://dx.doi.org/10.1046/j.1474-8673.2002.00257.x

Affiliations: 1: Departamento de Farmacobiología, Centro de Investigación y de Estudios Avanzados-Sede Sur, México and 2: Facultad de Estudios Superiores-Iztacala, Universidad Nacional Autónoma de México, México

Publication date: June 1, 2002

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