Blocking properties of terguride at the 5-HT2receptor subtypes mediating cardiovascular responses in the rat
| Autor: | Oscar Alcántara-Vázquez, Heinz H. Pertz, Carlos M. Villalón, Araceli Sánchez-López, David Centurión, Ma. Trinidad Villamil-Hernández |
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| Rok vydání: | 2020 |
| Předmět: | |
| Zdroj: | Canadian Journal of Physiology and Pharmacology. 98:511-521 |
| ISSN: | 1205-7541 0008-4212 |
| DOI: | 10.1139/cjpp-2019-0591 |
| Popis: | In vitro studies have suggested that terguride blocks the contractile and relaxant responses produced by 5-hydroxytryptamine (5-HT) via 5-HT2A/2Breceptors. This study has now investigated terguride’s blocking properties on central/peripheral 5-HT2receptors in anaesthetized or pithed rats. Male Wistar anaesthetized/pithed rats were cannulated for recording blood pressure and heart rate and for i.v. administration of several compounds. In both groups of rats, i.v. bolus injections of 5-HT or (±)-DOI (a 5-HT2receptor agonist; 1–1000 μg/kg) produced dose-dependent increases in diastolic blood pressure and heart rate. These responses were dose-dependently antagonized by terguride (10–3000 μg/kg). In anaesthetized rats, i.v. bolus injections of BW723C86 (a 5-HT2Breceptor agonist; 1–1000 μg/kg) produced dose-dependent increases in diastolic blood pressure and not dose-dependent increases in heart rate, while in pithed rats, these responses were attenuated. The vasopressor responses elicited by BW723C86 in anaesthetized rats were dose-dependently blocked by terguride (10–300 μg/kg), whereas its the tachycardic responses were dose-independently blocked. These results, taken together, suggest that terguride behaved as an antagonist at the 5-HT2receptors located in the central nervous system and (or) the systemic vasculature. This is the first evidence demonstrating that terguride can block central/peripheral 5-HT2receptors mediating cardiovascular responses in anaesthetized or pithed rats. |
| Databáze: | OpenAIRE |
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