5-Hydroxytryptamine (5-HT) induced concentration-related relaxations (EC50 = 9.1 microM) of guinea-pig proximal colon pretreated with ketanserin (1 microM) and ondansetron (10 microM). This 5-HT-induced effect was neuronally mediated since it was blocked by tetrodotoxin (0.3 microM). 5-Carboxamidotryptamine was a full agonist and ten times more potent than 5-HT. alpha-Methyl-5-HT was a partial agonist. 2-Methyl-5-HT was without effect. Methysergide and metergoline were antagonists of 5-HT producing parallel shifts at 0.1 microM but unsurmountable antagonism at higher concentrations. pKB values of 8.0 and 7.3 were calculated for methysergide and metergoline, respectively. This study has identified a 5-HT-induced relaxation of guinea-pig proximal colon which is mediated via a neuronal 5-HT1-like receptor. However, the subtype has yet to be established.
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Elswood et al. (1992) studied this question.
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