Summary
It is well recognized that 5-HT1 -like receptors are heterogeneous and since in the radioligand studies at least four different 5-HT1 binding site subtypes (5-HT1A, 5-HT1B, 5-HT1C and 5-HT1D) have been discriminated, four such receptor sites may well exist. Despite this multiplicity of 5-HT receptor subtypes, it appears that some 5-HT1 -like receptor-mediated functional responses, elicited by agonists such as 5-carboxamidotryptamine and blocked by methiothepin but not ketanserin, may not correspond to the above subtypes. These effects seem to include, among others, tachycardia in the cat, constriction of arteriovenous anastomoses in the pig and contraction of the rabbit isolated saphenous vein. In the cat heart the potency orders established for both the agonists (5-Carboxamidotryptamine > 5-HT ⋙ BEA 1654 ≫ 8-OH-DPAT=RU 24969=sumatriptan) and antagonists (methiothepin > methysergide > mesulergine ≫ metergoline ≫ mianserin > ketanserin > (±)propranolol) do not correlate with the order of affinity constants for any of the 5-HT1 binding site subtypes. Similarly, there are differences between the 5-HT1 -like receptors involved in the constriction of the porcine arteriovenous anastomoses and the rabbit saphenous vein and the 5-HT1A, 5-HT1B, 5-HT1C and 5-HT1D binding sites.
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© 1991 Birkhäuser Verlag Basel/Switzerland
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van Heuven-Nolsen, D., Villalón, C.M., den Boer, M.O., Saxena, P.R. (1991). 5-HT1-Like Receptors Unrelated to the Known Binding Sites?. In: Fozard, J.R., Saxena, P.R. (eds) Serotonin: Molecular Biology, Receptors and Functional Effects. Birkhäuser Basel. https://doi.org/10.1007/978-3-0348-7259-1_18
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DOI: https://doi.org/10.1007/978-3-0348-7259-1_18
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