Summary
The studies described here show that in isolated vascular rings contractile responses to 5-HT mediated via both 5-HT1-like and 5-HT2 receptors were potentiated by cooling from 37°C to 25°C. This potentiation could be accounted for mainly by an increase in agonist affinity. Antagonist affinity at the two receptor types was unaltered by cooling. These differences in ligand-receptor thermodynamics have clear cut implications for pharmacological receptor classification schemes based upon agonists as well as antagonists. In addition, the results demonstrate that 5-HT1,-like as well as 5-HT2 receptors participate in hypothermia-induced vascular supersensitivity to 5-HT, implying a possible role for either receptor type in cold-induced vasospasm.
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© 1991 Birkhäuser Verlag Basel/Switzerland
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Prentice, D.J., Barrett, V.J., MacLennan, S.J., Martin, G.R. (1991). Temperature Dependence of Agonist and Antagonist Affinity Constants at 5-HT1-like and 5-HT2 Receptors. 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_15
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DOI: https://doi.org/10.1007/978-3-0348-7259-1_15
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