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Evidence for two populations of 5-hydroxytryptamine receptors in dog basilar artery.
J Pharmacol Exp Ther. 1989 Jul; 250(1):379-87.JP

Abstract

The aim of the present study was the classification of the receptors that mediate 5-hydroxytryptamine (5-HT)-induced responses in dog basilar artery. Isolated preparations from basilar artery of mongrel dogs denuded of endothelium were contracted by 5-HT in the presence of 6 microM cocaine. In the presence of either ketanserin or spiperone, concentration-effect curves for 5-5-HT became biphasic. The responses to low concentrations of 5-5-HT were resistant to blockade by either antagonist. The responses to high concentrations of 5-HT were antagonized by ketanserin and spiperone in a concentration-dependent and partially surmountable manner. The lack of complete surmountability was at least partially due to fade during the determination of the cumulative concentration-effect curves. The pKB values for the component of the 5-HT-induced contractions that was antagonized by ketanserin and spiperone were 9.4 and 10.2 (-log M), respectively. The findings are consistent with the assumption of an interaction of ketanserin and spiperone with 5-HT at 5-HT2 receptors. On the other hand, the response to low concentrations of 5-HT is not mediated through 5-HT2 receptors. This response is antagonized by phentolamine with an affinity approximately 10 times lower than its affinity to 5-HT2 receptors, but not by prazosin or benextramine. It is conceivable that the receptor that mediates the response to low concentrations of 5-HT belongs to the 5-HT1A-subpopulation as suggested recently.

Authors+Show Affiliations

Department of Clinical Physiology, Physiological Institute, University of Düsseldorf, Federal Republic of Germany.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

2545865

Citation

Frenken, M. "Evidence for Two Populations of 5-hydroxytryptamine Receptors in Dog Basilar Artery." The Journal of Pharmacology and Experimental Therapeutics, vol. 250, no. 1, 1989, pp. 379-87.
Frenken M. Evidence for two populations of 5-hydroxytryptamine receptors in dog basilar artery. J Pharmacol Exp Ther. 1989;250(1):379-87.
Frenken, M. (1989). Evidence for two populations of 5-hydroxytryptamine receptors in dog basilar artery. The Journal of Pharmacology and Experimental Therapeutics, 250(1), 379-87.
Frenken M. Evidence for Two Populations of 5-hydroxytryptamine Receptors in Dog Basilar Artery. J Pharmacol Exp Ther. 1989;250(1):379-87. PubMed PMID: 2545865.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Evidence for two populations of 5-hydroxytryptamine receptors in dog basilar artery. A1 - Frenken,M, PY - 1989/7/1/pubmed PY - 1989/7/1/medline PY - 1989/7/1/entrez SP - 379 EP - 87 JF - The Journal of pharmacology and experimental therapeutics JO - J Pharmacol Exp Ther VL - 250 IS - 1 N2 - The aim of the present study was the classification of the receptors that mediate 5-hydroxytryptamine (5-HT)-induced responses in dog basilar artery. Isolated preparations from basilar artery of mongrel dogs denuded of endothelium were contracted by 5-HT in the presence of 6 microM cocaine. In the presence of either ketanserin or spiperone, concentration-effect curves for 5-5-HT became biphasic. The responses to low concentrations of 5-5-HT were resistant to blockade by either antagonist. The responses to high concentrations of 5-HT were antagonized by ketanserin and spiperone in a concentration-dependent and partially surmountable manner. The lack of complete surmountability was at least partially due to fade during the determination of the cumulative concentration-effect curves. The pKB values for the component of the 5-HT-induced contractions that was antagonized by ketanserin and spiperone were 9.4 and 10.2 (-log M), respectively. The findings are consistent with the assumption of an interaction of ketanserin and spiperone with 5-HT at 5-HT2 receptors. On the other hand, the response to low concentrations of 5-HT is not mediated through 5-HT2 receptors. This response is antagonized by phentolamine with an affinity approximately 10 times lower than its affinity to 5-HT2 receptors, but not by prazosin or benextramine. It is conceivable that the receptor that mediates the response to low concentrations of 5-HT belongs to the 5-HT1A-subpopulation as suggested recently. SN - 0022-3565 UR - https://www.unboundmedicine.com/medline/citation/2545865/Evidence_for_two_populations_of_5_hydroxytryptamine_receptors_in_dog_basilar_artery_ L2 - https://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=2545865 DB - PRIME DP - Unbound Medicine ER -