The potent 5-HT3 receptor antagonist (R)-zacopride labels an additional high affinity site in the central nervous system

Kidd, Emma Jane ORCID: https://orcid.org/0000-0001-5507-1170, Bouchelet de Vendegies, I., Levy, J. C., Hamon, M. and Gozlan, H. 1992. The potent 5-HT3 receptor antagonist (R)-zacopride labels an additional high affinity site in the central nervous system. European Journal of Pharmacology 211 (1) , pp. 133-136. 10.1016/0014-2999(92)90276-A

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Abstract

The binding characteristics of [3H](S)-zacopride were investigated in membranes from the rat entorhinal cortex and NG 108-15 clonal cells. In contrast to [3H](S)-zacopride which bound solely to 5-HT3 receptors, [3H](R)-zacopride recognized another class of binding sites, called the (R)-sites, in both membrane preparations. In addition to (R)-zacopride (Ki=3–11 nM), only (R)-iodo-zacopride, (R)-dechloro-zacopride, prazosin and mianserin exhibited high to moderate affinity for the (R)-sites, whose possible functions remain to be established.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Pharmacy
Subjects:	R Medicine > RM Therapeutics. Pharmacology
Uncontrolled Keywords:	[3H](R)-Zacopride; [3H](S)-Zacopride; 5-HT3 receptors; Brain (rat); (High affinity (R)-sites)
Publisher:	Elsevier
ISSN:	0014-2999
Last Modified:	18 Oct 2022 13:38
URI:	https://orca.cardiff.ac.uk/id/eprint/14744

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