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(−)Tertatolol is a potent antagonist at pre- and postsynaptic serotonin 5-HT1A receptors in the rat brain

Jolas, T., Hajdahmane, S., Lanfumey, L., Fattaccini, C. M., Kidd, Emma Jane ORCID:, Adrien, J., Gozlan, H., Guardiola-Lemaitre, B. and Hamon, M. 1993. (−)Tertatolol is a potent antagonist at pre- and postsynaptic serotonin 5-HT1A receptors in the rat brain. Naunyn Schmiedeburgs Archives of Pharmacology 347 (5) , pp. 453-463. 10.1007/BF00166735

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The potential 5-HT1A antagonist properties of the ß-antagonist tertatolol were assessed using biochemical and electrophysiological assays in the rat. (±) Tertatolol bound with high affinity (Ki = 38 nM) to 5-HT1A sites labelled by [3H]8-OH-DPAT in hippocampal membranes. The (–)stereoisomer (Ki = 18 nM) was about 50-fold more potent than the (+)stereoisomer (Ki = 864 nM) to inhibit the specific binding of [3H]-8-OHDPAT. As expected of a 5-HT1A antagonist, (–)tertatolol prevented in a concentration-dependent manner (Ki = 24 nM) the inhibitory effect of 8-OH-DPAT on forskolin-stimulated adenylate cyclase activity in rat hippocampal homogenates. Furthermore in vivo pretreatment with (–)tertatolol (5 mg/kg s.c.) significantly reduced the inhibitory influence of 8-OH-DPAT (0.3 mg/ kg s.c.) on the accumulation of 5-hydroxytryptophan in various brain areas after the blockade of aromatic L-amino acid decarboxylase by NSD-1015 (100 mg/kg i.p.). In vitro (in brainstem slices; Ki 50 nM) and in vivo (in chloral hydrate anaesthetized rats; ID50 0.40 mg/kg i.v.), (–)tertatolol prevented the inhibitory effects of the 5-HT1A receptor agonists 8-OH-DPAT, ipsapirone and lesopitron on the firing rate of serotoninergic neurones within the dorsal raphe nucleus. In about 25% of these neurones, the basal firing rate was significantly increased by (–)tertatolol (up to +47% in vitro, and +30% in vivo). These data indicate that (-)tertatolol is a potent competitive antagonist at both pre (in the dorsal raphe nucleus) - and post (in the hippocampus) - synaptic 5-HT1A receptors in the rat brain.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RM Therapeutics. Pharmacology
Uncontrolled Keywords: Tertatolol - 5-HT1A receptor - Dorsal raphe nucleus - Adenylate cyclase - Nerve impulse flow - 5-HT turnover - 8-OH-DPAT
Publisher: Springer Verlag
ISSN: 0028-1298
Last Modified: 18 Oct 2022 13:39

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