Effects of ipsapirone, a 5‐HT1Aagonist, on sleep/wakefulness cycles: probable post‐synaptic action
Open Access
- 1 June 1993
- journal article
- Published by Wiley in Journal of Sleep Research
- Vol. 2 (2) , 103-109
- https://doi.org/10.1111/j.1365-2869.1993.tb00070.x
Abstract
SUMMARY The effects of ipsapirone, a ligand of the 5‐HT1Areceptors and a new potential anxiolytic, on sleep/wakefulness regulation were examined in the rat. Injected i.p. at 1, 3 and 5 mg kg‐1, this compound induced a dose‐dependent reduction of paradoxical sleep for 2 to 4 hours, followed, at a dose of 5 mg kg‐1, by a secondary rebound. The other states of vigilance were not modified, except at the latter dose where the amounts of wakefulness were enhanced initially and decreased secondarily, while those of SWS were enhanced from 2 to 4 hours post‐treatment. The effects of ipsapirone (3 mg kg‐1) persisted after infusion of the neurotoxin 5,7‐dihydroxytryptamine into the dorsal raphe nucleus which induced the sub‐total destruction of the serotoninergic system. Thus, the action of the 5‐HT1Aagonist ipsapirone on sleep/wakefulness cycles probably involves the stimulation of the post‐synaptic 5‐HT1Areceptors.Keywords
This publication has 29 references indexed in Scilit:
- The α2-adrenoceptor antagonist activity of ipsapirone and gepirone is mediated by their common metabolite 1-(2-pyrimidinyl)-piperazine (PmP)Published by Elsevier ,2002
- Dose-Related Suppression of REM Sleep and PGO Waves by the Serotonin-1 Agonist EltoprazineNeuropsychopharmacology, 1993
- Differentiation of 8-OH-DPAT and Ipsapirone in Rat Models of 5-HT1A Receptor FunctionPublished by Springer Nature ,1991
- Functional role of 5-HT2 receptors in the regulation of sleep and wakefulness in the ratPsychopharmacology, 1989
- α2-adrenoceptor antagonist activity may account for the effects of buspirone in an anticonflict test in the ratEuropean Journal of Pharmacology, 1988
- Animal models of anxiety: the effect of compounds that modify 5-HT neurotransmissionTrends in Pharmacological Sciences, 1987
- Piperazine derivatives including the putative anxiolytic drugs, buspirone and ipsapirone, are agonists at 5-HT1A receptors negatively coupled with adenylate cyclase in hippocampal neuronsNaunyn-Schmiedebergs Archiv für experimentelle Pathologie und Pharmakologie, 1987
- 8-OH-DPAT is a strong antagonist of 5-HT action in rat hippocampusEuropean Journal of Pharmacology, 1986
- The effects of a 5-HT1 receptor ligand isapirone (TVX Q 7821) on 5-HT synthesis and the behavioural effects of 5-HT agonists in mice and ratsPsychopharmacology, 1986
- Identification and quantitation of 1-(2-pyrimidinyl)piperazine, an active metabolite of the anxiolytic agent buspirone, in rat plasma and brainJournal of Chromatography A, 1982