EFFECTS OF IPSAPIRONE, A 5-HT(1A) AGONIST, ON SLEEP-WAKEFULNESS CYCLES - PROBABLE POSTSYNAPTIC ACTION

被引:53
作者
TISSIER, MH [1 ]
LAINEY, E [1 ]
FATTACCINI, CM [1 ]
HAMON, M [1 ]
ADRIEN, J [1 ]
机构
[1] CHU PITIE SALPETRIERE, INSERM, U288, F-75634 PARIS 13, FRANCE
关键词
SHT RECEPTORS; SEROTONIN; SLEEP WAKEFULNESS;
D O I
10.1111/j.1365-2869.1993.tb00070.x
中图分类号
R74 [神经病学与精神病学];
学科分类号
摘要
The effects of ipsapirone, a ligand of the 5-HT1A receptors 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-HT1A agonist ipsapirone on sleep/wakefulness cycles probably involves the stimulation of the post-synaptic 5-HT1A receptors.
引用
收藏
页码:103 / 109
页数:7
相关论文
共 39 条
[1]  
ADRIEN J, 1990, SLEEP 90, P123
[2]   THE ALPHA2-ADRENOCEPTOR ANTAGONIST ACTIVITY OF IPSAPIRONE AND GEPIRONE IS MEDIATED BY THEIR COMMON METABOLITE 1-(2-PYRIMIDINYL)-PIPERAZINE (PMP) [J].
BIANCHI, G ;
CACCIA, S ;
DELLAVEDOVA, F ;
GARATTINI, S .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1988, 151 (03) :365-371
[3]  
BOCKAERT J, 1987, N-S ARCH PHARMACOL, V335, P588
[4]   IDENTIFICATION AND QUANTITATION OF 1-(2-PYRIMIDINYL)PIPERAZINE, AN ACTIVE METABOLITE OF THE ANXIOLYTIC AGENT BUSPIRONE, IN RAT PLASMA AND BRAIN [J].
CACCIA, S ;
GARATTINI, S ;
MANCINELLI, A ;
MUGLIA, M .
JOURNAL OF CHROMATOGRAPHY, 1982, 252 (DEC) :310-314
[5]   ANIMAL-MODELS OF ANXIETY - THE EFFECT OF COMPOUNDS THAT MODIFY 5-HT NEUROTRANSMISSION [J].
CHOPIN, P ;
BRILEY, M .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1987, 8 (10) :383-388
[6]   8-OH-DPAT IS A STRONG ANTAGONIST OF 5-HT ACTION IN RAT HIPPOCAMPUS [J].
COLINO, A ;
HALLIWELL, JV .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1986, 130 (1-2) :151-152
[7]  
DEPOORTERE H, 1988, SLEEP 86, P346
[8]  
Dourish C.T., 1987, BRAIN 5 HT1A RECEPTO, P261
[9]   FUNCTIONAL-ROLE OF 5-HT2 RECEPTORS IN THE REGULATION OF SLEEP AND WAKEFULNESS IN THE RAT [J].
DUGOVIC, C ;
WAUQUIER, A ;
LEYSEN, JE ;
MARRANNES, R ;
JANSSEN, PAJ .
PSYCHOPHARMACOLOGY, 1989, 97 (04) :436-442
[10]  
DZOLJIC MR, 1987, SLEEP RES, V16, P88