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• W2013688328 abstract "The neurochemical profile of the selective 5-HT1AreceptorantagonistWAY100135 [N-tert-butyl 3-4-(2-methoxyphenyl) piperazin-1-yl-2-phenylpropanamidedihydrochloride] anditsenantiomersatthesomatodenditic 5-HT1A eceptor was determined by studying the effects of these compounds on 5-HT (5-hydroxytryptamine, serotonin) release in the rat hippocampus using in vivo microdialysis. (±)-WAY100135, (+)-WAY100135 and (−)-WAY100135 (all at 10 mg/kg s.c.) had no significant effect on extracellular levels of 5-HT in the hippocampus demonstrating that these compounds are devoid of 5-HT1A receptor agonist properties. In contrast, the 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) (0.1 mg/kg s.c.) and the partial agonists BMY 7378 (1.0 mg/kg s.c.) and buspirone (5 mg/kg s.c.) significantly decreased hippocampal 5-HT. Pretreatment with (±)-WAY100135 (at 10 mg/kg s.c.) and (+)-WAY100135 (at 1.0–10 mg/kg s.c.) completely blocked the 8-OH-DPAT-induced decrease in 5-HT release demonstrating that these compounds are antagonists at the somatodendritic 5-HT1Aautoreceptor. (−)-WAY100135 atadoseof 10 mg/kgs.c. hadnosignificanteffectonthe 8-OH-DPAT-inducedinhibitionof 5-HTrelease.(±)-WAY100135 had no significant effect on extracellular levels of dopamine in the rat hippocampus but significantly increased extracellular levels of noradrenaline. The mechanism underlying the increase in noradrenaline is unknown at present. These data suggest that WAY100135 is a silent and selective receptor antagonist at the somatodendritic 5-HT1A receptor with activity residing in the (+)-enantiomer. In addition, these findings confirm that WAY100135 is likely to be a useful tool for further investigation of 5-HT1A receptor function." @default.
• W2013688328 created "2016-06-24" @default.
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• W2013688328 date "1993-08-01" @default.
• W2013688328 modified "2023-09-23" @default.
• W2013688328 title "Neurochemical profile of the selective and silent 5-HT1A receptor antagonist WAY100135: an in vivo microdialysis study" @default.
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• W2013688328 doi "https://doi.org/10.1016/0014-2999(93)90994-s" @default.
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