Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities

…, V Lacharme, A Newman-Tancredi…

Index: Cuisiat, Stephane; Bourdiol, Nathalie; Lacharme, Vincent; Newman-Tancredi, Adrian; Colpaert, Francis; Vacher, Bernard Journal of Medicinal Chemistry, 2007 , vol. 50, # 4 p. 865 - 876

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Citation Number: 47

Abstract

We report the discovery and the synthesis of novel, potential antipsychotic compounds combining potent dopamine D2 receptor antagonist and serotonin 5-HT1A receptor agonist properties in the same molecule. We describe the structure-activity relationship that lead us to the promising derivative: N-[(2, 2-dimethyl-2, 3-dihydro-benzofuran-7-yloxy) ethyl]-3- (cyclopent-1-enyl)-benzylamine 16. The latter has high affinity for D2 and 5-HT1A ...