Brexpiprazole I: In Vitro and In Vivo Characterization of a Novel Serotonin-Dopamine Activity Modulator
@article{Maeda2014BrexpiprazoleII, title={Brexpiprazole I: In Vitro and In Vivo Characterization of a Novel Serotonin-Dopamine Activity Modulator}, author={Kenji Maeda and Haruhiko Sugino and Hitomi Akazawa and Naoki Amada and Jun Shimada and Takashi Futamura and Hiroshi Yamashita and Nobuaki Ito and Robert Mcquade and Arne M{\o}rk and Alan L Pehrson and Morten Hentzer and Vibeke Nielsen and Christoffer Bundgaard and J{\o}rn Arnt and Tine Bryan Stensb{\o}l and Tetsuro Kikuchi}, journal={The Journal of Pharmacology and Experimental Therapeutics}, year={2014}, volume={350}, pages={589 - 604} }
Brexpiprazole (OPC-34712, 7-{4-[4-(1-benzothiophen-4-yl)piperazin-1-yl]butoxy}quinolin-2(1H)-one) is a novel drug candidate in clinical development for psychiatric disorders with high affinity for serotonin, dopamine, and noradrenaline receptors. In particular, it bound with high affinity (Ki < 1 nM) to human serotonin 1A (h5-HT1A)-, h5-HT2A-, long form of human D2 (hD2L)-, hα1B-, and hα2C-adrenergic receptors. It displayed partial agonism at h5-HT1A and hD2 receptors in cloned receptor systems…
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The results indicate that brexpiprazole has antipsychotic-like activity and robust efficacy in relevant models of cognitive impairment associated with schizophrenia, and the pharmacologic profile of brexpIPrazole is proposed to be based on its balanced effects on 5-HT1A, D2, and 5- HT2A receptors, with possible modulating activity through additional monoamine receptors.
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