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Brexpiprazole 913611-97-9
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C25H27N3O2S |
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433.57 |
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913611-97-9 |
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Introduction
Brexpiprazole is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors.
Brexpiprazole is a potent partial agonist at human 5-hydroxytryptamine (5-HT) 5-HT1A (Ki=0.12 nM) and dopamine D2L (Ki=0.3 nM) receptors, and an antagonist at 5-HT2A receptors (Ki=0.47 nM). It also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2Creceptors (Ki=0.59 nM). Furthermore, this drug displays moderate affinity for human D3, 5-HT2B and 5-HT7 receptors, as well as α1A, and α1D adrenergic receptors. Brexpiprazole potentiated NGF-induced neurite outgrowth in PC12 cells. It could significantly potentiate the effects of fluoxetine (or paroxetine) on neurite outgrowth.
Brexpiprazole is a potent partial agonist at human 5-hydroxytryptamine (5-HT) 5-HT1A (Ki=0.12 nM) and dopamine D2L (Ki=0.3 nM) receptors, and an antagonist at 5-HT2A receptors (Ki=0.47 nM). It also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2Creceptors (Ki=0.59 nM). Furthermore, this drug displays moderate affinity for human D3, 5-HT2B and 5-HT7 receptors, as well as α1A, and α1D adrenergic receptors. Brexpiprazole potentiated NGF-induced neurite outgrowth in PC12 cells. It could significantly potentiate the effects of fluoxetine (or paroxetine) on neurite outgrowth.