Eplivanserin (SR-46349) hemifumarate 是一种有效、选择性和口服活性的 5-HT2A 受体拮抗剂，在大鼠皮质膜中的 IC50 为 5.8 nM，Kd 为 1.14 nM。
Potent and selective 5-HT2A antagonist (IC50 values are 5.8 and 120 and >100 nM for 5-HT2A, 5-HT2B and 5-HT2C, respectively). Attenuates cocaine-induced hyperactivity. Increases dopamine (DA) release in rat medial prefrontal cortex (mPFC); potentiates haloperidol-induced DA release in the mPFC and nucleus accumbens.
Yadav et al (2011) Antagonist functional selectivity: 5-HT2A serotonin receptor antagonists differentially regulate 5-HT2A receptor protein level in vivo. J.Pharmacol.Exp.Ther. 339 99 PMID:21737536 |Filip et al (2004) Contribution of serotonin (5-hydroxytryptamine; 5-HT) 5-HT2 receptor subtypes to the hyperlocomotor effects of cocaine: acute and chronic pharmacological analyses. J.Pharmacol.Exp.Ther. 310 1246 PMID:15131246 |Bonaccorso et al (2002) SR46349-B, a 5-HT(2A/2C) receptor antagonist, potentiates haloperidol-induced DA release in rat medial prefrontal cortex and nucleus accumbens. Neuropsychopharmacology. 27 430 PMID:12225700
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