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Eplivanserin hemifumarate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Eplivanserin hemifumarate图片
CAS NO:130580-02-8
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
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。
Cas No.130580-02-8
别名富马酸依利色林,SR-46349 hemifumarate; SR 46349B
Canonical SMILESOC(C=C2)=CC=C2/C=C/C(C1=CC=CC=C1F)=N/OCCN(C)C.O=C(/C=C/C(O)=O)O.OC(C=C4)=CC=C4/C=C/C(C3=CC=CC=C3F)=N/OCCN(C)C
分子式C19H21FN2O2.0.5C4H4O4
分子量386.42
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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