130579-75-8
130579-75-8
Chemical Structure
Eplivanserin
Synonym(s): SR-46349
- CAS 番号: 130579-75-8
- Formula:C19H21FN2O2
- Molecular Weight:328.39
IUPAC Name: (1Z,2E)-1-(2-fluorophenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one O-(2-(dimethylamino)ethyl) oxime
InChIKey: VAIOZOCLKVMIMN-PRJWTAEASA-N
SMILES: OC1=CC=C(/C=C/C(C2=CC=CC=C2F)=N/OCCN(C)C)C=C1
Biological Activity: Eplivanserin (SR-46349) is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C[1][2].
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Eplivanserin | Eplivanserin (SR-46349) is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C. | |||||||||||||||||||||
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References
- [1]. Rinaldi-Carmona M, et al. Biochemical and pharmacological properties of SR 46349B, a new potent and selective 5-hydroxytryptamine2 receptor antagonist. J Pharmacol Exp Ther. 1992 Aug;262(2):759-68. [Content Brief]
- [2]. Malgorzata Filip, et al. 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. 2004 Sep;310(3):1246-54. [Content Brief]
