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Submit ReviewEplivanserin hemifumarate is a 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.
分子量 | 386.42 |
公式 | C19H21FN2O2.0.5C4H4O4 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 130580-02-8 |
PubChem ID | 6438382 |
InChI Key | UCLIFEBROADCQW-PWERMGERSA-N |
Smiles | OC(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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 19.32 | 50 |
以下数据基于产品分子量 386.42。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 5.18 mL | 25.88 mL | 51.76 mL |
2.5 mM | 1.04 mL | 5.18 mL | 10.35 mL |
5 mM | 0.52 mL | 2.59 mL | 5.18 mL |
25 mM | 0.1 mL | 0.52 mL | 1.04 mL |
参考文献是支持产品生物活性的出版物。
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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关键词: Eplivanserin hemifumarate, Eplivanserin hemifumarate supplier, antipsychotic, potent, selective, 5-HT2A, antagonist, SR-46349, hemifumarate, SR-46349B, Receptors, 4958, Tocris Bioscience
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We assessed the effect of the 5-HT2A antagonist, SR-46349B (eplivanserin hemifumarate; 0.5 mg/kg, s.c.), on MDMA (ecstasy)-induced locomotion and dorsal striatal single-unit electrophysiology. SR-46349B blocked nearly all MDMA-induced striatal excitations, which paralleled its significant attenuation of MDMA-induced locomotor activation (shown in figure).
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
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