Eplivanserin hemifumarate

Pricing Availability   Qty
说明: Potent and selective 5-HT2A antagonist
别名: SR-46349 hemifumarate,SR-46349B
化学名: (1Z,2E)-1-(2-Fluorophenyl)-3-(4-hydroxyphenyl)-2-propen-1-one O-[2-(dimethylamino)ethyl]oxime hemifumarate
纯度: ≥98% (HPLC)
说明书
引用文献
评论 (1)
文献 (3)

生物活性 for Eplivanserin hemifumarate

Eplivanserin 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.

技术数据 for Eplivanserin hemifumarate

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.

溶解性数据 for Eplivanserin hemifumarate

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 19.32 50

制备储备液 for Eplivanserin hemifumarate

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.

选择批次从而根据批次分子量重新计算:
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

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产品说明书 for Eplivanserin hemifumarate

参考文献 for Eplivanserin hemifumarate

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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Eplivanserin hemifumarate blocks MDMA-induced striatal activation and locomotion.
By Kevin Ball on 01/25/2019
分析类型: In Vivo
种属: Rat

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).

PMID: 16001122 参考文献
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