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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-EMD-281014
EMD-281014

Chemical Structure : EMD-281014

CAS No.: 443144-26-1

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EMD-281014 (Pruvanserin, LSN2411347, LY-2422347, EMD281014)

货号: PC-35383Not For Human Use, Lab Use Only.

EMD-281014 (Pruvanserin, LSN2411347, LY-2422347) is a potent, highly selective 5-HT2A antagonist with Ki of 0.87 nM, displays little to no affinity for 5-HT2C receptors (Ki=557 nM), human D2 receptors and IKr channels.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    EMD-281014 (Pruvanserin, LSN2411347, LY-2422347) is a potent, highly selective 5-HT2A antagonist with Ki of 0.87 nM, displays little to no affinity for 5-HT2C receptors (Ki=557 nM), human D2 receptors and IKr channels.
    EMD-281014 significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced swim test.
    EMD-281014 reduces dyskinesia and psychosis in the l-DOPA-treated parkinsonian marmoset.

    物理化学性质&存储条件

    分子量 376.435
    分子式 C22H21FN4O
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    7-[[4-[2-(4-Fluorophenyl)ethyl]-1-piperazinyl]carbonyl]-1H-indole-3-carbonitrile

    参考文献

    1. Hamadjida A, et al. Neuropharmacology. 2018 Jun 30;139:61-67.

    2. Lauffer L, et al. J Pharmacol Exp Ther. 2016 Jul;358(1):39-49.

    3. Patel JG, et al. Synapse. 2004 Apr;52(1):73-5.

    4. Ladduwahetty T, et al. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3201-4.

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