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首页-小分子抑制剂&激动剂-GPCR-Dopamine Receptor-Trazpiroben
Trazpiroben

Chemical Structure : Trazpiroben

CAS No.: 2250200-57-6

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Trazpiroben (TAK-906, TAK906)

货号: PC-72281Not For Human Use, Lab Use Only.

Trazpiroben (TAK-906) is a potent, peripherally selective D2/D3 dopamine receptor antagonist, moderate affinity for D4, and minimal for D1 and D5.

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

    生物&药学活性

    Trazpiroben (TAK-906) is a potent, peripherally selective D2/D3 dopamine receptor antagonist, moderate affinity for D4, and minimal for D1 and D5.
    Trazpiroben demonstrated the following receptor affinities: high for D2 and D3, moderate for D4, and minimal for D1 and D5, showed moderate affinity for adrenergic α 1B (α 1B) and 5HT)2A receptors and low potential for off-target adverse events (AEs).
    Trazpiroben potently inhibited dopamine-activated D2L receptor activation of cognate G-proteins in human embryonic kidney 293 cell membranes and was a neutral D2L receptor antagonist.
    Trazpiroben dose-dependently increased prolactin release in orally dosed rat (0.1-1 mg/kg).
    Trazpiroben is a potent D2/D3 receptor antagonist designed to avoid the serious potential AEs associated with current gastroparesis.therapies.

    物理化学性质&存储条件

    分子量 633.742
    分子式 C35H43N3O8
    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

    3-((1-cyclohexyl-4-oxo-8-(4-oxo-4-phenylbutyl)-1,3,8-triazaspiro[4.5]decan-3-yl)methyl)benzoic acid compound with maleic acid (1:1)

    参考文献

    1. Whiting RL, et al. J Pharmacol Exp Ther. 2021 Oct;379(1):85-95.

    2. Whiting RL, et al. Clin Pharmacol Drug Dev. 2021 Aug;10(8):927-939.

    3. Kaur Mukker J, et al. Clin Transl Sci. 2022 Feb 26.

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