延胡索乙素 T2714

Product Introduction
Bioactivity


英文名: L-(R,S)-Tetrahydropalmatine

描述: L-(R,S)-Tetrahydropalmatine (Rotundine) 是从延胡索 W. T. Wang 中提取的。

体外活性: Rotundine displays a higher affinity to dopamine D1 than D2 receptor with Ki of 124 nM and 388 nM, respectively, while the IC50 values are 166 nM (D1) and 1.47 μM (D2), respectively. Rotundine exhibits a weak inhibitory activity against dopamine D3 with IC50 of 3.25 μM. Rotundine also potently inhibits 5-HT1A with IC50 of 374 nM and Ki of 340 nM. In addition to the antagonism of postsynaptic dopamine receptors, inhibition of presynaptic autoreceptors by Rotundine leads to increased dopamine release, which is probably attributed to lower affinity of Rotundine for D2 receptors. Along with dopamine receptors, Rotundine can interact with a number of other receptor types, including α-1 adrenergic receptors, at which it functions as an antagonist, and γ-aminobutyric acid receptors, at which it facilitates γ-aminobutyric acid binding through positive allosteric effects. [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 55 mg/mL (154.74 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: Rotundine | TETRAHYDROPALMATINE Hydrochloride | L-Tetrahydropalmatine

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