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抑制剂描述:

产品名称:Chlorpromazine hydrochloride

产品别名:见爱必信官网

英文别名:Chlorpromazine hydrochloride

靶点:5-HT Receptor

CAS:69-09-0

纯度:≥98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Chlorpromazine Hydrochloride 是一种有效的 dopamine D2 受体,5-HT2A 受体,potassium channel,sodium channel 的拮抗剂,抑制 D2 受体和 serotonin 5-HT2A 受体的活性,Ki 值分别为 363 nM 和 8.3 nM。

溶解性:DMSO : 50 mg/mL
Water : 50 mg/mL
Ethanol : 50 mg/mL

体外研究:

Chlorpromazine affects miniature IPSCs (mIPSCs) by decreasing the binding (kon) and by increasing the unbinding (koff) rates of GABAARs. Chlorpromazine modulates activated TRPA1 currents in a voltage-dependent way, leading to a block at positive potentials and an increased open probability at negative potentials.

体内研究:Chlorpromazine independently down-regulates the production of various T cell-derived lymphokines (IL-2, IFN-gamma, IL-4, TNF, and GM-CSF) and up-regulates the secretion of IL-10 in an in vivo model of acute superantigen-driven immune activation. Chlorpromazine -mediated amplification of the SEB-driven Chlorpromazine secretion is accompanied by an enhanced IL-10 mRNA accumulation. Chlorpromazine protects mice, normal or adrenalectomized, and guinea pigs against lethality of LPS, and inhibits TNF serum levels. Chlorpromazine protects against LPS lethality when administered 30 minutes (min) before, simultaneously, or up to 10 min after LPS and is ineffective when given 30 min after LPS, paralleling the inhibitory effect on TNF production. Chlorpromazine significantly inhibits LPS lethality and hepatotoxicity in mice sensitized to LPS toxicity by actinomycin D, whereas under these conditions DEX is inactive. Chlorpromazine protects brain tissue from hypoxia-induced irreversible loss of synaptic transmission in rats. Chlorpromazine also significantly delays the occurrence of the hypoxia-induced spreading depression (SD) in rats.

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