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Loxapine hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Loxapine hydrochloride图片
CAS NO:54810-23-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
盐酸洛沙平
产品介绍
Loxapine hydrochloride 是一种具有口服活性的多巴胺 (dopamine) 抑制剂和5-HT受体拮抗剂,有抗精神病活性。
生物活性

Loxapine hydrochloride is an orally activedopamineinhibitor,5-HT receptorantagonist and also a dibenzoxazepine anti-psychotic agent[1][4].

IC50& Target

human 5-HT2

 

Human D4Receptor

 

Human D1Receptor

 

Human D2Receptor

 

体外研究
(In Vitro)

In the presence of Loxapine, [3H]ketanserin binds to 5-HT2receptor in Frontal cortex of brain in human and bovine with Kivalue of 6.2 nM and 6.6 nM, respectively. Loxapine has the rank order of potency for the various receptors appears to be as follows: 5-HT2≥D4>>>D1>D2in comparing competition experiments involving the human membranes[1].
Loxapine (0-20 μM, 24 h or 72 h) reduces IL-1β secretion by LPS-activated mixed glia cultures, reduces IL-2 secretion in mixed glia cultures, and decreases IL-1β and IL-2 secretion in LPS-induced microglia cultures[2].

体内研究
(In Vivo)

Loxapine (5 mg/kg; i.p.; daily for 4 or 10 weeks) decreases serotonin (S2) but does not elevate dopamine (D2) receptor numbers in the rat brain[3].

Animal Model:Adult male Wistar rats (150-175 g)[3]
Dosage:5 mg/kg
Administration:Intraperitoneal injection, daily for 4 or 10 weeks
Result:Induced a very significant reduction (more than 50%) of serotonin (S2) receptor density after 4 weeks or 10 weeks of daily injection, but did not produce any significant increase in dopamine receptor density.
Clinical Trial
分子量

364.27

Formula

C18H19Cl2N3O

CAS 号

54810-23-0

中文名称

盐酸洛沙平

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.