Loxapine hydrochloride

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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。

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 K_ivalue 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.