Zuclopenthixol

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Zuclopenthixol 是一种噻吨，其治疗作用与吩噻嗪类抗精神病药相似。它是 D1 和 D2 多巴胺受体的拮抗剂。

Zuclopenthixol, also known as Cisordinol, Clopixol, Acuphase, zuclopentixol, is a typical antipsychotic drug of the thioxanthene class. It was introduced in 1962 by Lundbeck. Zuclopenthixol is the cis-isomer of clopenthixol. Zuclopenthixol is not approved for use in the United States. Zuclopenthixol has high affinity for both dopamine D1 and D2 receptors, for α1-adrenoceptors and 5-HT2 receptors but no affinity for cholinergic muscarine receptors. It has weak histamine (H1) receptor affinity and no α2-adrenoceptor blocking activity.(In Vivo):After acute treatment, Zuclopenthixol (0.2 and 0.4 mg/kg)-treated animals exhibit ethopharmacological profiles characterized by a decrease in offensive behaviors without impairment of motor activity (0.2 mg/kg). In contrast, the antiaggressive action of the highest dose used (0.4 mg/kg) is accompanied by a marked increase of immobility. After subchronic treatment, no tolerance to Zuclopenthixol antiaggressive or motor activity is observed.Administration of Zuclopenthixol (0.7 and 1.4 mg/kg) significantly elevate MDA level compared to respective controls. Nevertheless, there is no difference between the two dose levels with respect to their effect on rat brain MDA level. Post hoc pairwise comparisons between the means of groups (n=12) receiving different dose levels of Zuclopenthixol reveal that administration of 1.4 mg/kg of Zuclopenthixol significantly reduces GSH level compared to both vehicle-treated and Zuclopenthixol (0.7 mg/kg)-treated animals (P<0.001). Nevertheless, the lower dose of the drug does not affect rat brain GSH level. Animals receiving 0.7 or 1.4 mg/kg of Zuclopenthixol exhibits significantly higher GSH levels than SCO treated animals. Administration of 0.7 mg/kg of Zuclopenthixol significantly elevated GSHPx activity compared to vehicle treated animals.

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After acute treatment, Zuclopenthixol (0.2 and 0.4 mg/kg)-treated animals exhibit ethopharmacological profiles characterized by a decrease in offensive behaviors without impairment of motor activity (0.2 mg/kg). In contrast, the antiaggressive action of the highest dose used (0.4 mg/kg) is accompanied by a marked increase of immobility. After subchronic treatment, no tolerance to Zuclopenthixol antiaggressive or motor activity is observed. Administration of Zuclopenthixol (0.7 and 1.4 mg/kg) significantly elevate MDA level compared to respective controls. Nevertheless, there is no difference between the two dose levels with respect to their effect on rat brain MDA level. Post hoc pairwise comparisons between the means of groups (n=12) receiving different dose levels of Zuclopenthixol reveal that administration of 1.4 mg/kg of Zuclopenthixol significantly reduces GSH level compared to both vehicle-treated and Zuclopenthixol (0.7 mg/kg)-treated animals (P<0.001). Nevertheless, the lower dose of the drug does not affect rat brain GSH level. Animals receiving 0.7 or 1.4 mg/kg of Zuclopenthixol exhibits significantly higher GSH levels than SCO treated animals. Administration of 0.7 mg/kg of Zuclopenthixol significantly elevated GSHPx activity compared to vehicle treated animals.

alpha-Clopenthixol | Clopenthixol | Zuclopenthixol

Others

Other Targets

D1| D2

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53772-83-1

400.96

C22H25ClN2OS

>98% (HPLC)

DMSO : ≥ 150 mg/mL; 374.10 mM

C1CN(CCN1CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl)CCO

2-[4-[(3Z)-3-(2-chlorothioxanthen-9-ylidene)propyl]piperazin-1-yl]ethanol

(-20℃)

With Ice Pack

≥ 2 years