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Zolantidine dimaleate

Zolantidine dimaleate用途

二马来酸唑安定(SKF 95282二马来酸)是一种强效、选择性和跨血脑屏障组胺H2拮抗剂。二马来酸左安定诱导镇痛感受[1][2]。

Zolantidine dimaleate名称

[ CAS 号 ]:
104076-39-3

[ 英文名 ]:
Zolantidine dimaleate

[英文别名 ]:

AL1YII70LM
Zolantidine dimaleate
SKF 95282 dimaleate
SKF-95282 dimaleate salt

Zolantidine dimaleate生物活性

[ 描述 ]:

二马来酸唑安定(SKF 95282二马来酸)是一种强效、选择性和跨血脑屏障组胺H2拮抗剂。二马来酸左安定诱导镇痛感受[1][2]。

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[ 靶点 ]

H2 Receptor

[体内研究]

二马来酸左安定(5、10、20、40mg/kg皮下注射) 在胆汁淤积大鼠中诱导抗伤害作用[2] 动物模型：200-250g,雄性Wistar大鼠(胆汁淤积大鼠)[2]剂量：5、10、20、40mg/kg给药：S.c.结果：甩尾潜伏期显著增加,并诱导镇痛感受。

[参考文献]

[1]. Calcutt CR, et al. Zolantidine (SK&F 95282) is a potent selective brain-penetrating histamine H2-receptor antagonist. Br J Pharmacol. 1988 Jan;93(1):69-78.

[2]. Hasanein P. Two histamine H2 receptor antagonists, zolantidine and cimetidine, modulate nociception in cholestatic rats. J Psychopharmacol. 2011 Feb;25(2):281-8.

Zolantidine dimaleate物理化学性质

[ 分子式 ]:
C₃₀H₃₅N₃O₉S

[ 分子量 ]:
613.68

[ 精确质量 ]:
613.209412

Zolantidine dimaleate安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

Zolantidine dimaleate文献

Zolantidine (SK&F 95282) is a potent selective brain-penetrating histamine H2-receptor antagonist.

Br. J. Pharmacol. 93(1) , 69-78, (1988)

1. The novel benzthiazole derivative zolantidine (SK&F 95282) is a potent antagonist of histamine at H2-receptors in guinea-pig atrium and rat uterus. Only apparent pA2 values of 7.46 and 7.26 respect...

Linking solubility and permeability assays for maximum throughput and reproducibility.

J. Biomol. Screen. 10(4) , 383-90, (2005)

Solubility and permeability are intimately linked in drug absorption processes. They have, however, been traditionally assayed separately. To support this linkage, a combined solubility/permeability a...

Identification of novel functional inhibitors of acid sphingomyelinase.

PLoS ONE 6 , e23852, (2011)

We describe a hitherto unknown feature for 27 small drug-like molecules, namely functional inhibition of acid sphingomyelinase (ASM). These entities named FIASMAs (Functional Inhibitors of Acid Sphing...

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