Methiothepin甲磺酸盐

Methiothepin甲磺酸盐用途

Methiothepin mesylate 是一种有效的,非选择性的 5-HT2 receptor 拮抗剂,pKd 值为 7.10 (5-HT1A),7.28 (5HT1B),7.56 (5HT1C),6.99 (5HT1D),7.0 (5-HT5A),7.8 (5-HT5B),8.74 (5-HT6) 和 8.99 (5-HT7),pKi 值为 8.50 (5HT2A),8.68 (5HT2B) 和 8.35 (5HT2C)。

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Methiothepin甲磺酸盐名称

[ CAS 号 ]:
74611-28-2

[ 中文名 ]:
Methiothepin甲磺酸盐

[ 英文名 ]:
Methiothepin mesylate

[英文别名 ]:

Methiothepin mesylate salt
Methiothepin methanesulfonate
Methiothepin mesylate
Metitepine mesylate salt

Methiothepin甲磺酸盐生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

研究领域 >> 神经疾病

[ 靶点 ]

pKd: 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D)[1], 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), 8.99 (5-HT7)[3] pKi: 8.50 (5-HT2A), 8.68 (5-HT2B), 8.35 (5-HT2C)[2]

[体外研究]

Methiothepin mesylate是一种5-HT受体拮抗剂,5-HT1A,5HT1B,5HT1C,5HT1D的pKds分别为7.10,7.28,7.56和6.99 [1]。 Methiothepin甲磺酸盐还显示5-HT5A,5-HT5B,5-HT6和5-HT7的pKds分别为7.0,7.8,8.74和8.99 [2]。 Methiothepin在5-HT2A,5HT2B和5HT2C上表现出高亲和力,pKis分别为8.50,8.68和8.35 [3]。

[参考文献]

[1]. Schoeffter P, et al. 5-Hydroxytryptamine (5-HT)-induced endothelium-dependent relaxation of pig coronary arteries is mediated by 5-HT receptors similar to the 5-HT1D receptor subtype. J Pharmacol Exp Ther. 1990 Jan;252(1):387-95.

[2]. Knight AR, et al. Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23. Epub 2004 Jul 30.

[3]. Hoyer D, et al. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol Rev. 1994 Jun;46(2):157-203.

[相关活性小分子]

Methiothepin甲磺酸盐物理化学性质

[ 分子式 ]:
C₂₁H₂₈N₂O₃S₃

[ 分子量 ]:
452.65400

[ 精确质量 ]:
452.12600

[ PSA ]:
119.83000

[ LogP ]:
4.86490

[ 储存条件 ]:
2-8℃

Methiothepin甲磺酸盐MSDS

详细MSDS(安全技术说明书)

Methiothepin甲磺酸盐安全信息

[ 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

Methiothepin甲磺酸盐文献

Characterization of the commercially-available fluorescent chloroquine-BODIPY conjugate, LynxTag-CQGREEN, as a marker for chloroquine resistance and uptake in a 96-well plate assay.

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Chloroquine was a cheap, extremely effective drug against Plasmodium falciparum until resistance arose. One approach to reversing resistance is the inhibition of chloroquine efflux from its site of ac...

Functional, endogenously expressed 5-hydroxytryptamine 5-ht7 receptors in human vascular smooth muscle cells.

Br. J. Pharmacol. 117 , 993-994, (1996)

Human uterine artery smooth muscle cells in culture were shown to express constitutively both 5-ht7 receptor mRNA and 5-ht7-like receptors functionally linked to cyclic AMP formation. 5-Carboxamidotry...

Characterisation of 5-HT receptors in human coronary arteries by molecular and pharmacological techniques.

Eur. J. Pharmacol. 372 , 49-56, (1999)

5-Hydroxytryptamine (5-HT) can produce both vasoconstrictor and vasorelaxant effects in human coronary arteries and the response to 5-HT can be influenced by the presence of disease. The aim of the pr...

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