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19728-88-2生产厂家

19728-88-2价格

19728-88-2

19728-88-2结构式
19728-88-2结构式
  • 常用中文名:Methiothepin (maleate)
  • 常用英文名:Methiothepin Maleate
  • CAS号:19728-88-2
  • 分子式:C24H28N2O4S2
  • 分子量:472.62
  • 相关类别: 信号通路 G 蛋白偶联受体/G 蛋白 5-HT受体
  • 发布时间:2017-02-01 08:26:18
  • 更新时间:2024-01-02 21:07:28
  • 马来酸甲硫氨酸是一种有效的非选择性5-HT2受体拮抗剂,pKds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),pKis为8.50(5HT2A)、8.68(5HT2B)和8.35(5HT2C)。

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中文名 马来酸甲硫基西平
英文名 methiothepin maleate
英文别名 methiothepin hydrogen maleate
N6-Cyclopentyladenosine
Metitepine maleate
metitepinmaleate
METHIOTHEPIN MALEATE
描述 马来酸甲硫氨酸是一种有效的非选择性5-HT2受体拮抗剂,pKds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),pKis为8.50(5HT2A)、8.68(5HT2B)和8.35(5HT2C)。
相关类别
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 马来酸甲硫氨酸是一种5-HT受体拮抗剂,5-HT1A、5HT1B、5HT1C、5HT1D[1]的pKds分别为7.10、7.28、7.56和6.99。甲磺酸甲硫庚平还显示5-HT5A、5-HT5B、5-HT6和5-HT7的pKds分别为7.0、7.8、8.74和8.99[2]。甲硫氨酸对5-HT2A、5HT2B和5HT2C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.  

沸点 462.9ºC at 760mmHg
分子式 C24H28N2O4S2
分子量 472.62
闪点 233.8ºC
精确质量 472.14900
PSA 131.68000
LogP 3.99190
蒸汽压 3.61E-08mmHg at 25°C
储存条件 -20°C,密闭,干燥

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TL4325000
CAS REGISTRY NUMBER :
19728-88-2
LAST UPDATED :
198706
DATA ITEMS CITED :
2
MOLECULAR FORMULA :
C20-H24-N2-S2.C4-H4-O4
MOLECULAR WEIGHT :
472.66
WISWESSER LINE NOTATION :
T C676 BS&T&J FS1 I- AT6N DNTJ D1 &QV1U1VQ -C

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
125 mg/kg
TOXIC EFFECTS :
Behavioral - ataxia
REFERENCE :
CCCCAK Collection of Czechoslovak Chemical Communications. (Academic Press Inc. Ltd., 24-28 Oval Rd., London NW1 7DX, UK) V.1- 1929- Volume(issue)/page/year: 39,3338,1974
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
67600 ug/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
REFERENCE :
CCCCAK Collection of Czechoslovak Chemical Communications. (Academic Press Inc. Ltd., 24-28 Oval Rd., London NW1 7DX, UK) V.1- 1929- Volume(issue)/page/year: 39,3153,1974