19728-88-2

• 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)。

名称

• 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

物化性质

• 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

生物活性

• 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:
  研究领域 >> 神经疾病
  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
• 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.

毒性和生态

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