Methiothepin (maleate)

Methiothepin (maleate)用途

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)。

Methiothepin (maleate)名称

[ CAS 号 ]:
19728-88-2

[ 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

Methiothepin (maleate)生物活性

[ 描述 ]:

[ 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.

Methiothepin (maleate)物理化学性质

[ 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

Methiothepin (maleate)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