美噻吨盐酸盐

美噻吨盐酸盐用途

Metixene hydrochloride 是一种抗胆碱能、抗帕金森剂,能够有效抑制二苯羟乙酸奎宁酯与毒蕈碱受体 (muscarinic receptor) 结合,IC50 和 Kd 值分别为 55 nM 和 15 nM。

美噻吨盐酸盐名称

[ CAS 号 ]:
1553-34-0

[ 中文名 ]:
美噻吨盐酸盐

[ 英文名 ]:
Metixene hydrochloride

[英文别名 ]:

美噻吨盐酸盐生物活性

[ 描述 ]:

Metixene hydrochloride 是一种抗胆碱能、抗帕金森剂,能够有效抑制二苯羟乙酸奎宁酯与毒蕈碱受体 (muscarinic receptor) 结合,IC50 和 Kd 值分别为 55 nM 和 15 nM。

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> mAChR
信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR
研究领域 >> 神经疾病

[ 靶点 ]

IC50: 55 nM (mAChR)[1] Ki: 15 nM (mAChR)[1]


[参考文献]

[1]. Syvälahti EK, et al. Effects of antiparkinsonian drugs on muscarinic receptor binding in rat brain, heart and lung. Pharmacol Toxicol. 1988 Feb;62(2):90-4.

美噻吨盐酸盐物理化学性质

[ 沸点 ]:
419.7ºC at 760 mmHg

[ 分子式 ]:
C20H24ClNS

[ 分子量 ]:
345.93

[ 闪点 ]:
207.6ºC

[ 精确质量 ]:
345.13200

[ PSA ]:
28.54000

[ LogP ]:
5.75490

[ 蒸汽压 ]:
2.99E-07mmHg at 25°C

美噻吨盐酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TN1944000
CHEMICAL NAME :
Piperidine, 1-methyl-3-(thioxanthen-9-ylmethyl)-, hydrochloride
CAS REGISTRY NUMBER :
1553-34-0
LAST UPDATED :
198812
DATA ITEMS CITED :
8
MOLECULAR FORMULA :
C20-H23-N-S.Cl-H
MOLECULAR WEIGHT :
345.96
WISWESSER LINE NOTATION :
T C666 BS IHJ I1- CT6NTJ A1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1460 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,824,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
295 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,824,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1519 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,824,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
24 mg/kg
TOXIC EFFECTS :
Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay)
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 141,331,1963
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
346 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,824,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
108 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,824,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
238 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,824,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
18 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JPMSAE Journal of Pharmaceutical Sciences. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.50- 1961- Volume(issue)/page/year: 63,568,1964

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