甲氯噻嗪

甲氯噻嗪用途

Methyclothiazide 是一种口服降压试剂 (antihypertensive) 和利尿剂 (diuretic agent)。Methyclothiazide 减少内源性血管收缩刺激 (如,去甲肾上腺素: HY-13715) 引起的血管反应。Methyclothiazide 拮抗体外的电压依赖性钙通道的 (VDCC) 活性。

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甲氯噻嗪名称

[ CAS 号 ]:
135-07-9

[ 中文名 ]:
甲氯噻嗪

[ 英文名 ]:
Methyclothiazide

[中文别名 ]:

[英文别名 ]:

Methycyclothiazide
methyl chlothiazide
EINECS 205-172-2
Enduronum
Enduron
UNII:L3H46UAC61
Aquatensen
Duretic
methylclothiazide
methychlothiazide

甲氯噻嗪生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> 代谢酶/蛋白酶 >> 碳酸酐酶

研究领域 >> 代谢疾病

[ 靶点 ]

IC50: voltage-dependent Ca-channel (VDCC)

[体外研究]

甲环噻嗪(0-100μM)仅在SHR的主动脉中诱导内皮依赖性抑制NE和AVP的血管收缩反应,去甲肾上腺素(HY-13715)和精氨酸加压素(AVP)的最大血管收缩作用分别降低59%和32.3%。甲环噻嗪(0-100μM)对去甲肾上腺素(HY-13715)的收缩反应有抑制作用,N-硝基-L-精氨酸(NOLA)可阻断HY-13715,但不能抑制消炎痛[1]。甲环噻嗪(100μM)在高K+去极化条件下影响血管对细胞外Ca2+的反应。在高K+,无Ca2+溶液中,它能减少Ca2+挛缩。最大挛缩减少90.4%[1]。

[参考文献]

[1]. Colas, B., et al., Mechanisms of methyclothiazide-induced inhibition of contractile responses in rat aorta. Eur J Pharmacol, 2000. 408(1): p. 63-7.

[2]. Colas, B., et al., Direct vascular actions of methyclothiazide and indapamide in aorta of spontaneously hypertensive rats. Fundam Clin Pharmacol, 2000. 14(4): p. 363-8.

[3]. Sasaki, S. and R.D. Bunag, Methyclothiazide attenuates salt-induced hypertension without affecting sympathetic responsiveness in Dahl rats. J Cardiovasc Pharmacol, 1983. 5(3): p. 378-83.

甲氯噻嗪物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
597.9±60.0 °C at 760 mmHg

[ 熔点 ]:
223-225ºC

[ 分子式 ]:
C₉H₁₁Cl₂N₃O₄S₂

[ 分子量 ]:
360.237

[ 闪点 ]:
315.4±32.9 °C

[ 精确质量 ]:
358.956787

[ PSA ]:
126.33000

[ LogP ]:
1.76

[ 外观性状 ]:
白色晶体粉末

[ 蒸汽压 ]:
0.0±1.7 mmHg at 25°C

[ 折射率 ]:
1.606

[ 储存条件 ]:
-20℃

甲氯噻嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DK8575000

CHEMICAL NAME :: 2H-1,2,4-Benzothiadiazine-7-sulfonamide, 6-chloro-3-(chloromethyl)-3,4-dihydro-, 1,1-dioxide

CAS REGISTRY NUMBER :: 135-07-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C9-H11-Cl2-N3-O4-S2

MOLECULAR WEIGHT :: 360.25

WISWESSER LINE NOTATION :: T66 BSWN EM DHJ C1 D1G HG ISZW

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 :: >4 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 870 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Rodent - hamster Lung

DOSE/DURATION :: 140 mg/L

REFERENCE :: GMCRDC Gann Monograph on Cancer Research. (Plenum Pub. Corp., 233 Spring St., New York, NY 10013) No. 11- 1971- Volume(issue)/page/year: 27,95,1981 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X9137 No. of Facilities: 54 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 859 (estimated) No. of Female Employees: 574 (estimated)

甲氯噻嗪

甲氯噻嗪用途

甲氯噻嗪名称

甲氯噻嗪生物活性

甲氯噻嗪物理化学性质

甲氯噻嗪毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

甲氯噻嗪安全信息

甲氯噻嗪合成路线

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