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135-07-9生产厂家

135-07-9价格

135-07-9

135-07-9结构式
135-07-9结构式
  • 常用中文名:甲氯噻嗪
  • 常用英文名:Methyclothiazide
  • CAS号:135-07-9
  • 分子式:C9H11Cl2N3O4S2
  • 分子量:360.237
  • 相关类别: 原料药 泌尿系统用药 利尿药
  • 发布时间:2018-06-18 13:32:24
  • 更新时间:2024-01-08 18:57:17
  • 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。

化源商城直购

中文名 甲氯噻嗪
英文名 6-chloro-3-(chloromethyl)-2-methyl-1,1-dioxo-3,4-dihydro-1λ6,2,4-benzothiadiazine-7-sulfonamide
中文别名 6-氯-3-氯甲基-3,4-二氢-2-甲基-2H-1,2,4-苯并噻二嗪-7-磺酰胺 1,1-二氧化物
英文别名 Methycyclothiazide
6-chloro-3-(chloromethyl)-3,4-dihydro-2-methyl-2H-1,2,4-benzothiadiazine-7-sulfonamide-1,1-di-oxide
6-Chloro-3-(chloromethyl)-2-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
methyl chlothiazide
EINECS 205-172-2
Enduronum
Enduron
UNII:L3H46UAC61
Aquatensen
Duretic
methylclothiazide
6-chloro-3-(chlorométhyl)-2-méthyl-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide-1,1-dioxyde
2H-1,2,4-Benzothiadiazine-7-sulfonamide, 6-chloro-3-(chloromethyl)-3,4-dihydro-2-methyl-, 1,1-dioxide
methychlothiazide
methyclothiazide
Aquaresen
Naturon
MFCD00242610
Methyclothiazid
描述 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。
相关类别
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.

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℃
分子结构

分子性质数据:

1、 摩尔折射率:77.02

2、 摩尔体积(m3/mol):223.2

3、 等张比容(90.2K):608.4

4、 表面张力(3.0 dyne/cm):55.1

5、 极化率(0.5 10 -24cm 3):30.53

计算化学

1.疏水参数计算参考值(XlogP):无

2.氢键供体数量:2

3.氢键受体数量:7

4.可旋转化学键数量:2

5.互变异构体数量:无

6.拓扑分子极性表面积126

7.重原子数量:20

8.表面电荷:0

9.复杂度:571

10.同位素原子数量:0

11.确定原子立构中心数量:0

12.不确定原子立构中心数量:1

13.确定化学键立构中心数量:0

14.不确定化学键立构中心数量:0

15.共价键单元数量:1

毒理学数据:

急性毒性数据:

大鼠经口LD50:>4mg/kg

大鼠腹腔LD50:2mg/kg

小鼠经口LD50:>10mg/kg

小鼠腹腔LD50:870mg/kg

小鼠静脉LD50:400mg/kg

致突变数据:

仓鼠成纤维细胞:250mg/L

仓鼠肺:140mg/L

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)

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