二甲替嗪
二甲替嗪用途
二甲噻嗪(Dimethothiazine,Dimetotiazine；Fonazine)是一种口服活性三环抗组胺、抗5-羟色胺药物,对去脑强直有很高的活性,具有轻微的镇静作用和催眠作用。二甲噻嗪可以减少或消除去脑猫的静态和动态纺丝运动对肌梭的影响。二甲噻嗪可用于研究偏头痛和痉挛[1][2][3]。
二甲替嗪名称
[ CAS 号 ]:
7456-24-8
[ 中文名 ]:
二甲替嗪
[ 英文名 ]:
Dimetotiazine
[英文别名 ]:
- dimethothiazine
- FONAZINE
- Dimetiotazine
- Dimethodin
- Dimetotiazinum [INN-Latin]
- Dimetotiazine
- Dimetotiazine [INN:BAN]
- Bayer 1483
- Dimetotiazina [INN-Spanish]
- Dimetiotazin
二甲替嗪生物活性
[ 描述 ]:
二甲噻嗪(Dimethothiazine,Dimetotiazine；Fonazine)是一种口服活性三环抗组胺、抗5-羟色胺药物,对去脑强直有很高的活性,具有轻微的镇静作用和催眠作用。二甲噻嗪可以减少或消除去脑猫的静态和动态纺丝运动对肌梭的影响。二甲噻嗪可用于研究偏头痛和痉挛[1][2][3]。
[ 相关类别 ]:
[ 靶点 ]
Histamine, 5-HT[1]
[体内研究]
二甲噻嗪(0.5-16 mg/kg；静脉注射；单剂量)可降低猫的去脑强直[2]。动物模型：猫(去脑模型；颈动脉被夹闭,大脑中段大约在丘之间)[2]剂量：0.5、1、2、4、8和16 mg/kg,静脉注射。；单剂量结果：一级和二级终末的放电频率降低了1-4mg/kg。在准备完整的腹根时,降低了肌梭拉伸的敏感性。降低了动态熔断器纤维的活性。
[参考文献]
二甲替嗪物理化学性质
[ 密度 ]:
1.235g/cm3
[ 沸点 ]:
533.7ºC at 760 mmHg
[ 分子式 ]:
C19H25N3O2S2
[ 分子量 ]:
391.55100
[ 闪点 ]:
276.6ºC
[ 精确质量 ]:
391.13900
[ PSA ]:
77.54000
[ LogP ]:
4.63550
[ 折射率 ]:
1.612
二甲替嗪毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- SP5250000
- CHEMICAL NAME :
- Phenothiazine-2-sulfonamide, 10-(2-(dimethylamino)propyl)-N,N-dimethyl-
- CAS REGISTRY NUMBER :
- 7456-24-8
- LAST UPDATED :
- 199612
- DATA ITEMS CITED :
- 5
- MOLECULAR FORMULA :
- C19-H25-N3-O2-S2
- MOLECULAR WEIGHT :
- 391.59
- WISWESSER LINE NOTATION :
- T C666 BN ISJ B1Y1&N1&1 ESWN1&1
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 :
- 740 mg/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes
- 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: 159,70,1966
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 190 mg/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes
- 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: 159,70,1966
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 475 mg/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes
- 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: 159,70,1966
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 100 mg/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes
- 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: 159,70,1966 ** REPRODUCTIVE DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 600 mg/kg
- SEX/DURATION :
- female 9-14 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
- REFERENCE :
- OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 4,381,1970
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