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托西溴苄铵

托西溴苄铵用途

Bretylium (tosylate)是血管收缩的神经递质突触前释放的抑制剂,是交感神经和肾上腺素神经的阻断剂。

托西溴苄铵名称

[ CAS 号 ]:
61-75-6

[ 中文名 ]:
溴苄乙胺

[ 英文名 ]:
Bretylium (tosylate)

[中文别名 ]:

托西溴苄铵

[英文别名 ]:

Bretylium Tosilate
EINECS 200-516-8
bretylan
Bretylium Tosylate
bretilium tosilate
MFCD00038731
Bretylium (tosylate)

托西溴苄铵生物活性

[ 描述 ]:

Bretylium (tosylate)是血管收缩的神经递质突触前释放的抑制剂,是交感神经和肾上腺素神经的阻断剂。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 神经疾病

[参考文献]

[1]. McGinn R et al. Adenosine receptor inhibition attenuates the suppression of postexercise cutaneous blood flow. J Physiol. 2014 Jun 15;592(12):2667-78.

[2]. Tew GA et al. Aging and aerobic fitness affect the contribution of noradrenergic sympathetic nerves to the rapid cutaneous vasodilator response to local heating. J Appl Physiol (1985). 2011 May;110(5):1264-70

[3]. Cakir B et al.Leptin inhibits gastric emptying in rats: role of CCK receptors and vagal afferent fibers. Physiol Res. 2007;56(3):315-22. Epub 2006 Jun 22.

[相关活性小分子]

托西溴苄铵物理化学性质

[ 熔点 ]:
97-99°

[ 分子式 ]:
C₁₈H₂₄BrNO₃S

[ 分子量 ]:
414.357

[ 精确质量 ]:
413.066010

[ PSA ]:
65.58000

[ LogP ]:
5.02530

[ 外观性状 ]:
white

[ 储存条件 ]:
库房通风低温干燥

[ 水溶解性 ]:
H2O: soluble50mg/mL

托西溴苄铵毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: BO9450000

CHEMICAL NAME :: Ammonium, (o-bromobenzyl)ethyldimethyl-, p-toluenesulfonate

CAS REGISTRY NUMBER :: 61-75-6

LAST UPDATED :: 199603

DATA ITEMS CITED :: 15

MOLECULAR FORMULA :: C11-H17-Br-N.C7-H7-O3-S

MOLECULAR WEIGHT :: 414.40

WISWESSER LINE NOTATION :: ER B1K2&1&1 &OSWR D1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 81500 ug/kg/15M-C

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Behavioral - coma Vascular - BP lowering not characterized in autonomic section

REFERENCE :: AJEMEN American Journal of Emergency Medicine. (WB Saunders, Philadelphia, PA) V.1- 1983- Volume(issue)/page/year: 13,177,1995

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 57 mg/kg

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

REFERENCE :: PHMGBN Pharmacology: International Journal of Experimental and Clinical Pharmacology. (S. Karger AG, Postfach CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 21,256,1980

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 17 mg/kg

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

REFERENCE :: PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 2,148,1979

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 84 mg/kg

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

REFERENCE :: PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 2,148,1979

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 400 mg/kg

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

REFERENCE :: BJPCAL British Journal of Pharmacology and Chemotherapy. (London, UK) V.1-33, 1946-68. For publisher information, see BJPCBM. Volume(issue)/page/year: 14,536,1959

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 39 mg/kg

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

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: 155,69,1965

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 72 mg/kg

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

REFERENCE :: BJPCAL British Journal of Pharmacology and Chemotherapy. (London, UK) V.1-33, 1946-68. For publisher information, see BJPCBM. Volume(issue)/page/year: 14,536,1959

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 14 mg/kg

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

REFERENCE :: PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 2,148,1979

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 64 mg/kg

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

REFERENCE :: PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 2,148,1979

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 43 mg/kg

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

REFERENCE :: PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 2,148,1979

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 100 mg/kg

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

REFERENCE :: PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 2,148,1979

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 30 mg/kg

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

REFERENCE :: PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 2,148,1979

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 160 mg/kg

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

REFERENCE :: PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 2,148,1979 *** REVIEWS *** TOXICOLOGY REVIEW PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 2,148,1979 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5621 No. of Facilities: 51 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 1056 (estimated) No. of Female Employees: 657 (estimated)

托西溴苄铵安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302 + H312 + H332

[ 警示性声明 ]:
P261-P280-P301 + P312 + P330

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
20/21/22

[ 安全声明 (欧洲) ]:
S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
BO9450000

托西溴苄铵制备

以邻甲苯胺为原料，经重氮化脱氮并用溴置换生成邻溴甲苯，在光照下和溴素溴化生成邻溴苄基溴甲烷，再用二甲胺在压力下胺化得邻溴苄基二甲胺，最后与对-甲基磺酸乙酯加成得成品。

托西溴苄铵文献

Catecholamines, α-, and β-adrenoceptors are not responsible for activation of duodenum motility induced by sympathetic nerve stimulation.

Bull. Exp. Biol. Med. 152(1) , 5-8, (2011)

Stimulation of sympathetic nerve in anesthetized dogs not treated with adrenergic blockers more frequently exerted stimulating rather than inhibitory effect on duodenal motility. Blockade of α- and β-...

Exogenous melatonin delays gastric emptying rate in rats: role of CCK2 and 5-HT3 receptors.

J. Physiol. Pharmacol. 56(4) , 543-53, (2005)

Pineal hormone melatonin is proposed as a potential treatment for severe sleep disturbances, and various gastrointestinal disorders. It was shown that melatonin increases intestinal motility and influ...

Tone of sympathetic nerves and regulation of heart activity.

Bull. Exp. Biol. Med. 130(10) , 930-3, (2000)

Tone of sympathetic nerves to the heart was studied in rats and guinea pigs. Experiments with pharmacological blockade of the sympathetic nervous system and vagotomy confirmed the general notion on th...

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