盐酸曲唑酮_MSDS_作用_用途_盐酸曲唑酮CAS号【25332-39-2】

Trazodone盐酸盐是5羟色胺受体拮抗剂和重吸收抑制剂,可作用于焦虑症。

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用作抗忧郁药

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[ 描述 ]:

Trazodone盐酸盐是5羟色胺受体拮抗剂和重吸收抑制剂,可作用于焦虑症。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

研究领域 >> 神经疾病

[参考文献]

[1]. Haria, M., A. Fitton, and D. McTavish, Trazodone. A review of its pharmacology, therapeutic use in depression and therapeutic potential in other disorders. Drugs Aging, 1994. 4(4): p. 331-55.

[2]. Nierenberg, A.A., et al., Trazodone for antidepressant-associated insomnia. Am J Psychiatry, 1994. 151(7): p. 1069-72.

[3]. Fink, H.A., et al., Trazodone for erectile dysfunction: a systematic review and meta-analysis. BJU Int, 2003. 92(4): p. 441-6.

[相关活性小分子]

[ 沸点 ]:
528.5ºC at 760 mmHg

[ 熔点 ]:
223ºC

[ 分子式 ]:
C₁₉H₂₃Cl₂N₅O

[ 分子量 ]:
408.325

[ 闪点 ]:
273.4ºC

[ 精确质量 ]:
407.127960

[ PSA ]:
45.78000

[ LogP ]:
3.16660

[ 外观性状 ]:
powder | off-white

[ 蒸汽压 ]:
2.94E-11mmHg at 25°C

[ 储存条件 ]:
-20°C Freezer

[ 水溶解性 ]:
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 23.3 mg/mL

详细MSDS(安全技术说明书)

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XZ5660000

CHEMICAL NAME :: s-Triazolo(4,3-a)pyridin-3(2H)-one, 2-(3-(4-(m-chlorophenyl)-1-piperazinyl)propyl)-, monohydrochloride

CAS REGISTRY NUMBER :: 25332-39-2

LAST UPDATED :: 199706

DATA ITEMS CITED :: 29

MOLECULAR FORMULA :: C19-H22-Cl-N5-O.Cl-H

MOLECULAR WEIGHT :: 408.37

WISWESSER LINE NOTATION :: T56 ANVNNJ C3- AT6N DNTJ DR CG &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 5714 ug/kg/4D-I

TOXIC EFFECTS :: Behavioral - euphoria Behavioral - excitement

REFERENCE :: BJPYAJ British Journal of Psychiatry. (Headley Brothers, Ltd., Ashford, Kent TN24 8HH, UK) V.109- 1963- Volume(issue)/page/year: 158,275,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 43 mg/kg/30D-I

TOXIC EFFECTS :: Blood - agranulocytosis Blood - other changes

REFERENCE :: AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921- Volume(issue)/page/year: 150,1563,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 750 ug/kg

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions

REFERENCE :: AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921- Volume(issue)/page/year: 141,434,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 720 mg/kg/34W-I

TOXIC EFFECTS :: Liver - hepatitis (hepatocellular necrosis), zonal Liver - jaundice (or hyperbilirubinemia) hepatocellular Kidney, Ureter, Bladder - other changes in urine composition

REFERENCE :: AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 118,791,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 46 mg/kg/8D-I

TOXIC EFFECTS :: Behavioral - excitement Cardiac - pulse rate increase, without fall in BP Kidney, Ureter, Bladder - urine volume increased

REFERENCE :: JCPYDR Journal of Clinical Pyschopharmacology. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1981- Volume(issue)/page/year: 6,117,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 667 ug/kg

TOXIC EFFECTS :: Cardiac - cardiomyopathy including infarction

REFERENCE :: AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921- Volume(issue)/page/year: 141,1472,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 80 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: JATOD3 Journal of Analytical Toxicology. (Preston Pub. Inc., POB 48312, Niles, IL 60648) V.1- 1977- Volume(issue)/page/year: 8,91,1984

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 690 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 178 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2729 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 22,967,1991

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 91 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 584 mg/kg

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

REFERENCE :: DDREDK Drug Development Research. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1981- Volume(issue)/page/year: 22,385,1991

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 255 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: 81,99,1992

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1500 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 22,967,1991

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 91 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 500 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Behavioral - aggression

REFERENCE :: MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >40 mg/kg

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

REFERENCE :: MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 25 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands

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: 3,94,1981

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 560 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 52 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 66175 mg/kg/78W-C

TOXIC EFFECTS :: Endocrine - changes in adrenal weight Endocrine - changes in thyroid weight Related to Chronic Data - changes in testicular weight

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,5865,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 2730 mg/kg/13W-I

TOXIC EFFECTS :: Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 5),S1259,1989 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 159 mg/kg

SEX/DURATION :: male 7 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - impotence

REFERENCE :: AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921- Volume(issue)/page/year: 140,1256,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 112 mg/kg

SEX/DURATION :: male 6 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - other effects on male

REFERENCE :: JCLPDE Journal of Clinical Psychiatry. (Physicians Postgraduate Press, Inc., POB 240008, Memphis, TN 38124) V.39- 1978- Volume(issue)/page/year: 45,232,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 667 ug/kg

SEX/DURATION :: male 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - other effects on male

REFERENCE :: AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921- Volume(issue)/page/year: 142,142,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3300 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 5),1283,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1100 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - physical

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 5),1283,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 750 mg/kg

SEX/DURATION :: female 7-20 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 5),1301,1989 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5669 No. of Facilities: 24 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 333 (estimated) No. of Female Employees: 219 (estimated)

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[ 符号 ]:

GHS02, GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H301 + H311 + H331-H370

[ 警示性声明 ]:
P210-P260-P280-P301 + P310-P311

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R22;R40

[ 安全声明 (欧洲) ]:
S22-S36

[ 危险品运输编码 ]:
3249

[ WGK德国 ]:
3

[ RTECS号 ]:
XZ5660000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2933990090

盐酸曲唑酮上游产品

盐酸曲唑酮下游产品

1. 吡啶肼的制备

在反应瓶中加入2-氯吡啶3.8g(0.04mol)和水合肼30ml,搅拌回流24h.应液用乙醚(20ml×2)提取,水层浓缩,用乙醚(15ml×6)提取,合并乙醚提取液,水洗,无水Na2SO4干燥,蒸去乙醚,冷却,得白色固体,干燥得吡啶肼2.9g,收率67%,mp50~51ºC.

2. 1,2,4-三唑并-[4,3-a]吡啶-3(2H)-酮制备

在反应瓶中加入吡啶肼1.4g(0.013mol)和脲1.7g(0.03mol),混合,加热熔融,于155~160ºC反应2h.稍冷后加入水30ml,搅拌,抽滤,水洗,干燥得1,2,4-三唑并-[4,3-a]吡啶-3(2H)-酮1.5g,收率86.5%,mp224~226ºC.

3. 盐酸曲唑酮的合成

在反应瓶中加入1,2,4-三唑并-[4,3-a]吡啶-3(2H)-酮1.0g(7.4mmol)、1-(3-氯苯基)-4-(3-氯丙基)哌嗪盐酸盐2.4g(7.4mmol)和乙醇20ml,搅拌下加入NaOH0.6g(0.015mol),搅拌回流30h.热过滤,少量乙醇洗,洗液和滤液合并,减压浓缩至干.剩余物加水10ml,用二氯甲烷(10ml×3) 提取.合并提取液,水洗,无水Na2SO4干燥,过滤,滤液蒸除溶剂,加无水乙醇10ml溶解,通入干燥的HCl气体,产生大量固体,过滤,滤饼用少量无水乙醇洗,用无水乙醇重结晶,得白色固体盐酸曲唑酮2.1g,收率67.5%,mp222~225 ºC.

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[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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