19216-56-9

• 常用中文名：哌唑嗪
• 常用英文名：Prazosin
• CAS号：19216-56-9
• 分子式：C₁₉H₂₁N₅O₄
• 分子量：383.40100
• 相关类别： 原料药 循环系统用药 抗高血压病药
• 发布时间：2018-06-02 08:00:00
• 更新时间：2024-01-05 15:19:48
• Prazosin是α肾上腺素阻断剂,可作用于高血压、焦虑和恐慌症等。

名称

• 中文名: 哌唑嗪
• 英文名: prazosin
• 中文别名: 1-(4-氨基-6,7-二甲氧基-2-喹唑啉基-4-(2-呋喃基羰基))哌嗪
• 英文别名: [14C]-Prazosin; Prazosinum [INN-Latin]; Minipress; (4-(4-Amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl)(furan-2-yl)methanone; [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(furan-2-yl)methanone; [125I]-Prazosin; Prazosinum; 4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazinyl furan-2-yl ketone; [Bodipyl-FL]-Prazosin; Prazosine; Prazosina; Furazosin; Prazosina [INN-Spanish]; 2-[4-(2-furoyl)-piperazin-1-yl]-4-amino-6,7-dimethoxy-quinazoline; Prazosine [INN-French]; Lentopres

物化性质

• 密度: 1.352g/cm3
• 沸点: 638.4ºC at 760mmHg
• 熔点: 278-280ºC
• 分子式: C₁₉H₂₁N₅O₄
• 分子量: 383.40100
• 闪点: 339.9ºC
• 精确质量: 383.15900
• PSA: 107.68000
• LogP: 1.71760
• 蒸汽压: 3.4E-16mmHg at 25°C
• 折射率: 1.651
• 储存条件: 库房通风低温干燥

生物活性

• 描述: Prazosin是α肾上腺素阻断剂,可作用于高血压、焦虑和恐慌症等。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体
  天然产物 >> 生物碱
  研究领域 >> 心血管疾病
• 参考文献:

  [1]. Day HE, et al. Distribution of alpha 1a-, alpha 1b- and alpha 1d-adrenergic receptor mRNA in the rat brain and spinal cord. J Chem Neuroanat. 1997 Jul;13(2):115-39.

  [2]. Yu CX, et al. Selective MT(2) melatonin receptor antagonist blocks melatonin-induced antinociception in rats. Neurosci Lett. 2000 Mar 24;282(3):161-4.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : VA1300000 CHEMICAL NAME : Quinazoline, 4-amino-6,7-dimethoxy-2-(4-(2-furoyl)piperazin-1-yl)- CAS REGISTRY NUMBER : 19216-56-9 BEILSTEIN REFERENCE NO. : 0768345 LAST UPDATED : 199703 DATA ITEMS CITED : 9 MOLECULAR FORMULA : C19-H21-N5-O4 MOLECULAR WEIGHT : 383.45 WISWESSER LINE NOTATION : T66 BN DNJ C- AT6N DNTJ DV- BT5OJ&& EZ HO1 IO1 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 20 ug/kg TOXIC EFFECTS : Vascular - BP lowering not characterized in autonomic section Gastrointestinal - nausea or vomiting REFERENCE : AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 97,455,1982 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - man DOSE/DURATION : 1143 ug/kg TOXIC EFFECTS : Vascular - BP lowering not characterized in autonomic section REFERENCE : AMSVAZ Acta Medica Scandinavica. (Almqvist & Wiksell, POB 45150, S-10430 Stockholm, Sweden) V.52-224, 1919-88. Volume(issue)/page/year: 213,157,1983 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human DOSE/DURATION : 280 ug/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - hallucinations, distorted perceptions Vascular - BP lowering not characterized in autonomic section REFERENCE : BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 2,508,1976 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human DOSE/DURATION : 1260 ug/kg TOXIC EFFECTS : Behavioral - changes in motor activity (specific assay) Kidney, Ureter, Bladder - other changes REFERENCE : BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 1,622,1978 TYPE OF TEST : LD - Lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >3 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4734418 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >4 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 128,129,1989 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 REFERENCE : RPTOAN Russian Pharmacology and Toxicology (English Translation). Translation of FATOAO. (Euromed Pub., 33, Woodlands Rd., Surbiton, Surrey, UK) V.30- 1967- Volume(issue)/page/year: 50,182,1987 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 30 mg/kg/60D-I TOXIC EFFECTS : Cardiac - changes in heart weight Vascular - BP lowering not characterized in autonomic section Endocrine - changes in adrenal weight REFERENCE : ETPAEK Experimental and Toxicologic Pathology. (Gustav Fischer Verlag Jena, Postfach 100537, D-07705 Jena, Germany) V.44- 1992- Volume(issue)/page/year: 45,109,1993 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 2571 ug/kg SEX/DURATION : male 60 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct REFERENCE : AMSVAZ Acta Medica Scandinavica. (Almqvist & Wiksell, POB 45150, S-10430 Stockholm, Sweden) V.52-224, 1919-88. Volume(issue)/page/year: 213,319,1983

安全

• 海关编码: 2934999090

合成路线

57200-93-8 26961-27-3 ~% 19216-56-9

文献：US3935213 A1, ;

65679-29-0 ~% 19216-56-9

文献：US4062844 A1, ;

65679-30-3 ~% 19216-56-9

文献：US4062844 A1, ;

527-69-5 60547-97-9 ~% 19216-56-9

文献：Tetrahedron Letters, , vol. 47, # 15 p. 2549 - 2552

23680-84-4 ~% 19216-56-9

文献：Tetrahedron Letters, , vol. 47, # 15 p. 2549 - 2552

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57200-93-8 26961-27-3 65679-29-0 65679-30-3
527-69-5 60547-97-9 23680-84-4
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海关

海关编码	2934999090
中文概述	2934999090. 其他杂环化合物. 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
Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%