3978-86-7

• 常用中文名：马来酸阿扎他啶
• 常用英文名：Azatadine dimaleate
• CAS号：3978-86-7
• 分子式：C₂₈H₃₀N₂O₈
• 分子量：522.546
• 相关类别： 原料药 抗变态反应药 抗组胺药
• 发布时间：2018-09-07 14:22:34
• 更新时间：2024-01-08 18:29:11
• Azatadine马来酸氢盐是组胺受体和胆碱受体抑制剂,IC50分别为6.5 nM和10 nM。

名称

• 中文名: 马来酸阿扎他啶
• 英文名: azatadine maleate
• 中文别名: 阿折地平二马来酸盐
• 英文别名: 11-(1-methyl-piperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine; 11-(1-methylpiperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine (2Z)-but-2-enedioate (1:2); Azatadinum [INN-Latin]; Azatadina [INN-Spanish]; 11-(1-methylpiperidin-4-ylidene)-5,6-dihydrobenzo[1,2]cyclohepta[3,4-b]pyridine; Azatadina; Optimine; Idulian; Azatadinum; Azatidine; 5H-Benzo[5,6]cyclohepta[1,2-b]pyridine, 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-, (2Z)-2-butenedioate (1:2); 11-(1-Methyl-4-piperidinylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine (2Z)-2-butenedioate (1:2); Azatadine [INN:BAN]; 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine; Azatadine dimaleate; 6,11--dihydro-11-(N-methyl-4-piperidylidene)-5H-benzo-[5,6]-cyclohepta-[1,2-b]-pyridine; Azatadine maleate; (Z)-but-2-enedioic acid,11-(1-methylpiperidin-4-ylidene)-5,6-dihydrobenzo[1,2]cyclohepta[3,4-b]pyridine; Zadine; Azatadin maleate; AZATADINE; EINECS 223-615-8; Azatadine (dimaleate)

物化性质

• 沸点: 450.1ºC at 760 mmHg
• 熔点: 152-154°
• 分子式: C₂₈H₃₀N₂O₈
• 分子量: 522.546
• 闪点: 226ºC
• 精确质量: 522.200195
• PSA: 165.33000
• LogP: 3.06920
• 储存条件: 室温，干燥

生物活性

• 描述: Azatadine马来酸氢盐是组胺受体和胆碱受体抑制剂,IC50分别为6.5 nM和10 nM。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体
  信号通路 >> 免疫及炎症 >> 组胺受体
  研究领域 >> 炎症/免疫
• 参考文献:

  [1]. Wilson JD, et al. Azatadine maleate (Zadine): evaluation in the management of allergic rhinitis. N Z Med J. 1981 Aug 12;94(689):79-81.

  [2]. Tozzi S, et al. The pharmacology of azatadine, a potential antiallergy drug. Agents Actions. 1974 Oct;4(4):264-70.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : DE8025500 CHEMICAL NAME : 11H-Benzo(5,6)cyclohepta(1,2-b)pyridine, 5,6-dihydro-11-(1-methyl-4-piperidylidene)-, dimaleate CAS REGISTRY NUMBER : 3978-86-7 LAST UPDATED : 199604 DATA ITEMS CITED : 11 MOLECULAR FORMULA : C20-H22-N2.2C4-H4-O4 MOLECULAR WEIGHT : 522.60 WISWESSER LINE NOTATION : T C676 DN&T&J B1- AT6N CUTJ &QV1U1VQ 2 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - man DOSE/DURATION : 286 mg/kg/24H-I TOXIC EFFECTS : Behavioral - muscle contraction or spasticity REFERENCE : MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 141,449,1984 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 440 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 18,185,1971 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 166 mg/kg TOXIC EFFECTS : Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes REFERENCE : JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa, Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year: 1,173,1975 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1 gm/kg TOXIC EFFECTS : Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes REFERENCE : JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa, Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year: 1,173,1975 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 165 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : AGACBH Agents and Actions, A Swiss Journal of Pharmacology. (Birkhaeuser Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1969/70- Volume(issue)/page/year: 4,264,1974 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 105 mg/kg TOXIC EFFECTS : Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes REFERENCE : JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa, Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year: 1,173,1975 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 178 mg/kg TOXIC EFFECTS : Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes REFERENCE : JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa, Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year: 1,173,1975 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 50 mg/kg TOXIC EFFECTS : Behavioral - tremor Gastrointestinal - nausea or vomiting Lungs, Thorax, or Respiration - respiratory stimulation REFERENCE : JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa, Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year: 1,79,1975 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - guinea pig DOSE/DURATION : 356 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : AGACBH Agents and Actions, A Swiss Journal of Pharmacology. (Birkhaeuser Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1969/70- Volume(issue)/page/year: 4,264,1974 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 8400 mg/kg/4W-I TOXIC EFFECTS : Gastrointestinal - changes in structure or function of endocrine pancreas Liver - fatty liver degeneration Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa, Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year: 1,173,1975 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 27300 mg/kg/26W-I TOXIC EFFECTS : Liver - fatty liver degeneration Musculoskeletal - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa, Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year: 1,173,1975

安全

• 符号: GHS07
• 信号词: Warning
• 危害声明: H302-H336
• 警示性声明: P301 + P312 + P330
• 危险品运输编码: NONH for all modes of transport