阿伐斯汀

中文名称:

阿伐斯汀

中文同义词:

(E)-3-[6-[(E)-1-(4-甲基苯基)-3-吡咯烷-1-基丙-1-烯基]吡啶-2-基]-2-丙烯酸;阿伐司丁;阿伐司汀;阿伐斯汀;(E,E)-3-[6-[1-(对甲苯基)-3-吡咯烷-1-基-1-丙烯基]-2-吡啶基]丙烯酸;阿伐斯汀杂质

英文名称:

Acrivastine

英文同义词:

(e)-3-[6-[(e)-1-(4-methylphenyl)-3-pyrrolidin-1-ylprop-1-enyl]pyridin-2-yl]prop-2-enoic acid;ACRIVASTINE;Acrivastin;(E，E)-3-[6-[1-(4-Methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl]-2-pyridinyl]-2-propenoic acid;BW-270C;BW-825C;BW-A825C;(E)-3-[6-[(E)-1-(4-Methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl]-2-pyridinyl]propenoic acid

CAS号:

87848-99-5

分子式:

C22H24N2O2

分子量:

348.44

EINECS号:

相关类别:

抗组胺药;药物;组胺H1受体拮抗剂;药物成分 (研究实验用);医用原料;医药原料;医用原料;医药原料药-科研原料;API;其它产品;医药原料;原料药;化工原料

Mol文件:

87848-99-5.mol

熔点 

222° (dec)

沸点 

555.1±50.0 °C(Predicted)

密度 

1.170±0.06 g/cm3(Predicted)

储存条件 

2-8°C

溶解度 

DMSO: >2mg/mL (warmed)

酸度系数(pKa)

1.99±0.10(Predicted)

形态

powder

颜色

white to beige

CAS 数据库

87848-99-5(CAS DataBase Reference)

药理作用

阿伐斯汀是一种中等强度的竞争性组织胺H1受休拮抗剂，属于抗组胺药，20世纪80年代末由葛兰素威康公司推出的酚嗪类抗组胺类抗过敏药物，具有选择性地阻断组胺H1受体的作用，没有明显抗胆碱作用。对中枢神经系统的穿透能力低，可通过完全或部分阻止组织胺释放而缓解由其引起的症状。不易通过血脑屏障，无镇静作用。口服吸收良好，1．5小时达血药峰浓度，大部分原形药物经肾排泄，少部分经肝代谢，代谢产物仍具活性，由尿排出。适用于治疗过敏性鼻炎、枯草热、荨麻疹、湿疹、皮肤瘙痒症等。

生物活性

Acrivastine (BW825C) 是用于研究过敏性鼻炎的短效histamine 1受体拮抗剂。

体内研究

Acrivastine (usually 8mg three times daily) is an effective and well tolerated antihistamine in the treatment of chronic urticaria and allergic rhinitis. Acrivastine is more effective than placebo and similar in efficacy to clemastine or terfenadine in the treatment of seasonal allergic rhinitis. In the treatment of dermatoses in which histamine has a pathogenetic role, the efficacy of acrivastine is superior to that of placebo and similar to that of usual dosages of clemastine, hydroxyzine, chlorpheniramine, cyproheptadine or terfenadine. Acrivastine causes less drowsiness than clemastine, the incidence of adverse effects being indistinguishable from that with placebo or terfenadine. Both 4 mg and 8 mg acrivastine alleviate the symptoms of seasonal allergic rhinitis with significant improvements in the symptom scores for sneezing, running nose and the calculated overall score. In addition, 8 mg acrivastine reduces the symptom scores for watery eyes and itchy throat. Acrivastine is both well tolerated and effective in the treatment of seasonal allergic rhinitis.

化学性质 

从异丙醇结晶，熔点222℃(分解)。

用途 

竞争性H1受体拮抗剂。用于过敏性鼻炎、花粉病、慢性原发性荨麻疹、皮肤划痕症、拟副交感神经性荨麻疹、特异性风冷型荨麻疹等。

生产方法 

从2，6-二溴吡啶、4-甲基苯甲腈、EtO2CH2P(O)(Oet)2和(2-吡咯烷基乙基)三苯基膦溴化物，经五步反应得到。

WGK Germany 

3

RTECS号

UD3474000