中文同义词:
比哌立登;碧卜利旦;3-哌啶基-1-苯基-双环庚烯基-1-丙醇;1-(5-双环[2.2.1]庚-2-烯基)-1-苯基-3-(1-哌啶基)丙-1-醇;安克痉;双环哌丙醇;碧卜利旦 碧卜利旦;比哌立登/碧卜利旦
英文同义词:
alpha-(bicyclo(2.2.1)hept-5-en-2-yl)-alpha-phenyl-1-piperidinopropanol;alpha-5-norbornen-2-yl-alpha-phenyl-1-piperidinepropano;alpha-5-Norbornen-2-yl-alpha-phenyl-1-piperidinepropanol;alpha-bicyclo(2.2.1)hept-5-en-2-yl-alpha-phenyl-1-piperidinepropano;alpha-phenyl-alpha-(2-piperidinoethyl)-5-norbornene-2-methano;Beperiden;-Bicyclo[2,2,1]hept-5-en-2yl-phenyl-1-piperidinepropanol;Bicyclo[2.2.1]hept-5-ene-2-methanol, alpha-phenyl-alpha-[2-(1-piperidinyl)ethyl]-
相关类别:
小分子抑制剂;现货;医药原料;生物化工类;医用原料;医药原料药
沸点
451.49°C (rough estimate)
密度
1.0202 (rough estimate)
酸度系数(pKa)
14.05±0.29(Predicted)
NIST化学物质信息
Biperiden(514-65-8)
生物活性
Biperiden(KL 373)有抗帕金森症活性,是中枢M1胆碱受体阻断剂。
化学性质
结晶体。熔点112-116℃(101℃)。不易溶于水,微溶于乙醇,易溶于甲醇。该品的盐酸盐(C21H29NO·HCI)又称安克痉(Akineton,Akinophyl),为白色结晶。约275℃分解,也有报道其熔点为238℃。
用途
该品为抗震颤麻痹药、解痉药。小鼠口服LD50为545mg/kg,静脉注射为56mg/kg。
用途
Biperiden is antiparkinsonian; non-selective muscarinic receptor antagonist. Biperiden is used for the adjunctive treatment of all forms of Parkinson鈥瞫 Disease (postencephalitic, idiopathic, and arter iosclerotic); also commonly used to improve parkinsonian signs and symptoms related to antipsychotic drug therapy.
生产方法
以环戊二烯为原料,先与氯乙烯合成氯代双环庚烯,再与镁和乙醚反应,得双环庚烯镁化氯,最后与β-哌啶苯丙酮缩合制得比哌立登。β-哌啶苯丙酮的制备:以苯乙酮为原料与哌啶盐酸盐、甲醛、二甲胺经曼氏反应得到。
急性毒性
口服-大鼠 LD50: 750 毫克/公斤; 口服-小鼠 LD50: 530 毫克/公斤
毒害物质数据
514-65-8(Hazardous Substances Data)
毒性
LD50 in mice (mg/kg): 195 s.c., 56 i.v. (Klavehn)