Eberlein W, Schmidt G, Reuter A, Kutter E
Arzneimittelforschung. 1977 Feb;27(2):356-9.
Compound 5,11-dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one dihydrochloride (pirenzepine, L-S 519) represents a new type of drug in ulcer therapy. It has been selected for broad clinical investigations because of its outstanding pharmacological profile. Pirenzepine is devoid of any central activity despite certain structural similarities in relation to psychotropic tricyclic compounds. The extraordinary pharmacokinetic and pharmacodynamic behaviour of this compound can be easily derived from its inherent physicochemical properties: The inability to pass the blood-brain barrier as well as its inability to activate the unspecific and specific psychotropic receptors is due to thermodynamic factors.
化合物5,11 - 二氢 - 11 - [(4 - 甲基 - 1 - 哌嗪基)乙酰基] - 6H - 吡啶并[2,3 - b][1,4]苯二氮䓬 - 6 - 酮二盐酸盐（哌仑西平，L - S 519）是溃疡治疗中的一种新型药物。由于其出色的药理学特性，它已被选用于广泛的临床研究。尽管与精神otropic三环化合物在结构上有某些相似之处，但哌仑西平没有任何中枢活性。该化合物非凡的药代动力学和药效学行为可以很容易地从其固有的物理化学性质推导出来：无法通过血脑屏障以及无法激活非特异性和特异性精神otropic受体是由于热力学因素。
