Literature DB >> 577153

[Anti-ulcer agent pirenzepine (LS 519)--a tricyclic compound with particular physico-chemical properties (author's transl)].

W Eberlein, G Schmidt, A Reuter, E Kutter.   

Abstract

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.

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Year:  1977        PMID: 577153

Source DB:  PubMed          Journal:  Arzneimittelforschung        ISSN: 0004-4172


  4 in total

1.  Muscarinic receptor blockade by pirenzepine: effect on prolactin secretion in man.

Authors:  A Masala; S Alagna; L Devilla; P P Rovasio; S Rassa; R Faedda; A Satta
Journal:  J Endocrinol Invest       Date:  1982 Jan-Feb       Impact factor: 4.256

2.  Relationship of erosive gastritis to the acid secreting area and intestinal metaplasia, and the healing effect of pirenzepine.

Authors:  M Tatsuta; H Iishi; S Okuda
Journal:  Gut       Date:  1987-05       Impact factor: 23.059

Review 3.  Pirenzepine. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in peptic ulcer disease and other allied diseases.

Authors:  A A Carmine; R N Brogden
Journal:  Drugs       Date:  1985-08       Impact factor: 9.546

4.  Binding and functional profiles of the selective M1 muscarinic receptor antagonists trihexyphenidyl and dicyclomine.

Authors:  A Giachetti; E Giraldo; H Ladinsky; E Montagna
Journal:  Br J Pharmacol       Date:  1986-09       Impact factor: 8.739

  4 in total

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