[Anti-ulcer agent pirenzepine (LS 519)--a tricyclic compound with particular physico-chemical properties (author's transl)].
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.
D000897:Anti-Ulcer Agents / Q000494:pharmacology*; D001570:Benzodiazepinones / Q000378:metabolism / Q000494:pharmacology*; D001921:Brain / Q000187:drug effects; D002463:Cell Membrane Permeability; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D008055:Lipids; D008968:Molecular Conformation; D010879:Piperazines / Q000378:metabolism / Q000494:pharmacology*; D011619:Psychotropic Drugs; D012995:Solubility; D013329:Structure-Activity Relationship
D000897:Anti-Ulcer Agents; D001570:Benzodiazepinones; D008055:Lipids; D010879:Piperazines; D011619:Psychotropic Drugs
Das Ulkustherapeutikum Pirenzepin (L-S 519)--eine tricyclische Verbindung mit besonderen physikalisch-chemischen Eigenschaften