Synthesis and structure of novel 2,3, 5,6-tetrahydro-1H-imidazo[2,1-b][1,3,5]benzotriazepines with vasocontractile activity in rabbit aortic rings.
A series of novel 2,3,5,6-tetrahydro-1H-imidazo[2,1-b][1,3,5]benzotriazepines (3a-n) and hydrochlorides (4a-b) were prepared and their structure was determined by IR and NMR spectroscopic data as well as by X-ray analysis of the hydrochloride 4a. The newly synthesized benzotriazepine 4b exhibited concentration-dependent vasocontractile activity in isolated rabbit aortic rings. Rimalkalim was found to induce a relaxation in rabbit aortic rings precontracted by 4b (3x10(-5) mol). Present results indicate that K(ATP)-dependant channels may contribute in the contractile activity of benzotriazepine 4b.
Department of Chemical Technology of Drugs, Medical University of Gdansk, Al. Gen. Hallera 107, 80-416 Gdansk, Poland. saczew@sanus.amg.gda.pl
Franciszek
F
Saczewski
Ewa
E
Kobierska
Jacek
J
Petrusewicz
Anna
A
Gendzwill
Maria
M
Gdaniec
D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects* / Q000502:physiology; D001552:Benzazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D002839:Chromans / Q000138:chemical synthesis / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D011759:Pyrrolidines / Q000138:chemical synthesis / Q000494:pharmacology; D011817:Rabbits; D014661:Vasoconstriction / Q000187:drug effects* / Q000502:physiology
D001552:Benzazepines; D002839:Chromans; D011759:Pyrrolidines; C075012:rilmakalim