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J Med Chem ; 27(2): 206-12, 1984 Feb.
Article in English | MEDLINE | ID: mdl-6319701

ABSTRACT

A series of imidazo[1,2-alpha]pyrazine derivatives was synthesized by condensation of alpha-halogenocarbonyl compounds and aminopyrazines. Various compounds resulted from competitive reactions or reagent isomerization and demonstrated in vitro uterine-relaxing and in vivo antibronchospastic activities. On isolated atria, 5-bromoimidazo-[1,2-alpha]pyrazine showed positive chronotropic and inotropic properties; the latter was associated with an increase in the cyclic AMP tissue concentration. Potentiation of the isoproterenol positive inotropic effect of 5-bromoimidazo[1,2-alpha]pyrazine and the lack of blockade of the 5-bromoimidazo[1,2-alpha]pyrazine positive inotropic effect by propranolol suggested phosphodiesterase-inhibiting properties.


Subject(s)
Bronchial Spasm/drug therapy , Heart/drug effects , Imidazoles/pharmacology , Pyrazines/pharmacology , Uterine Contraction/drug effects , Animals , Atrial Function , Chemical Phenomena , Chemistry , Cyclic AMP/metabolism , Dose-Response Relationship, Drug , Drug Interactions , Female , Guinea Pigs , Heart Rate/drug effects , Imidazoles/chemical synthesis , Isoproterenol/pharmacology , Male , Myocardial Contraction/drug effects , Propranolol/pharmacology , Rats , Stimulation, Chemical , Structure-Activity Relationship
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