RESUMO
The synthesis of N-substituted 1,7,7-trimethyl-2-piperidinobicyclo[2.2.1]hept-2-ene 3 carboxamides (II) by reaction of 1,7,7-trimethyl-2-piperidinobicyclo[2.2.1]hept-2-ene (I) with alkyl and aryl isocyanates, as well as the alkaline hydrolysis of (II) to N-substituted 1,7,7-trimethylbicyclo[2.2.1]heptan-2-one 3 carboxamides (III), are described. A number of compounds (II) and (III) showed strong hypotensive and bradycardiac activities in rats, as well as weak infiltration anesthesia and antiarrhythmic activity in mice. Antiacetylcholine activity in vitro is also reported.
Assuntos
Anti-Hipertensivos/síntese química , Compostos Bicíclicos com Pontes/síntese química , Hidrocarbonetos Aromáticos com Pontes/síntese química , Acetilcolina/antagonistas & inibidores , Anestésicos Locais/síntese química , Animais , Antiarrítmicos/síntese química , Pressão Sanguínea/efeitos dos fármacos , Fenômenos Químicos , Química , Cobaias , Frequência Cardíaca/efeitos dos fármacos , Técnicas In Vitro , Camundongos , Piperidinas/síntese química , RatosRESUMO
Fructose-1,6-diphosphate (FDP) has been reported to exert beneficial effects on several cardiac functions. We studied the effects of FDP on the biochemical and dynamic functions of the heart in anesthetized dogs. Significant effects of FDP were noted mostly as related to pyruvate and lactate metabolism. The results seem to indicate that FDP may improve heart metabolism, and coronary function in restricted animals.
Assuntos
Frutosedifosfatos/administração & dosagem , Hemodinâmica/efeitos dos fármacos , Hexosedifosfatos/administração & dosagem , Miocárdio/metabolismo , Animais , Pressão Sanguínea/efeitos dos fármacos , Circulação Coronária/efeitos dos fármacos , Cães , Frutosedifosfatos/farmacologia , Frequência Cardíaca/efeitos dos fármacos , Lactatos/metabolismo , Ácido Láctico , Masculino , Oxirredução/efeitos dos fármacos , Piruvatos/metabolismo , Ácido PirúvicoRESUMO
In vitro researches documented that reproterol, as well as salbutamol, is a powerful stimulant of adenyl cyclase activity in the trachea and bronchi but less potent than isoprenaline. The stimulation was antagonized by beta-blockers.
Assuntos
Adenilil Ciclases/metabolismo , Encéfalo/enzimologia , Brônquios/enzimologia , Broncodilatadores/farmacologia , Metaproterenol/análogos & derivados , Miocárdio/enzimologia , Teofilina/análogos & derivados , Traqueia/enzimologia , Adenilil Ciclases/análise , Antagonistas Adrenérgicos beta/farmacologia , Animais , Broncodilatadores/antagonistas & inibidores , Galinhas , Combinação de Medicamentos , Ativação Enzimática , Hipotálamo/enzimologia , Técnicas In Vitro , Metaproterenol/antagonistas & inibidores , Metaproterenol/farmacologia , Teofilina/antagonistas & inibidores , Teofilina/farmacologiaRESUMO
Phosphocreatine has been shown having significant effects on striated skeletal musculature. In fact, it was shown, by experimental researches, that phosphocreatine interfered with the state of fatigue induced in the Mus musculus and in rats, by the swimming test.