RESUMO
The neuroleptic, analgesic, antiinflammatory, antihypoxic, diuretic, bacteriostatic, and fungistatic activity of bicyclic noncondensed thiazolidons-2 with alkylene and aryl bridges was studied. Certain regularities in the relations between the structure of the compounds under study and their biological activity were found.
Assuntos
Tiazóis/farmacologia , Analgésicos/farmacologia , Analgésicos/toxicidade , Animais , Anti-Infecciosos/farmacologia , Anti-Infecciosos/toxicidade , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/toxicidade , Antifúngicos/farmacologia , Antifúngicos/toxicidade , Antipsicóticos/farmacologia , Antipsicóticos/toxicidade , Diuréticos/farmacologia , Diuréticos/toxicidade , Feminino , Masculino , Camundongos , Ratos , Relação Estrutura-Atividade , Tiazóis/toxicidadeRESUMO
The effect of cholinergic agents on the analgetic effect of analgin (pyrazoline derivative) and chemical compounds (quinazoline and triazole derivatives) has been studied in experiments on white mice using a "hot plate" technique. It has been found that an M-cholinomimetic pilocarpine decreases pain sensitivity and enhances considerably the analgetic effect of non-narcotic analgesics, especially that of quinazoline and triazole derivatives. At high doses (10 mg/kg) pilocarpine increases drastically the toxicity of analgin. Contrastingly, an M-cholinoblocker atropine does not affect considerably the pain sensitivity, however blocks completely the analgetic effect of all the drugs studied. The role of cholinergic mechanisms in the maintenance of pain sensitivity level and the onset of the analgetic effect of non-narcotic analgesics as well as the clinical value of the data obtained are discussed.
Assuntos
Analgésicos/farmacologia , Parassimpatomiméticos/farmacologia , Aminopirina/farmacologia , Animais , Sinergismo Farmacológico , Feminino , Camundongos , Pilocarpina/farmacologiaRESUMO
The action of adrenoblocking agents on the dynamics of the pain allaying effect of narcotic analgesics, measured by the magnitude of the pain reaction threshold after irritation of the tail skin with electric current was studies in tests on mice. The beta-adreno-blocking agent (anaprillin or inderal) was found to significantly potentiate and to lengthen the action of morphine, and so did, to a lesser degree, promedol (trimeperedin) and phentanyl, while the alpha-adrenoblocking agent (phentolamine) weakened the analgesic effects of morphine and promedol, without having any essential influence on the effect of phentanyl. Phentolamine does not eliminate the potentiating effect of anapraline on the analgesic action of morphine but is capable to lessen it.
Assuntos
Analgésicos Opioides/farmacologia , Dor/tratamento farmacológico , Simpatolíticos/farmacologia , Animais , Interações Medicamentosas , Sinergismo Farmacológico , Feminino , Fentanila/farmacologia , Camundongos , Morfina/farmacologia , Fentolamina/farmacologia , Promedol/farmacologia , Propranolol/farmacologia , Fatores de TempoRESUMO
A study is presented of the carbohydrate energy metabolism and processes of peroxidation in rats with experimental pitutrin-isadrin myocardial infarction. Essential changes of these values were noted. It is concluded that quinasopyrin and preparation E normalize to a greater extent and riboxin to a smaller extent metabolic disorders in the ischemia-involved myocardium tissues.
Assuntos
Fármacos Cardiovasculares/uso terapêutico , Inosina Difosfato/uso terapêutico , Nucleotídeos de Inosina/uso terapêutico , Infarto do Miocárdio/tratamento farmacológico , Quinazolinas/uso terapêutico , Animais , Avaliação Pré-Clínica de Medicamentos , Coração/efeitos dos fármacos , Isoproterenol , Masculino , Infarto do Miocárdio/induzido quimicamente , Infarto do Miocárdio/metabolismo , Miocárdio/metabolismo , Hormônios Neuro-Hipofisários , Ratos , Ratos EndogâmicosRESUMO
The effect of quinazopyrine on skin wound healing in rats was studied. Quinazopyrine was found to stimulate synthesis of nucleic acids, maturation of fibroblasts and to increase mechanical strength of the postoperative scar. This effect retains in animals with alloxan-induced diabetes. The wound-healing activity of quinazopyrine was higher than that of methyluracil, dimexide, pentoxyl, sodium nucleinate, potassium orotate and riboxine.
Assuntos
Quinazolinas/farmacologia , Cicatrização/efeitos dos fármacos , Animais , Diabetes Mellitus Experimental/complicações , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Feminino , Dose Letal Mediana , Masculino , Camundongos , Quinazolinas/administração & dosagem , Quinazolinas/toxicidade , Ratos , Pele/efeitos dos fármacos , Fenômenos Fisiológicos da Pele , Infecções Cutâneas Estafilocócicas/tratamento farmacológico , Estimulação Química , Infecção dos Ferimentos/tratamento farmacológicoRESUMO
During experiments on rats it was established that some methoxy- and nitro-derivatives of acridinyl-9-thioacetic acids possess the hepatoprotective properties contributing to a decrease of the liver tissue cell destruction under the action of CCl4 and lipid peroxidation in the liver.
Assuntos
Acridinas/farmacologia , Antioxidantes/farmacologia , Fígado/efeitos dos fármacos , Acridinas/toxicidade , Alanina Transaminase/sangue , Animais , Antioxidantes/toxicidade , Tetracloreto de Carbono/toxicidade , Malondialdeído/metabolismo , Ratos , Vitamina E/farmacologiaRESUMO
The antiarrhythmic activity of quinasopirine was studied in the experiments on rats with the use of models of calcium chloride- and aconitine-induced arrhythmias, disorders of cardiac rhythm in myocardial infarction produced by isadrine and pituitrin and also in the experiments on cats in arrhythmias caused by electric stimulation of the myocardium, postinfarction and reperfusion arrhythmias. Quinasopirine exhibits the antiarrhythmic effect being superior to that of anapriline and novocainamide in arrhythmias induced by calcium chloride and aconitine. In other types of the cardiac rhythm disorder its activity is comparable with that of ethmosine, obsidane and cordarone. Quinasopirine reduces automatism and contractile function of the myocardium.