Assuntos
Sesquiterpenos/toxicidade , Animais , Cães , Feminino , Haplorrinos , Macaca mulatta , Gravidez , Coelhos , RatosAssuntos
Álcoois Benzílicos/farmacologia , Compostos de Benzil/farmacologia , Tiofenos/farmacologia , Animais , Anticonvulsivantes , Ataxia/induzido quimicamente , Bile/efeitos dos fármacos , Diurese/efeitos dos fármacos , Interações Medicamentosas , Feminino , Cobaias , Técnicas In Vitro , Lactação/efeitos dos fármacos , Masculino , Camundongos , Atividade Motora/efeitos dos fármacos , Relaxamento Muscular/efeitos dos fármacos , Parassimpatolíticos , Úlcera Péptica/prevenção & controle , Gravidez , Coelhos , Ratos , Reflexo/efeitos dos fármacos , Respiração/efeitos dos fármacos , Sono/efeitos dos fármacosRESUMO
Structure-activity relationships of 90 bronchospasmolytic compenylethyl-aminoalkyl-xanthines are reported. Particularly the influence of substituents in the phenyl moiety as well as of the carbon bridge between the xanthine residue and the beta-phenylethylamine moiety is described. 2. A method is shown for the selection of one optimally bronchospasmolytic substance from many potential compounds synthetised via multiple screening steps to profound biological studies.
Assuntos
Broncodilatadores , Fenetilaminas/farmacologia , Xantinas/farmacologia , Animais , Brônquios/efeitos dos fármacos , Fenômenos Químicos , Química , Cães , Feminino , Cobaias , Frequência Cardíaca/efeitos dos fármacos , Isoproterenol/farmacologia , Masculino , Relação Estrutura-AtividadeRESUMO
Only slight toxicity of 7-(3-[2-(3,5-dihydroxyphenyl-2-hydroxy-ethylamino]-propyl)-theophylline (reproterol, Bronchospasmin) was shown in the examination of acute, subacute and chronic trials on various animal species with different modes of application. Slight side-effects noted with high toxically active dosages correspond with those of other well-known beta-sympathicomimetics. No influence on the pre-,peri- and postnatal development could be proven with doses tolerated by the parent animals.
Assuntos
Fenetilaminas/toxicidade , Xantinas/toxicidade , Anormalidades Induzidas por Medicamentos , Administração Oral , Aerossóis , Animais , Animais Recém-Nascidos , Peso ao Nascer/efeitos dos fármacos , Broncodilatadores/toxicidade , Cães , Feminino , Fertilidade/efeitos dos fármacos , Crescimento/efeitos dos fármacos , Injeções Intravenosas , Dose Letal Mediana , Masculino , Fenetilaminas/administração & dosagem , Gravidez , Coelhos , Ratos , Xantinas/administração & dosagemRESUMO
1. 7-(3-[2-(3,5-Dihydroxyphenyl)-2-hydroxy-ethylamino]-propyl)-theophylline (reproterol, D 1959, Bronchospasmin) was developed as a bronchospasmolytic agent from the structure class of the phenylethyl-aminoalkyl-xanthines. 2. The pharmacological effects characterize reproterol as a bronchospasmolytic with preferential impact on the adrenergic beta2-receptors. 3. In the therapeutic dose range, reproterol stands out because of its nearly non-existent cardiovascular or central nervous side effects. Effects of over and above pharmacodynamically effective doses as well as toxic ones may be reversed with beta1-receptor blockers.
