Assuntos
Amino Álcoois/síntese química , Amino Álcoois/farmacologia , Animais , Camundongos , CoelhosRESUMO
Three new derivatives of morphine: O3-(beta-isopropylaminoethyl) ether of morphine (T .3289), O3, O6-[N,N'-bis(methylcarbamate] ester of morphine (T .3298) and beta-dimethylamino-ethyl-ether of dihydromorphinone (T .3403) were tested for their action on CNS. A detailed study of pain threshold, motor activity, conditioned behavior and noradrenaline levels in brain was carried out. The compounds T .3289 and T .3298 exhibited analgesic action. The spontaneous activity of rats was decreased by T .3289 and increased by T .3298. The conditioned avoidance response was decreased and the brain nor-adrenaline levels were altered.
Assuntos
Derivados da Morfina/farmacologia , Analgésicos , Animais , Aprendizagem da Esquiva/efeitos dos fármacos , Química Encefálica/efeitos dos fármacos , Feminino , Camundongos , Atividade Motora/efeitos dos fármacos , Ratos , Fatores de TempoRESUMO
The geometry of the condensation products between ethyl cyanoacetate and 20-ketosteroids (5 alpha-pregnane-20-one, 3 beta-hydroxypregn-5-en-20-one and 3 beta-acetoxypregn-5-en-20-one) was established by NMR spectra. Reduction of these steroid C-20 alkylidene cyanoacetates was shown to afford one of the two possible 20-C epimers, which seen to correspond to the 20 beta-methyl configuration.