RESUMO
Nuclear polyadenylate polymerase from I activity in the brains of seizure-prone EL mice was significantly higher than in seizure-non-susceptible progenitor ddY mice. This finding may be essential in acquiring susceptibility to seizures, since there was no significant difference between EL(S) mice and those that did not receive stimulation, EL(NS) mice. Lower form II enzymatic activity was observed in both groups of EL mice but not in ddY mice. Moreover, significantly lower activities of form II 7 days after seizures were found in EL(S) mice compared with EL(NS) mice, suggesting that this is a consequence of repeated seizures. The activity of form I enzyme decreased immediately and at 30 and 60 min after seizures, then returned to control levels at 100 min. Form II enzymatic activity was significantly decreased only at 30 min after seizures, implying that seizures exerted a later effect on form II enzyme. These changes may cause a decrease in the rate of polyadenylation in the brain; thus, alteration of post-transcriptional events, including messenger RNA processing and transport, may occur during epileptic seizures.
Assuntos
Encéfalo/enzimologia , Epilepsia/enzimologia , Polinucleotídeo Adenililtransferase/metabolismo , Convulsões/etiologia , Animais , Modelos Animais de Doenças , Camundongos , RNA Mensageiro/metabolismo , Convulsões/fisiopatologiaAssuntos
Química Encefálica/fisiologia , Biossíntese de Proteínas , RNA Mensageiro/biossíntese , Convulsões/metabolismo , Animais , Autorradiografia , Química Encefálica/genética , Sistema Livre de Células , Eletroforese em Gel de Poliacrilamida , Metionina/metabolismo , Camundongos , Camundongos Endogâmicos , Convulsões/genéticaRESUMO
The structure of vasodilating active substances, Mer-A2026A and B, produced by Streptomyces pactum Me2108 were determined on the basis of their spectral and chemical properties.
Assuntos
Piridinas/química , Vasodilatadores/química , Conformação Molecular , Piridinas/farmacologia , Análise Espectral , Streptomyces/metabolismo , Vasodilatadores/farmacologiaRESUMO
A strain of Streptomyces was found to produce new piericidins. The compounds were purified and separated into two substances named Mer-A2026A and B. These new piericidins exhibited vasodilating and depressor activities.
Assuntos
Piridinas/isolamento & purificação , Streptomyces/metabolismo , Vasodilatadores/isolamento & purificação , Animais , Anti-Hipertensivos/isolamento & purificação , Anti-Hipertensivos/metabolismo , Anti-Hipertensivos/farmacologia , Fermentação , Masculino , Piridinas/farmacologia , Ratos , Ratos Endogâmicos SHR , Ratos Sprague-Dawley , Streptomyces/classificação , Vasodilatadores/farmacologiaRESUMO
The therapeutic efficacy, utility and safety of bifemelane hydrochloride were studied in 52 elderly depressive patients. The drug was administered as a tablet containing 50 mg orally three times daily for 8 consecutive weeks. The final global improvement rating and global utility rating were respectively 80.8 and 73.1 percent for all patients. The improvement rates on the Hamilton depression rating scale (HAM-D) were more than 60% for depressed mood, guilt, suicide, middle insomnia, delayed insomnia, psychotic anxiety, gastro-intestinal symptom, hypochondriasis, depersonalization and derealization. The rates regarding global symptoms evaluated by the Psychoneurotic rating scale for doctor's use were more than 60% for tension, agitation, irritability and excitement, phobia, depression, hypochondria and nocturnal delirium in psychotic symptoms, and insomnia in addition to palpitation in somatic symptoms. A significant decrease was also observed in the symptoms covered by the Self-rating depression scale of Zung after treatment with this drug. There were no instances of side-effects, nor any abnormalities in laboratory tests, encountered throughout the trial. Therefore, bifemelane hydrochloride is of value for the treatment of geriatric depression.
Assuntos
Antidepressivos/uso terapêutico , Compostos Benzidrílicos/uso terapêutico , Transtorno Depressivo/tratamento farmacológico , Idoso , Antidepressivos/efeitos adversos , Compostos Benzidrílicos/efeitos adversos , Transtorno Depressivo/psicologia , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Escalas de Graduação PsiquiátricaRESUMO
Fourty-five schizophrenic inpatients were randomly assigned to bromperidol or sulpiride in an 8 week single-blind clinical trial. No statistically significant differences were observed for final global improvement rating. Regarding BPRS items and compared to sulpiride, bromperidol was particularly effective to relieve emotional withdrawal and hallucinatory behavior, although the only significant between group difference was in favour of sulpiride for improvements of somatic concern. No significant differences were observed for all PES items, although sulpiride was found more effective for hypochondriasis and neurotic complaint as was bromperidol for hallucination and disturbance of self-conscious. The rate of side-effects and abnormal laboratory test results were comparable in the two groups. They were not severe enough to require termination of administration. Bromperidol and sulpiride are concluded to have different clinical profile in the treatment of schizophrenic hospitalized patients.
Assuntos
Haloperidol/análogos & derivados , Esquizofrenia/tratamento farmacológico , Sulpirida/uso terapêutico , Adulto , Escalas de Graduação Psiquiátrica Breve , Feminino , Haloperidol/efeitos adversos , Haloperidol/uso terapêutico , Hospitalização , Humanos , Masculino , Pessoa de Meia-Idade , Esquizofrenia/diagnóstico , Método Simples-Cego , Sulpirida/efeitos adversosRESUMO
The hybridization kinetics in the complementary DNAs (cDNA) to polyadenylated messenger RNA (mRNA) in the brain of seizure-susceptible El mice were examined to elucidate the correlation between seizure susceptibility and genetic expression. Homologous and heterologous saturation hybridizations indicated that cDNA of seizure-nonsusceptible ddY mice hybridized with less mRNA in seizure-experienced El(+) or seizure-nonexperienced El(o) mice than that in ddY mice, cDNA of El(+) mice hybridized to a lesser extent with mRNA of El(o) mice than that of ddY or El(+) mice, and no difference was observed with cDNA hybridization results of El(o) mice to individual mRNAs of ddY, El(+) or El(o) mice. The results suggest that some sequences found in mRNA of ddY are lacking in both El strains and are responsible for the inbred predisposition, while those present in El(+) mRNA but missing in El(o) may associate with seizure susceptibility, since common sequences are present in the mRNA of those groups of animal. The sequence diversity among the 3 groups of mice was mainly observed with the rare class of mRNA. Molecular cloning of the cDNA corresponding to this class of mRNA found in the El(+) mice would clarify the gene expression in the brains of epileptics.