RESUMO
The toxicity of new gamma-carboline derivative [ethyl 3-(8-fluoro-2-methyl-2,3,4,5-tetrahydro-1H-gamma-carbolin-5-yl)-propionate dihydrochloride, CD-008-040] has been studied.
Assuntos
Antialérgicos/efeitos adversos , Antialérgicos/farmacologia , Carbolinas/efeitos adversos , Carbolinas/farmacologia , Animais , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Humanos , Masculino , CamundongosRESUMO
The influence of ethyl-3-(8-fluoro-2-methyl-2,3,4,5-tetrahydro-1H-gamma-carboline-5-yl)propionate dihydrochloride belonging to the class of gamma-carbolines on the allergic reactions (inflammation and systemic anaphylaxis) has been studied on laboratory animals. It was established that the given substance administered in a dose of 5 - 20 mg/kg exhibits a pronounced antiallergic action. Unlike many other antihistamine drugs, this gamma-carboline derivative probably does not produce sedative effect.
Assuntos
Antialérgicos/uso terapêutico , Carbolinas/uso terapêutico , Antagonistas dos Receptores Histamínicos/uso terapêutico , Anafilaxia/tratamento farmacológico , Anafilaxia/imunologia , Animais , Cobaias , Inflamação/tratamento farmacológico , Inflamação/imunologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Endogâmicos CBARESUMO
The properties of 2,3,4,5-tetrahydro-1H-gamma-carbolines containing acid, ether, and amido-substituents, were assessed as potential antagonists of histamine H1 receptors (H1R), capable of blocking histamine-induced calcium fluxes in SK-N-SH cells. The structure--activity relationship for their antagonistic activity is discussed. Among the gamma-carbolines used in the study, the antihistamine activity considerably depends on the nature of substituents in positions 2, 5, and 8 of the heterocycle. The most active antagonist, ethyl 3-(2-methyl-8-fluoro-2,3,4,5-tetrahydro-1H-gamma-carboline-5-yl)propionate, with high affinity to the H1R (Ki = 6.5 nM), produces no adverse effects on motor activity of mice in doses 1-40 mg/kg, which shows the absence of a sedative effect.
Assuntos
Cálcio/metabolismo , Carbolinas/farmacologia , Antagonistas dos Receptores Histamínicos H1/farmacologia , Atividade Motora/efeitos dos fármacos , Receptores Histamínicos H1/metabolismo , Animais , Carbolinas/química , Linhagem Celular , Avaliação Pré-Clínica de Medicamentos , Antagonistas dos Receptores Histamínicos H1/química , Masculino , Camundongos , Relação Estrutura-AtividadeRESUMO
The paper outlines materials on how to improve a method for indication of water viral pollution in different water objects of the environment, by applying a MFM filtration module based on tangentially radial-mode water microfiltration and viral concentration on the positively charged membranes, by using the secondary stage of concentration. Experimental and full-scale studies have demonstrated that this method for virus isolation has a high effectiveness and is based on the employment of the materials made in Russia. This determines its rapid introduction into the system for the sanitary-virological monitoring of practical laboratories of various departments, which will favor the higher efficiency of epidemiological surveillance as an integral part of nonspecific prophylactic measures of virus infections of water etiology.
