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Tucumanin, a β-hydroxy-γ-lactone bistetrahydrofuranic acetogenin from Annona cherimolia, is a potent inhibitor of mitochondrial complex I
(Georg Thieme Verlag Kg, 2004-09)
A new β-hydroxy-γ-methyl-γ-lactone bistetrahydrofuranic acetogenin, tucumanin, with the infrequent symmetrical threo/trans/threo/trans/ threo relative configuration at the tetrahydrofuran rings was isolated from Annona ...
Drimane Sesquiterpenoids Noncompetitively Inhibit Human α4β2 Nicotinic Acetylcholine Receptors with Higher Potency Compared to Human α3β4 and α7 Subtypes
(American Chemical Society, 2018-04)
The drimane sesquiterpenoids drimenin, cinnamolide, dendocarbin A, and polygodial were purified from the Canelo tree (Drimys winteri) and chemically characterized by spectroscopic methods. The pharmacological activity of ...
Desenvolvimento e padronização de um ensaio in vitro para determinação da potência neutralizante de antivenenos antibotrópicos
(Universidade Federal de Minas GeraisBrasilICB - DEPARTAMENTO DE BIOQUÍMICA E IMUNOLOGIAPrograma de Pós-Graduação em Bioquímica e ImunologiaUFMG, 2019-06-19)
Accidents with poisonous snakes are a major health hazard in tropical countries. Bothrops genus is responsible for more than 70 % of snakebites in Brazil. Immunotherapy is the only recommended specific treatment against ...
Analgesic and behavioral effects of amphetamine enantiomers, p-methoxyamphetamine and n-alkyl-p-methoxyamphetamine derivatives
(PERGAMON-ELSEVIER SCIENCE LTD, 2004-10)
The analgesic effects of (+)- and (-)-amphetamine (AMPH), (+/-)-p-methoxyamphetamine (MA), (+/-)-N-methyl-p-methoxyamphetamine (MMA) and (+/-)-N-ethyl-p-methoxyamphetamine (EMA) were compared using two different algesimetric ...
Steroids differentially inhibit the nicotinic acetylcholine receptor
(Lippincott Williams, 2001-12-02)
The effect of various natural and synthetic steroids on the function of the nicotinic acetylcholine receptor (AChR) was studied at the single-channel level. AChR channel kinetics was affected by some substitutions in the ...
The Inhibitory Activity of Plants from Central Argentina on p-Hydroxyphenylpyruvate Dioxygenase: Isolation and Mechanism of Inhibition of a Flavanone from Flourensia oolepis
(Georg Thieme Verlag Kg, 2015-10)
The enzyme 4-hydroxyphenylpyruvate dioxygenase catalyzes the second step in the tyrosine degradation pathway. In mammals, this enzyme is the molecular target of drugs used for the treatment of metabolic disorders associated ...
Impact of impurity on kinetic estimates from transport and inhibition studies
(AMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICS, 2008)
Although in vitro transport/inhibition studies are commonly performed on impure drug candidates to screen for pharmacokinetic properties in early development, quantitative guidelines concerning acceptable impurity levels ...
[D-Leu1]MC-LR has lower PP1 inhibitory capability and greater toxic potency than MC-LR in animal and plant tissues
(Multidisciplinary Digital Publishing Institute, 2020-10-01)
Two microcystins, MC-LR and [D-Leu1]MC-LR, present in La Plata Basin blooms, are differentiated by substitution of D-Alanine for D-Leucine at position 1. Our objective was to evaluate acute toxicity of [D-Leu1]MC-LR and ...
MONOAMINE OXIDASE INHIBITORY EFFECTS OF SOME 4-AMINOPHENETHYLAMINE DERIV ATIVES
(Elsevier Science Ltd., 1993-11-13)
The in vitra and ex viva monoamine oxidase (MAO) inhibitory effects of (±)4-dimethylaminoa-
methyl-phenethylamine (4-DMAA) and (± )4-methylamino-a-methyl-phenethylamine (4-MAA) were
reassessed, in comparison with the ...