Molecular determinants for the action of general anesthetics at recombinant alpha2beta3gamma2 gamma-aminobutyric acidA receptors
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چکیده
منابع مشابه
Colchicine is a competitive antagonist at human recombinant gamma-aminobutyric acidA receptors.
Colchicine is an alkaloid that is used clinically in the treatment of arthritic gout. This potent microtubule disrupting agent has also been used extensively as an experimental tool in studies characterizing the role of the cytoskeleton in a variety of cellular processes. Colchicine has also been used as a selective neurotoxin and in animal models of Alzheimer's disease and epilepsy. Although t...
متن کاملMutational analysis of molecular requirements for the actions of general anaesthetics at the gamma-aminobutyric acidA receptor subtype, alpha1beta2gamma2
BACKGROUND: Amino acids in the beta subunit contribute to the action of general anaesthetics on GABA(A) receptors. We have now characterized the phenotypic effect of two beta subunit mutations in the most abundant GABA(A) receptor subtype, alpha1beta2gamma2. RESULTS: The beta2(N265M) mutation in M2 decreased the modulatory actions of propofol, etomidate and enflurane, but not of alphaxalone, wh...
متن کاملColchicine Is a Competitive Antagonist at Human Recombinant g-Aminobutyric AcidA Receptors
Colchicine is an alkaloid that is used clinically in the treatment of arthritic gout. This potent microtubule disrupting agent has also been used extensively as an experimental tool in studies characterizing the role of the cytoskeleton in a variety of cellular processes. Colchicine has also been used as a selective neurotoxin and in animal models of Alzheimer’s disease and epilepsy. Although t...
متن کاملCompounds Exhibiting Selective Efficacy for Different Subunits of Human Recombinant -Aminobutyric AcidA Receptors
Inhibitory GABAA receptor modulators are widely used therapeutic agents for a variety of central nervous system disorders. Ltk cells stably expressing human recombinant GABAA subunits ( 1 1–3 2s) were seeded into 96-well plates, loaded with chlorocoumarin-2-dimyristoyl phosphatidylethanolamine and bis(1,3-diethyl-2-thiobarbiturate)trimethineoxonol, and rapid fluorescence resonance energy transf...
متن کاملMutational analysis of molecular requirements for the actions of general anaesthetics at the γ-aminobutyric acidA receptor subtype, α1β2γ2
BACKGROUND Amino acids in the beta subunit contribute to the action of general anaesthetics on GABA(A) receptors. We have now characterized the phenotypic effect of two beta subunit mutations in the most abundant GABA(A) receptor subtype, alpha1beta2gamma2. RESULTS The beta2(N265M) mutation in M2 decreased the modulatory actions of propofol, etomidate and enflurane, but not of alphaxalone, wh...
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ژورنال
عنوان ژورنال: Journal of Neurochemistry
سال: 2002
ISSN: 0022-3042,1471-4159
DOI: 10.1046/j.0022-3042.2001.00682.x