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1.
Probl Endokrinol (Mosk) ; 55(5): 28-30, 2009 Oct 15.
Artigo em Russo | MEDLINE | ID: mdl-31569852

RESUMO

This experimental study was designed to evaluate effects of hypo- and hyperthyroidism on the density of 3H-muscimol and 3H-diazepam-binding sites in synaptic membranes of the rat brain. It was shown that density of both 3H-muscimol and 3H-diazepam-binding sites increases in animals with hypothyroidism and decreases in hyperthyroidism. This difference may account for the predominance of general inhibitory reaction in animals with hypothyroidism and general excitation in hyperthyroid rats.

2.
Ukr Biokhim Zh (1978) ; 60(3): 78-81, 1988.
Artigo em Russo | MEDLINE | ID: mdl-2901152

RESUMO

The Argiope lobata venom is shown to block synaptic potential at locust neuromuscular junctions and inhibit the high-affinity sodium independent L[3H]glutamate binding site in locust muscle membranes. The data obtained due to fractionation of venom evidence that it contains components which block synaptic potential and inhibit the binding of L[3H]glutamate (5 kDa and more) as well as components which block synaptic potential but do not inhibit the binding of L[3H]glutamate less than 5 kDa. These observations indicate that spider venom contains at least two components with different mechanism of action.


Assuntos
Venenos de Artrópodes/farmacologia , Glutamatos/metabolismo , Junção Neuromuscular/metabolismo , Venenos de Aranha/farmacologia , Animais , Ligação Competitiva , Ácido Glutâmico , Gafanhotos , Técnicas In Vitro , Peso Molecular , Junção Neuromuscular/efeitos dos fármacos , Venenos de Aranha/isolamento & purificação
3.
Farmakol Toksikol ; 48(2): 38-40, 1985.
Artigo em Russo | MEDLINE | ID: mdl-2987029

RESUMO

It has been shown that tetrodotoxin inhibits GABA-receptor binding of muscimol with solubilized membranes of the rat brain in a competitive manner, with the inhibition constant amounting to about 3 nM. Muscimol has been also demonstrated to competitively inhibit 3H-tetrodotoxin binding with the same drug.


Assuntos
Muscimol/metabolismo , Oxazóis/metabolismo , Receptores de GABA-A/metabolismo , Tetrodotoxina/metabolismo , Animais , Ligação Competitiva/efeitos dos fármacos , Encéfalo/metabolismo , Muscimol/antagonistas & inibidores , Ratos , Solubilidade , Tetrodotoxina/antagonistas & inibidores , Trítio , Ácido gama-Aminobutírico/metabolismo
4.
Ukr Biokhim Zh (1978) ; 54(4): 428-31, 1982.
Artigo em Russo | MEDLINE | ID: mdl-6291205

RESUMO

The Na+-dependent and Na+-independent (receptor) binding of [3H] GABA is measured in rat brain synaptic membranes. The receptor binding is presented by at least 3 types of binding sites differing in kinetic parameters (dissociation constants and maximal concentration of binding sites). Phenyl-GABA and pyracetam do not affect receptor binding while 4-hydroxybutyric acid, apamine and bicuculline inhibit it with inhibition constants K1=100, 2 and 1 micron, respectively. Solubilization of synaptic membranes with 2% potassium cholate in the presence of total brain phospholipids does not inactivate [3H] GABA receptor binding.


Assuntos
Encéfalo/metabolismo , Receptores de Superfície Celular/metabolismo , Membranas Sinápticas/metabolismo , Ácido gama-Aminobutírico/metabolismo , Animais , Cinética , Fosfolipídeos , Ratos , Receptores de Superfície Celular/isolamento & purificação , Receptores de GABA-A , Solubilidade
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