CNS depressants accelerate the dissociation of 35S-TBPS binding and GABA enhances their displacing potencies

G. Maksay; M. K. Ticku

doi:10.1016/0024-3205(88)90589-9

CNS depressants accelerate the dissociation of ³⁵S-TBPS binding and GABA enhances their displacing potencies

G. Maksay, M. K. Ticku

Department of Pharmacology

Resultado de la investigación: Article › revisión exhaustiva

12 Citas (Scopus)

Resumen

The specific binding of ³⁵S-t-butylbicyclophos-phorothionate (TBPS) was studied in synaptosomal membranes of rat cerebral cortex. The displacing potencies of eleven CNS depressants and three convulsants were determined in the presence of 1 μM GABA and 10 nM R 5135. GABA enhanced the displacing potencies of depressants of most diverse chemical structures: diaryltriazine (LY 81067), pyrazolopyridine (etazolate), cinnamide, glutarimide, 2, 3-benzodiazepine (tofizopam) and alcohol derivatives, barbiturates, (+) etomidate, methaqualone and meprobamate. In contrast, the IC₅₀ values of convulsants (picrotoxinin, pentetrazol and the barbiturate enantiomer S(+) MPPB) were not significantly affected. The depressants accelerated either basal or GABA-augmented dissociation of ³⁵-TBPS mainly by increasing the contribution of its rapid first phase.

Idioma original	English (US)
Páginas (desde-hasta)	1331-1337
Número de páginas	7
Publicación	Life Sciences
Volumen	43
N.º	16
DOI	https://doi.org/10.1016/0024-3205(88)90589-9
Estado	Published - 1988

ASJC Scopus subject areas

Biochemistry, Genetics and Molecular Biology(all)
Pharmacology, Toxicology and Pharmaceutics(all)

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10.1016/0024-3205(88)90589-9

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title = "CNS depressants accelerate the dissociation of 35S-TBPS binding and GABA enhances their displacing potencies",

abstract = "The specific binding of 35S-t-butylbicyclophos-phorothionate (TBPS) was studied in synaptosomal membranes of rat cerebral cortex. The displacing potencies of eleven CNS depressants and three convulsants were determined in the presence of 1 μM GABA and 10 nM R 5135. GABA enhanced the displacing potencies of depressants of most diverse chemical structures: diaryltriazine (LY 81067), pyrazolopyridine (etazolate), cinnamide, glutarimide, 2, 3-benzodiazepine (tofizopam) and alcohol derivatives, barbiturates, (+) etomidate, methaqualone and meprobamate. In contrast, the IC50 values of convulsants (picrotoxinin, pentetrazol and the barbiturate enantiomer S(+) MPPB) were not significantly affected. The depressants accelerated either basal or GABA-augmented dissociation of 35-TBPS mainly by increasing the contribution of its rapid first phase.",

author = "G. Maksay and Ticku, {M. K.}",

note = "Funding Information: Technical assistance of Ms. Andrea Martinek is appreciated. Nonlinear computer fitting is thanked to Dr. Istv~n Lukovits. This study was supported by a grant of the Hungarian Academy of Sciences no. AKA-I-3-86-340 and a NIH grant NS-15339.",

year = "1988",

doi = "10.1016/0024-3205(88)90589-9",

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AU - Ticku, M. K.

N1 - Funding Information: Technical assistance of Ms. Andrea Martinek is appreciated. Nonlinear computer fitting is thanked to Dr. Istv~n Lukovits. This study was supported by a grant of the Hungarian Academy of Sciences no. AKA-I-3-86-340 and a NIH grant NS-15339.

PY - 1988

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N2 - The specific binding of 35S-t-butylbicyclophos-phorothionate (TBPS) was studied in synaptosomal membranes of rat cerebral cortex. The displacing potencies of eleven CNS depressants and three convulsants were determined in the presence of 1 μM GABA and 10 nM R 5135. GABA enhanced the displacing potencies of depressants of most diverse chemical structures: diaryltriazine (LY 81067), pyrazolopyridine (etazolate), cinnamide, glutarimide, 2, 3-benzodiazepine (tofizopam) and alcohol derivatives, barbiturates, (+) etomidate, methaqualone and meprobamate. In contrast, the IC50 values of convulsants (picrotoxinin, pentetrazol and the barbiturate enantiomer S(+) MPPB) were not significantly affected. The depressants accelerated either basal or GABA-augmented dissociation of 35-TBPS mainly by increasing the contribution of its rapid first phase.

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