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Effects of corazol on the regulation of GABAa receptor-channel complex

Kryzhanovskiĭ, G.N.; Rebrov, I.G.; Glebov, R.N.

Biulleten' Eksperimental'noi Biologii i Meditsiny 114(9): 249-252

1992

ISSN/ISBN: 0365-9615
PMID: 1335797
Document Number: 393097
Effects of corazol (pentylenetetrazole, PTZ) on the GABAA receptor-channel complex mediated 36Cl- influx into synaptoneurosomes isolated from rat cerebral cortex, were studied. PTZ inhibited the 36Cl- influx stimulated by a GABA agonist, muscimol, concentration-dependently with an IC50 of 2.11 +/- 0.25 mM. In addition, the rate of muscimol-dependent desensitization of the GABAA receptor-channel complex was significantly reduced in the presence of PTZ. Apparently, the superimposition of these two mutually opposing effects is the cause of a mixed (competitive/noncompetitive) type of inhibition displayed by PTZ. The rate of desensitization of GABAA receptor-channel complex is suggested to be regulated by intracellular concentration of Cl- through a feed-back mechanism.

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