Effect of muscimol on the picrotoxinand bicuculline-induced delay in the desensitization of the GABA receptor/Cl? channel complex |
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Authors: | I G Rebrov G N Kryzhanovskii N P Belykh T F Shukalova R N Glebov |
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Institution: | (1) Institute of General Pathology and Pathophysiology, Russian Academy of Medical Sciences, Moscow |
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Abstract: | Effects of picrotoxin and bicuculline on the muscimol-dependent36Cl− entry into synaptoneurosomes of the rat cerebral cortex are examined as well as desensitization of36Cl− entry at muscimol concentrations of 5 and 50 μM. At the 5 μM concentration (which is close to the muscimol IC50), picrotoxin and bicuculline inhibited Cl− entry into synaptoneurosomes and decreased the desensitization. At the 50 μM concentration, muscimol completely abolishes
the bicuculline effects both on Cl− entry and desensitization. Inhibition of Cl− entry by picrotoxin is also abolished by 50 μM muscimol, whereas the picrotoxin-induced decrease in the desensitization rate
is not. It is shown that both bicuculline effects result from inhibition of the GABA receptor, but the action of picrotoxin
on the desensitization of Cl− entry into synaptoneurosomes is not closely related to the functional activity of the GABA receptor/Cl− channel complex.
Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 122, No. 8, pp. 144–147, August, 1996 |
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Keywords: | desensitization GABA receptor/Cl − channel complex muscimol picrotoxin bicuculline 36Cl− synaptoneurosomes |
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