PMID: 12367621Oct 9, 2002

Modulation of GABA(A) receptor-mediated currents by benzophenone derivatives in isolated rat Purkinje neurones

Neuropharmacology
M V KopanitsaO A Krishtal

Abstract

We investigated modulation of GABA(A) receptor-mediated whole-cell currents in cerebellar Purkinje neurones by several derivatives of benzophenone. A metabolite of phenazepam, 5-bromo-2'-chloro-2-aminobenzophenone (I), caused dual modification of peak amplitudes of GABA-gated currents that depended upon the concentration of applied GABA and incubation time. Following short 10 s pre-incubations, 1-30 microM I facilitated activation and delayed deactivation of currents evoked by 500 ms pulses of 20 microM GABA. In addition, 10 microM I prominently enhanced desensitisation of currents during applications of 500 microM GABA mainly by decreasing the value of the fast time constant of the desensitisation. Continuous 6 min incubation with 10 microM I during GABA stimulation or its administration between but not during 1 s pulses of 500 microM GABA led to a gradual, partly reversible attenuation of GABA-activated currents. This inhibition was not observed when I was applied only during pulses of GABA, indicating that the blockade was not use-dependent. One of the possible mechanisms of this down-modulation could be an intracellular effect of I, because when applied intracellularly it caused slow inhibition of responses to consecutive G...Continue Reading

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Citations

Mar 7, 2012·Journal of Forensic and Legal Medicine·Peter D MaskellDerrick J Pounder
Apr 25, 2017·Acta Crystallographica. Section E, Crystallographic Communications·Diana Peña-SolórzanoCristian Ochoa-Puentes
Dec 2, 2017·The Journal of Experimental Biology·Sergey Snigirov, Sergiy Sylantyev

Related Concepts

5-bromo-2'-chloro-2-aminobenzophenone
Benzophenones
Cell Separation
Electrophysiology (Science)
Gamma-Aminobutyric Acid, Zinc Salt (2:1)
Ion Channel
Resting Potentials
Van-Pen-G
Picrotoxin
Purkinje Cells

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