gamma-Hydroxybutyric acid binding sites: interaction with the GABA-benzodiazepine-picrotoxin receptor complex.
The effect of three compounds known to allosterically modulate binding to the GABA/benzodiazepine/picrotoxin receptor complex on 4-hydroxy-2,3 [3H]butyric acid (GHB) binding was investigated. Pentobarbital, pentylenetetrazole, and picrotoxin enhanced [3H]GHB binding in a dose dependent fashion. Pentobarbital enhanced 4-hydroxy-2,3 [3H]butyric acid binding was associated with an increase in Bmax while pentylenetetrazole and picrotoxin altered the affinity of GHB for its binding site producing a decrease in Kd. These findings suggest that the GHB and GABA receptor complex may share certain moieties in common.
Snead
O C
OC
Division of Neurology, Childrens Hospital, Los Angeles, California.
Nichols
A C
AC
Liu
C C
CC
D000818:Animals; D001921:Brain / Q000378:metabolism*; D008297:Male; D010424:Pentobarbital / Q000494:pharmacology; D010433:Pentylenetetrazole / Q000494:pharmacology; D010852:Picrotoxin / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011963:Receptors, GABA-A / Q000187:drug effects / Q000378:metabolism*; D012978:Sodium Oxybate / Q000378:metabolism; D013570:Synaptic Membranes / Q000378:metabolism*; D005680:gamma-Aminobutyric Acid / Q000378:metabolism*
D010424:Pentobarbital; D010433:Pentylenetetrazole; D010852:Picrotoxin; D011963:Receptors, GABA-A; D012978:Sodium Oxybate; D005680:gamma-Aminobutyric Acid; C037480:picrotoxinin receptor