Partial agonists acting at benzodiazepine receptors can be differentiated in tests of ingestional behaviour.
Several categories of compounds active at benzodiazepine receptors (BZR) in the brain have been distinguished: agonists, antagonists and the novel category of inverse agonist. In terms of their effects on ingestional responses (e.g., food, saline and water consumption), agonists increase levels of intake, inverse agonists reduce intake in some, if not all, tests, while antagonists block the effects of both agonists and inverse agonists. Attention is currently focussed upon a range of compounds which fall between full agonists and antagonists. These partial agonists are of particular interest since they act more selectively than full agonists, retaining effects in animal models of anxiolytic and anticonvulsant activity, for example, while largely lacking behaviourally-depressant effects. Recent data indicate that tests of ingestional behaviour distinguish between various BZR partial agonists. The benzodiazepines Ro23-0364, Ro16-6028 and Ro17-1812, as well as the beta-carboline ZK 91296, enhanced ingestional responses. The pyrazoloquinolines, CGS 9895 and CGS 9896, did not, but antagonized agonist-induced increases in ingestion.
Cooper
S J
SJ
Department of Psychology, University of Birmingham, U.K.
Yerbury
R E
RE
Neill
J C
JC
Desa
A
A
D000818:Animals; D014151:Anti-Anxiety Agents; D001569:Benzodiazepines / Q000494:pharmacology*; D001570:Benzodiazepinones / Q000494:pharmacology; D002243:Carbolines / Q000494:pharmacology*; D005247:Feeding Behavior / Q000187:drug effects*; D011720:Pyrazoles / Q000494:pharmacology*; D051381:Rats; D011963:Receptors, GABA-A / Q000187:drug effects*
D014151:Anti-Anxiety Agents; D001570:Benzodiazepinones; D002243:Carbolines; D011720:Pyrazoles; D011963:Receptors, GABA-A; D001569:Benzodiazepines; C034704:2-(4-chlorophenyl)-2,5-dihydropyrazolo(4,3-c)quinoline-3(3H)-one; C039232:2,5-dihydro-2-(4-methoxyphenyl)-3H-pyrazolo(4,3-c)quinolin-3-one; C038933:ZK 91296; C049715:Ro 17-1812; C054626:bretazenil; C053272:Ro 23-0364