The Effect of Neuroactive Steroids on the GAVA-Benzodiazepine Receptor Complex.
- Author:
Jong Bum LEE
1
;
Hyung Bae PARK
;
Jong Hak LEE
;
Ki Guk PARK
;
Chang Su KIM
;
Hye Soo SUH
;
Jeoung Hee HA
Author Information
1. Department of Psychiatry, College of Medicine, Yeungnam University, Korea.
- Publication Type:Original Article
- Keywords:
Neuroactive steroids;
GABA(A)-benzodiazepine receptor complex
- MeSH:
Animals;
Barbiturates;
Benzodiazepines;
Binding Sites;
Dexamethasone;
Flunitrazepam;
gamma-Aminobutyric Acid;
Ligands;
Muscimol;
Pregnanolone;
Progesterone;
Rats;
Receptors, GABA-A;
Steroids*;
Testosterone
- From:Korean Journal of Psychopharmacology
1997;8(2):218-223
- CountryRepublic of Korea
- Language:Korean
-
Abstract:
Pregnolone[5beta-pregnan-3alpha-ol-one(5beta3alpha)] and allopregnanolone [(5alpha-pregnan-3alpha-ol-20-one(5alpha3alpha))] are neuroactive steroids that are reduced metabolites of progesterone. It was reported that Neuroactive steroids may have anxiolytic and anticonvulsant action similar to benzodiazepines and barbiturates. Therefore, the present study was designed to assess the interaction of steroids with GABAA-benzodiazepine receptor complex. The effect of steroids on the ligands binding to GABAA receptor complex was investigated using rat cortices. 5beta3alpha and 5alpha3alpha enhanced the binding of [3H] flunitrazepam to GABAA receptor, but testosterone, progesterone and dexamethasone did not. GABA also showed the enhancement of [3H] flunitrazepam binding, but did not show the additive effect. Unlike to GABA, 5beta3alpha and 5alpha3alpha did not affect on the [3H] muscimol binding to rat cortices. From these findings, it can be concluded that Neuroactive steroids are potent positive modulators of the GABA A receptor, and do not act at GABA binding site.
