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BioAssay: AID 265567

Effect on GABA-A-induced 36chloride ion influx in mouse embryo cortical neurons at 10 uM relative to basal value

A GABA(A) receptor study of several B-nor analogues of allopregnanolone and pregnanolone has been carried out. B-norallopregnanolone (i.e., 3alpha-hydroxy-7-nor-5alpha-pregnan-20-one) was found comparable to allopregnanolone when measured with labeled TBPS. Analogous results were obtained from their effect on neurons in culture: this time, both 3alpha-hydroxy-7-nor-5xi-pregnan-20-ones (5 and 6) more ..
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 Tested Compounds
 Tested Compounds
All(14)
 
 
Unspecified(14)
 
 
 Tested Substances
 Tested Substances
All(14)
 
 
Unspecified(14)
 
 
 Related BioAssays
 Related BioAssays
AID: 265567
Data Source: ChEMBL (359603)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-24
Modify Date: 2014-08-25

Data Table ( Complete ):           View All Data
Targets
Sequence: RecName: Full=Gamma-aminobutyric acid receptor subunit alpha-2; AltName: Full=GABA(A) receptor subunit alpha-2; Flags: Precursor
Description ..   
Protein Family: Neurotransmitter-gated ion-channel ligand binding domain
Comment ..   

Gene:GABRA2     Related Protein 3D Structures     More BioActivity Data..


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Tested Compounds:
Description:
Title: Activity of B-nor analogues of neurosteroids on the GABA(A) receptor in primary neuronal cultures.

Abstract: A GABA(A) receptor study of several B-nor analogues of allopregnanolone and pregnanolone has been carried out. B-norallopregnanolone (i.e., 3alpha-hydroxy-7-nor-5alpha-pregnan-20-one) was found comparable to allopregnanolone when measured with labeled TBPS. Analogous results were obtained from their effect on neurons in culture: this time, both 3alpha-hydroxy-7-nor-5xi-pregnan-20-ones (5 and 6) were found to stimulate [3H]flunitrazepam binding and GABA-induced 36Cl- influx. These effects were inhibited by GABA(A) receptor antagonists. Other analogues carrying electronegative substituents (epoxides 9 and 10 and ketone 12) in the B ring were inactive. Similarly, B-normal ketones 17, and 18 and 6-azasteroids 20 and 21 were also inactive. B-Nor analogues 5 and 6 did not induce neurotoxicity at relevant concentrations. A computational analysis of active and inactive neurosteroid analogues allowed the proposal of a 3D pharmacophoric hypothesis of their interaction with the GABA(A) receptor.
(PMID: 16722640)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Functional
Assay Data Source: Scientific Literature
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat%
5Activity standard valueActivity standard valueFloat%

Data Table (Concise)
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