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BioAssay: AID 265566

Increase in [3H]flunitrazepam binding to GABA-A receptor in mouse embryo cortical neurons

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)
 
 
Inactive(9)
 
 
Inconclusive(1)
 
 
Unspecified(4)
 
 
 Tested Substances
 Tested Substances
All(14)
 
 
Inactive(9)
 
 
Inconclusive(1)
 
 
Unspecified(4)
 
 
 Related BioAssays
 Related BioAssays
AID: 265566
Data Source: ChEMBL (359602)
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: Binding
Assay Data Source: Scientific Literature
Result Definitions
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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
6Log EC50 activity commentLog EC50 activity commentString
7Log EC50 standard flagLog EC50 standard flagInteger
8Log EC50 qualifierLog EC50 qualifierString
9Log EC50 published valueLog EC50 published valueFloat
10Log EC50 standard valueLog EC50 standard valueFloat

Data Table (Concise)
Data Table ( Complete ):     View All Data
Classification
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