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BioAssay: AID 320061

Displacement of [3H]cystisine from nicotinic alpha-4-beta-2 receptor in rat brain

Novel nicotinic ligands, characterized by the presence of an amino substituted cyclopropane ring connected to a pyridine nucleus, are described. Pharmacological investigation revealed that these compounds exhibit highest affinity for the rat alpha4beta2 subtype of the nicotinic receptor with no affinity for the muscarinic receptor. No appreciable affinity for the muscular or for the ganglionic nicotinic receptor was observed at concentrations up to 10 microM. The increase in cortical ACh release as well as a positive effect on memory in a social recognition test in rat are exemplified. ..more
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 Tested Compounds
 Tested Compounds
All(27)
 
 
Active(27)
 
 
 Tested Substances
 Tested Substances
All(27)
 
 
Active(27)
 
 
AID: 320061
Data Source: ChEMBL (468087)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2014-05-25

Data Table ( Complete ):           View Active Data    View All Data
Targets
Sequence: RecName: Full=Neuronal acetylcholine receptor subunit beta-2; AltName: Full=Neuronal acetylcholine receptor non-alpha-1 chain; Short=N-alpha 1; Flags: Precursor
Description ..   
Protein Family: Neurotransmitter-gated ion-channel ligand binding domain
Comment ..   

Gene:CHRNB2     Related Protein 3D Structures     More BioActivity Data..


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BioActive Compounds: 27
Description:
Title: Preparation and affinity profile of novel nicotinic ligands.

Abstract: Novel nicotinic ligands, characterized by the presence of an amino substituted cyclopropane ring connected to a pyridine nucleus, are described. Pharmacological investigation revealed that these compounds exhibit highest affinity for the rat alpha4beta2 subtype of the nicotinic receptor with no affinity for the muscarinic receptor. No appreciable affinity for the muscular or for the ganglionic nicotinic receptor was observed at concentrations up to 10 microM. The increase in cortical ACh release as well as a positive effect on memory in a social recognition test in rat are exemplified.
(PMID: 18262785)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: tissue-based format

Assay Tissue: Brain

Target Type: Target is a defined protein complex, consisting of multiple subunits

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ki*Ki PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6Ki activity commentKi activity commentString
7Ki standard flagKi standard flagInteger
8Ki qualifierKi qualifierString
9Ki published valueKi published valueFloatnM
10Ki standard valueKi standard valueFloatnM
11Ki binding domainsKi binding domainsString

* Activity Concentration.

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