Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H19ClN2O3S |
| Molecular Weight | 402.894 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCC(=O)C1=C(C)N(C(=C1)C2=CC=C(Cl)C=C2)C3=CC=C(C=C3)S(N)(=O)=O
InChI
InChIKey=ABACVOXFUHDKNZ-UHFFFAOYSA-N
InChI=1S/C20H19ClN2O3S/c1-3-20(24)18-12-19(14-4-6-15(21)7-5-14)23(13(18)2)16-8-10-17(11-9-16)27(22,25)26/h4-12H,3H2,1-2H3,(H2,22,25,26)
| Molecular Formula | C20H19ClN2O3S |
| Molecular Weight | 402.894 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Targeting alpha7 neuronal acetylcholine receptors (nAChRs) with selective agonists and positive allosteric modulators (PAMs) is considered a therapeutic approach for managing cognitive deficits in schizophrenia and Alzheimer's disease. A-867744 is a novel type II positive allosteric modulator of α7 nAChR, which was developed by Abbott Laboratories, and has a good potency and selectivity.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Positive allosteric modulation of alpha7 neuronal nicotinic acetylcholine receptors: lack of cytotoxicity in PC12 cells and rat primary cortical neurons. | 2009 Dec |
|
| In vitro pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107. | 2010 Sep 1 |
Patents
Sample Use Guides
In oocytes expressing alpha7 neuronal acetylcholine receptors (nAChRs), A-867744 potentiated acetylcholine (ACh)-evoked currents, with an EC(50) value of approximately 1 uM. In the presence of A-867744, ACh concentration responses were potentiated by increases in potency, Hill slope, and maximal efficacy. When examined in rat hippocampus CA1 stratum radiatum interneurons or dentate gyrus granule cells, A-867744 (10 uM) increased choline-evoked alpha7 currents and recovery from inhibition/desensitization, and enhanced spontaneous inhibitory postsynaptic current activity.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 10:57:39 GMT 2023
by
admin
on
Sat Dec 16 10:57:39 GMT 2023
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| Record UNII |
O6NW23A765
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| Record Status |
Validated (UNII)
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| Record Version |
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1000279-69-5
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