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TP003
- Soluble in DMSO and EtOH
- MF: C23H16F3N3O
- MW: 407.39
Description
TP003 is an α3-preferring GABAA receptor benzodiazepine-site partial agonist with high efficacy at α3-containing receptor subtypes.
Selective modulation of α2/α3-containing GABAA receptors is used to separate anxiolytic and analgesic effects from the sedation associated mainly with α1-containing receptors. TP003 is a tool compound for GABAA subtype–function studies.
Key Features
- α3-preferring GABAA receptor partial agonist
- Acts at the benzodiazepine allosteric site
- High efficacy at α3-containing receptors
- Supports separation of anxiolytic from α1-mediated sedative effects
Applications
- GABAA receptor subtype profiling
- α3-containing receptor functional assays
- Anxiety and inhibitory-neurotransmission models
- Sedation versus anxiolysis pharmacology studies
More Information
| Parent CAS No. | 628690-75-5 |
|---|---|
| Chemical Name | 4,2'-difluoro-5'-[8-fluoro-7-(1-hydroxy-1-methylethyl)imidazol[1,2-a`]pyridine-3-yl]biphenyl-2-carbonitrile |
| SMILES | C1(C2=CC(C3=CN=C4C(F)=C(C(O)(C)C)C=CN43)=CC=C2F)C(C#N)=CC(F)=CC=1 |
| MFCD | MFCD13152400 |
| InChi | InChI=1S/C23H16F3N3O/c1-23(2,30)18-7-8-29-20(12-28-22(29)21(18)26)13-3-6-19(25)17(10-13)16-5-4-15(24)9-14(16)11-27/h3-10,12,30H,1-2H3 |
| InChiKey | SJMMDWXJSSJHOQ-UHFFFAOYSA-N |
| CID | 10001434 |
| Short Description | GABAA-α3 agonist |
References
- R Dias et al. Evidence for a significant role of alpha 3-containing GABAA receptors in mediating the anxiolytic effects of benzodiazepines. J. Neurosci. 2005, 25(46), 10682–10688.
- RL Fradley et al. Differential contribution of GABA(A) receptor subtypes to the anticonvulsant efficacy of benzodiazepine site ligands. J. Psychopharmacol. 2007, 4, 384-391.
- W Sieghart. GABAA receptors as targets for different classes of drugs. Drugs Fut. 2006, 31(8), 685.
- J Knabl et al. Reversal of pathological pain through specific spinal GABAAreceptor subtypes. Nature 2008, 451, 330-334.
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