Chemical Name: 2',4-Difluoro-5'-[8-fluoro-7-(1-hydroxy-1-methylethyl)imidazo[1,2-a]-pyridin-3-yl]-[1,1'-biphenyl]-2-carbonitrile
Biological ActivityTP 003 is a GABAA receptor partial agonist that demonstrates affinity for the benzodiazepine site. Potentiates GABAA α3 response with high efficacy. Produces anxiolytic-like effects in rodent elevated plus maze via action at GABAA α2 subtype receptors. Also evokes GABAA α1 mediated sedation and GABAA α3 mediated muscle relaxation in mice.
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Evidence for a significant role of α3-containing GABAA receptors in mediating the anxiolytic effects of benzodiazepines.
Dias et al.
Contribution of GABA(A) receptors containing α3 subunits to the therapeutic-related and side effects of benzodiazepine-type drugs in monkeys.
Fischer et al.
Psychopharmacology (Berl.), 2011;215:311
TP003 is a non-selective benzodiazepine site agonist that induces anxiolysis via α2GABAA receptors.
Neumann et al.
Citations for TP 003
The citations listed below are publications that use Tocris products. Selected citations for TP 003 include:
3 Citations: Showing 1 - 3
Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors.
Authors: Soderhielm Et al.
Biochem Pharmacol 2018;158:339
GABAA Receptor Subtypes Regulate Stress-Induced Colon Inflammation in Mice.
Authors: Seifi Et al.
Molecular and functional diversity of GABA-A receptors in the enteric nervous system of the mouse colon.
Authors: Seifi Et al.
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