TP 003
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
Purity: ≥98%
Biological Activity
TP 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Molecular and functional diversity of GABA-A receptors in the enteric nervous system of the mouse colon.
Seifi M, Brown J, Mills J, Bhandari P, Belelli D, Lambert J, Rudolph U, Swinny J
, 2014;0(0):. -
Evidence for a significant role of α3-containing GABAA receptors in mediating the anxiolytic effects of benzodiazepines.
Dias et al.
J.Neurosci., 2005;25:10682 -
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.
Neuropharmacology, 2018;143:71
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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
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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
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GABAA Receptor Subtypes Regulate Stress-Induced Colon Inflammation in Mice.
Authors: Seifi Et al.
Gastroenterology 2018;155:852
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Molecular and functional diversity of GABA-A receptors in the enteric nervous system of the mouse colon.
Authors: Seifi Et al.
Gastroenterology 2014;34:10361
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