TP 003

Catalog #: 4414
3 Citations Datasheet / COA / SDS

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TP 003 | CAS No. 628690-75-5 | GABA-A Receptor Agonists

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Description: GABAA partial agonist; acts at benzodiazepine site

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%

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Product Details

Citations (3)

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Biological Activity

TP 003 is a GABA_A receptor partial agonist that demonstrates affinity for the benzodiazepine site. Potentiates GABA_A α3 response with high efficacy. Produces anxiolytic-like effects in rodent elevated plus maze via action at GABA_A α2 subtype receptors. Also evokes GABA_A α1 mediated sedation and GABA_A α3 mediated muscle relaxation in mice.

Technical Data

M.Wt:

407.39

Formula:

C₂₃H₁₆F₃N₃O

Solubility:

Soluble to 100 mM in DMSO and to 50 mM in ethanol

Purity:

≥98%

Storage:

Store at +4°C

CAS No:

628690-75-5

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

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 α2GABA_A 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

Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABA_A receptors.
Authors: Soderhielm Et al.
Biochem Pharmacol 2018;158:339
GABAA Receptor Subtypes Regulate Stress-Induced Colon Inflammation in Mice.
Authors: Seifi Et al.
Gastroenterology 2018;155:852
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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