Chemical Name: 4-Chloro-N-[2-(2-thienyl)imidazo[1,2-a]pyridin-3-yl]benzamide
Biological ActivityDS2 is a positive allosteric modulator of GABAA receptors. Potentiates GABA-evoked currents mediated by α4β3δ receptors (EC50 = 142 nM, in vitro). Displays complex selectivity profile, with selectivity for δ-containing receptors (α4/6βxδ > α1βxδ >> γ2 > α4β3 GABAA receptors). Enhances tonic currents of thalamocortical neurons in wild-type mice.
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Novel compounds selectively enhance δ subunit containing GABAA receptors and increase tonic currents in thalamus.
Wafford et al.
A study of subunit selectivity, mechanism and site of action of the delta selective compound 2 (DS2) at human recombinant and rodent native GABAA receptors.
Jensen et al.
A pharmacological assessment of agonists and modulators at α4β2γ2 and α4β2δ GABAA receptors: The challenge in comparing apples with oranges.
Ahring et al.
Citations for DS2
The citations listed below are publications that use Tocris products. Selected citations for DS2 include:
8 Citations: Showing 1 - 8
Delineation of the functional properties and the mechanism of action of AA29504, an allosteric agonist and positive allosteric modulator of GABAA receptors.
Authors: Olander Et al.
Biochem Pharmacol 2018;150:305
Context-Dependent Modulation of GABAAR-Mediated Tonic Currents.
Authors: Patel Et al.
J Neurosci 2016;36:607
Ectopic Expression of α6 and δ GABAA Receptor Subunits in Hilar Somatostatin Neurons Increases Tonic Inhibition and Alters Network Activity in the Dentate Gyrus.
Authors: Tong Et al.
J Neurosci 2015;35:16142
Functional characterization of the 1,5-benzodiazepine clo. and its major active metabolite N-desmethylclobazam at human GABA(A) receptors expressed in Xenopus laevis oocytes.
Authors: Hammer Et al.
PLoS One 2015;10:e0120239
Unexpected Properties of δ-Containing GABAA Receptors in Response to Ligands Interacting with the α+ β- Site.
Authors: Mirheydari Et al.
Neurochem Res 2014;39:1057
Synaptic GABAA receptor clustering without the γ2 subunit.
Authors: Kerti-Szigeti Et al.
Nat Methods 2014;34:10219
Phosphatidylinositol 4,5-bisphosphate depletion fails to affect neurosteroid modulation of GABAA receptor function.
Authors: Mennerick Et al.
Psychopharmacology (Berl) 2014;231:3493
Characteristics of concatemeric GABA(A) receptors containing α4/δ subunits expressed in Xenopus oocytes.
Authors: Shu Et al.
Br J Pharmacol 2012;165:2228
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