DS2
Chemical Name: 4-Chloro-N-[2-(2-thienyl)imidazo[1,2-a]pyridin-3-yl]benzamide
Purity: ≥97%
Biological Activity
DS2 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.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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Probing alpha4betadelta GABAA receptor heterogeneity: differential regional effects of a functionally selective alpha4beta1delta/alpha4beta3delta receptor agonist on tonic and phasic inhibition in rat brain.
Hoestgaard-Jensen K, Dalby N, Krall J, Hammer H, Krogsgaard-Larsen P, Frolund B, Jensen A
J Neurosci, 2014;34(49):16256-72. -
Novel compounds selectively enhance δ subunit containing GABAA receptors and increase tonic currents in thalamus.
Wafford et al.
Neuropharmacology, 2009;56:182 -
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.
Br.J.Pharmacol., 2013;168:1118 -
A pharmacological assessment of agonists and modulators at α4β2γ2 and α4β2δ GABAA receptors: The challenge in comparing apples with oranges.
Ahring et al.
Pharmacol.Res., 2016;111:563
Product Datasheets
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Citations for DS2
The citations listed below are publications that use Tocris products. Selected citations for DS2 include:
8 Citations: Showing 1 - 8
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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
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Context-Dependent Modulation of GABAAR-Mediated Tonic Currents.
Authors: Patel Et al.
J Neurosci 2016;36:607
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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
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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
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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
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Synaptic GABAA receptor clustering without the γ2 subunit.
Authors: Kerti-Szigeti Et al.
Nat Methods 2014;34:10219
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Phosphatidylinositol 4,5-bisphosphate depletion fails to affect neurosteroid modulation of GABAA receptor function.
Authors: Mennerick Et al.
Psychopharmacology (Berl) 2014;231:3493
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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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