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Description: Positive allosteric modulator of GABAA receptors; displays subunit selectivity
Chemical Name: 4-Chloro-N-[2-(2-thienyl)imidazo[1,2-a]pyridin-3-yl]benzamide
Purity: ≥97% (HPLC)
Citations (8)
Literature (2)

Biological Activity for DS2

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.

Compound Libraries for DS2

DS2 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for DS2

M. Wt 353.83
Formula C18H12ClN3OS
Storage Desiccate at +4°C
Purity ≥97% (HPLC)
CAS Number 374084-31-8
PubChem ID 979718
Smiles O=C(C4=CC=C(Cl)C=C4)NC2=C(C3=CC=CS3)N=C1C=CC=CN12

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.

Solubility Data for DS2

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 17.69 50

Preparing Stock Solutions for DS2

The following data is based on the product molecular weight 353.83. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 5.65 mL 28.26 mL 56.52 mL
2.5 mM 1.13 mL 5.65 mL 11.3 mL
5 mM 0.57 mL 2.83 mL 5.65 mL
25 mM 0.11 mL 0.57 mL 1.13 mL

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Product Datasheets for DS2

Certificate of Analysis / Product Datasheet
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References for DS2

References are publications that support the biological activity of the product.

Wafford et al (2009) Novel compounds selectively enhance δ subunit containing GABAA receptors and increase tonic currents in thalamus. Neuropharmacology 56 182 PMID: 18762200

Jensen et al (2013) 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. Br.J.Pharmacol. 168 1118 PMID: 23061935

Ahring et al (2016) A pharmacological assessment of agonists and modulators at α4β2γ2 and α4β2δ GABAA receptors: The challenge in comparing apples with oranges. Pharmacol.Res. 111 563 PMID: 27178730

If you know of a relevant reference for DS2, please let us know.

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Keywords: DS2, DS2 supplier, Positive, allosteric, modulators, delta, GABAA, receptors, PAM, Receptors, 3679, Tocris Bioscience

8 Citations for DS2

Citations are publications that use Tocris products. Selected citations for DS2 include:

Olander et al (2018) Delineation of the functional properties and the mechanism of action of AA29504, an allosteric agonist and positive allosteric modulator of GABAA receptors. Biochem Pharmacol 150 305 PMID: 29454619

Mennerick et al (2014) Phosphatidylinositol 4,5-bisphosphate depletion fails to affect neurosteroid modulation of GABAA receptor function. Psychopharmacology (Berl) 231 3493 PMID: 24553581

Patel et al (2016) Context-Dependent Modulation of GABAAR-Mediated Tonic Currents. J Neurosci 36 607 PMID: 26758848

Kerti-Szigeti et al (2014) Synaptic GABAA receptor clustering without the γ2 subunit. Nat Methods 34 10219 PMID: 25080584

Do you know of a great paper that uses DS2 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

GABA Receptors Scientific Review

GABA Receptors Scientific Review

Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.

Addiction Poster

Addiction Poster

The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.