DS-1 (drug)

Summary

DS-1 is a drug from the imidazopyridine family, which is the first drug developed that acts as a GABAA receptor positive allosteric modulator (PAM) selective for the α4β3δ subtype, which is not targeted by other GABAA receptor PAMs such as the benzodiazepines or other nonbenzodiazepine drugs. Novel selective drugs such as DS-1 are useful in the study of this receptor subtype.[1][2][3]

DS-1
Identifiers
  • 4-chloro-N-(6,8-dibromo-2-thiophen-2-ylimidazo[1,2-a]pyridin-3-yl)benzamide
CAS Number
  • 372497-52-4 checkY
PubChem CID
  • 979735
IUPHAR/BPS
  • 4183
ChemSpider
  • 849261 checkY
CompTox Dashboard (EPA)
  • DTXSID60359667 Edit this at Wikidata
ECHA InfoCard100.209.966 Edit this at Wikidata
Chemical and physical data
FormulaC18H10Br2ClN3OS
Molar mass511.62 g·mol−1
3D model (JSmol)
  • Interactive image
  • s4cccc4-c2nc1c(Br)cc(Br)cn1c2NC(=O)c(cc3)ccc3Cl
  (verify)

See also edit

References edit

  1. ^ Wafford KA, van Niel MB, Ma QP, Horridge E, Herd MB, Peden DR, et al. (January 2009). "Novel compounds selectively enhance delta subunit containing GABA A receptors and increase tonic currents in thalamus". Neuropharmacology. 56 (1): 182–189. doi:10.1016/j.neuropharm.2008.08.004. PMID 18762200. S2CID 207224202.
  2. ^ Yakoub K, Jung S, Sattler C, Damerow H, Weber J, Kretzschmann A, et al. (March 2018). "Structure-Function Evaluation of Imidazopyridine Derivatives Selective for δ-Subunit-Containing γ-Aminobutyric Acid Type A (GABAA) Receptors". Journal of Medicinal Chemistry. 61 (5): 1951–1968. doi:10.1021/acs.jmedchem.7b01484. PMID 29451785.
  3. ^ Solomon VR, Tallapragada VJ, Chebib M, Johnston GA, Hanrahan JR (June 2019). "GABA allosteric modulators: An overview of recent developments in non-benzodiazepine modulators". European Journal of Medicinal Chemistry. 171: 434–461. doi:10.1016/j.ejmech.2019.03.043. PMID 30928713. S2CID 89619321.