Date published: 2026-4-25

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α5IA (CAS 215874-86-5)

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CAS Number:
215874-86-5
Purity:
97%
Molecular Weight:
362.35
Molecular Formula:
C17H14N8O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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α5IA is extensively used in neuroscientific research focused on its role as a GABA A receptor agonist, specifically targeting the α5 subunit-containing receptors. This compound is of interest due to its selectivity, which enables detailed studies of the α5 subunit′s role in modulating brain function. Researchers use α5IA to investigate the effects of enhanced GABAergic transmission in areas of the brain involved in memory and cognition. Additionally, α5IA is employed in studies exploring its potential to influence synaptic plasticity and neuronal network stability. Through these research initiatives, α5IA aids in advancing the understanding of GABA A receptor subtypes in regulating neural activity and their implications in cognitive processes.


α5IA (CAS 215874-86-5) References

  1. An inverse agonist selective for alpha5 subunit-containing GABAA receptors enhances cognition.  |  Dawson, GR., et al. 2006. J Pharmacol Exp Ther. 316: 1335-45. PMID: 16326923
  2. GABA(A) receptor subtype-selective efficacy: TPA023, an alpha2/alpha3 selective non-sedating anxiolytic and alpha5IA, an alpha5 selective cognition enhancer.  |  Atack, JR. 2008. CNS Neurosci Ther. 14: 25-35. PMID: 18482097
  3. The plasma-occupancy relationship of the novel GABAA receptor benzodiazepine site ligand, alpha5IA, is similar in rats and primates.  |  Atack, JR., et al. 2009. Br J Pharmacol. 157: 796-803. PMID: 19422390
  4. In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)-pyrazolo[1,5-d]-[1,2,4]triazine (MRK-016), a GABAA receptor alpha5 subtype-selective inverse agonist.  |  Atack, JR., et al. 2009. J Pharmacol Exp Ther. 331: 470-84. PMID: 19704033
  5. Preclinical and clinical pharmacology of the GABAA receptor alpha5 subtype-selective inverse agonist alpha5IA.  |  Atack, JR. 2010. Pharmacol Ther. 125: 11-26. PMID: 19770002
  6. Occupancy of human brain GABA(A) receptors by the novel α5 subtype-selective benzodiazepine site inverse agonist α5IA as measured using [¹¹C]flumazenil PET imaging.  |  Eng, W., et al. 2010. Neuropharmacology. 59: 635-9. PMID: 20696179
  7. Specific targeting of the GABA-A receptor α5 subtype by a selective inverse agonist restores cognitive deficits in Down syndrome mice.  |  Braudeau, J., et al. 2011. J Psychopharmacol. 25: 1030-42. PMID: 21693554
  8. Postnatal down-regulation of the GABAA receptor γ2 subunit in neocortical NG2 cells accompanies synaptic-to-extrasynaptic switch in the GABAergic transmission mode.  |  Balia, M., et al. 2015. Cereb Cortex. 25: 1114-23. PMID: 24217990
  9. Deficient tonic GABAergic conductance and synaptic balance in the fragile X syndrome amygdala.  |  Martin, BS., et al. 2014. J Neurophysiol. 112: 890-902. PMID: 24848467
  10. Physiological and pharmacological properties of inhibitory postsynaptic currents mediated by α5β1γ2, α5β2γ2 and α5β3γ2 GABAA receptors.  |  Chen, X., et al. 2017. Neuropharmacology. 125: 243-253. PMID: 28757051
  11. Long-lasting correction of in vivo LTP and cognitive deficits of mice modelling Down syndrome with an α5-selective GABAA inverse agonist.  |  Duchon, A., et al. 2020. Br J Pharmacol. 177: 1106-1118. PMID: 31652355
  12. Inhibition of a tonic inhibitory conductance in mouse hippocampal neurones by negative allosteric modulators of α5 subunit-containing γ-aminobutyric acid type A receptors: implications for treating cognitive deficits.  |  Manzo, MA., et al. 2021. Br J Anaesth. 126: 674-683. PMID: 33388140
  13. Prodromal dysfunction of α5GABA-A receptor modulated hippocampal ripples occurs prior to neurodegeneration in the TgF344-AD rat model of Alzheimer's disease.  |  Ratner, MH., et al. 2021. Heliyon. 7: e07895. PMID: 34568591

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

α5IA, 5 mg

sc-252345
5 mg
$185.00

α5IA, 25 mg

sc-252345A
25 mg
$714.00