NS11394 is a drug which acts as a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes. NS-11394 has been researched as an analgesic for use in chronic or neuropathic pain. NS-11394 possesses a functional selectivity profile at GABA(A) receptors of alpha(5) > alpha(3) > alpha(2) > alpha(1) based on oocyte electrophysiology with human GABA(A) receptors. Compared with other subtype-selective ligands, NS11394 is unique in having superior efficacy at GABA(A)-alpha(3) receptors while maintaining low efficacy at GABA(A)-alpha(1) receptors. NS11394 has an excellent pharmacokinetic profile, which correlates with pharmacodynamic endpoints (CNS receptor occupancy). NS11394 is potent and highly effective in rodent anxiety models. NS11394 has a significantly reduced side effect profile in rat (sedation, ataxia, and ethanol interaction) and mouse (sedation), even at full CNS receptor occupancy. NS11394 has a unique subtype-selective GABA(A) receptor profile and represents an excellent pharmacological tool to further understanding on the relative contributions of GABA(A) receptor subtypes in various therapeutic areas.
CAS Number: 951650-22-9
Molecular Weight: 353.42
Chemical Name: 3'-(5-(2-hydroxypropan-2-yl)-1H-benzo[d]imidazol-1-yl)-[1,1'-biphenyl]-2-carbonitrile
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
NS11394 (1-120 mg/kg) selectively attenuates injury-induced nociceptive behaviors in the formalin test. NS11394 (1–10 mg/kg) markedly attenuates the deficit in hindpaw weight bearing [F(4, 61) = 7.569, p < 0.001] in CFA rats.
- Hofmann M, Kordás KS, Gravius A, Bölcskei K, Parsons CG, Dekundy A, Danysz W, Dézsi L, Wittko-Schneider IM, Sághy K, Gyertyán I, Horváth C. Assessment of the effects of NS11394 and L-838417, α2/3 subunit-selective GABA(A) [corrected] receptor-positive allosteric modulators, in tests for pain, anxiety, memory and motor function. Behav Pharmacol. 2012 Dec;23(8):790-801. doi: 10.1097/FBP.0b013e32835a7c7e. Erratum in: Behav Pharmacol. 2013 Apr;24(2):153. PubMed PMID: 23075708.
- Hansen RR, Erichsen HK, Brown DT, Mirza NR, Munro G. Positive allosteric modulation of GABA-A receptors reduces capsaicin-induced primary and secondary hypersensitivity in rats. Neuropharmacology. 2012 Dec;63(8):1360-7. doi: 10.1016/j.neuropharm.2012.08.002. Epub 2012 Aug 17. PubMed PMID: 22985969.
- Mirza NR, Larsen JS, Mathiasen C, Jacobsen TA, Munro G, Erichsen HK, Nielsen AN, Troelsen KB, Nielsen EØ, Ahring PK. NS11394 [3'-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile], a unique subtype-selective GABAA receptor positive allosteric modulator: in vitro actions, pharmacokinetic properties and in vivo anxiolytic efficacy. J Pharmacol Exp Ther. 2008 Dec;327(3):954-68. doi: 10.1124/jpet.108.138859. Epub 2008 Sep 12. PubMed PMID: 18791063.
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