NS11394


Catalog No. size PriceQuantity
M6628-2 2mg solid $111
M6628-10 10mg solid $447

Description

Cas:951650-22-9

Product Information:

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.

 

Chemical Formula: C23H19N3O

 

Exact Mass: 353.15281

 

Molecular Weight: 353.42

 

Elemental Analysis: C, 78.16; H, 5.42; N, 11.89; O, 4.53

 

Synonym:

 

NS-11394

NS 11394

NS11394

 

Chemical Name: 3'-(5-(2-hydroxypropan-2-yl)-1H-benzo[d]imidazol-1-yl)-[1,1'-biphenyl]-2-carbonitrile

 

InChi Key:

HLKYSQGBIIIQJN-UHFFFAOYSA-N

 

InChi Code: InChI=1S/C23H19N3O/c1-23(2,27)18-10-11-22-21(13-18)25-15-26(22)19-8-5-7-16(12-19)20-9-4-3-6-17(20)14-24/h3-13,15,27H,1-2H3

 

Smiles Code:

N#CC1=CC=CC=C1C2=CC=CC(N3C4=CC=C(C(C)(O)C)C=C4N=C3)=C2

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vivo

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.

 

 

References

 

  1. 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.

 

  1. 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.

 

  1. 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.

 

  1. Munro G, Lopez-Garcia JA, Rivera-Arconada I, Erichsen HK, Nielsen EØ, Larsen JS, Ahring PK, Mirza NR. Comparison of the novel subtype-selective GABAA receptor-positive allosteric modulator NS11394 [3'-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile] with diazepam, zolpidem, bretazenil, and gaboxadol in rat models of inflammatory and neuropathic pain. J Pharmacol Exp Ther. 2008 Dec;327(3):969-81. doi: 10.1124/jpet.108.144568. Epub 2008 Sep 12. PubMed PMID: 18791060.

 

Products are for research use only. Not for human use.

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