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W-212393

Chemical Structure W-212393

CAS No.: 610323-32-5

W-212393 (W212393;MT-7716 free base)

Catalog No.: PC-61541Not For Human Use, Lab Use Only.

W-212393 (MT-7716 free base) is a highly potent, brain penetrant ORL1 receptor (NOP receptor) agonist with Ki of 0.76 and 0.50  nM for rat and human ORL1 receptors, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

W-212393 (MT-7716 free base) is a highly potent, brain penetrant ORL1 receptor (NOP receptor) agonist with Ki of 0.76 and 0.50  nM for rat and human ORL1 receptors, respectively; displays a relative selectivity over μ receptor and serotonin transporter; significantly suppresses the activity of spontaneously firing rat suprachiasmatic nucleus neurons at 100 nM; induces a significant phase advance at circadian time 6 (CT6) and CT9, but not at other CTs, represents an interesting agent for the study of circadian rhythms; MT-7716 dose-dependently decreases GABAergic transmission and effectively blocks the ethanol-induced increase in GABA release at these synapses.

Alcoholism

Phase 1 Discontinued

Physicochemical Properties

M.Wt 440.547
Formula C27H28N4O2
CAS No. 610323-32-5
Storage
Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 3 Month
Shipping
Solubility

Chemical Name

2-{3-[1-((1R)-acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide

Clinical Information

References

1. Teshima K, et al. Br J Pharmacol. 2005 Sep;146(1):33-40.

2. Miyakawa K, et al. Neuropharmacology. 2007 Mar;52(3):1055-64.

3. Kallupi M, et al. Front Integr Neurosci. 2014 Feb 18;8:18.

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