ML 154

• CAT Number: I008257
• CAS Number: 1345964-89-7
• Molecular Formula: C29H26N2PS.Br
• Molecular Weight: 545.47
• Purity: ≥95%
• IUPAC Name: [2-methyl-1-[(E)-3-phenylprop-2-enyl]imidazo[1,2-a]pyridin-4-ium-3-yl]-diphenyl-sulfanylidene-λ5-phosphane;bromide
• InChI: InChI=1S/C29H26N2PS.BrH/c1-24-29(32(33,26-17-7-3-8-18-26)27-19-9-4-10-20-27)31-22-12-11-21-28(31)30(24)23-13-16-25-14-5-2-6-15-25;/h2-22H,23H2,1H3;1H/q+1;/p-1/b16-13+
• SMILES: CC1=C([N+]2=CC=CC=C2N1C/C=C/C3=CC=CC=C3)P(=S)(C4=CC=CC=C4)C5=CC=CC=C5.[Br-]

Competitive, selective, and brain penetrant NPS receptor antagonist that preferentially blocks NPS-induced ERK phosphorylation over intracellular Ca2+ or cAMP responses (IC50 values 22.1 nM, 36.5 nM, and 5.0 nM, in Ca2+, cAMP, and binding assays, respectively). NCGC84 decreases alcohol self-administration in vivo, and does not inhibit the vasopressin V1b or the endogenous purinergic receptor at concentrations up to 10 µM.

Reference

A. Thorsell et al. A novel brain penetrant NPS receptor antagonist, NCGC00185684, blocks alcohol-induced ERK-phosphorylation in the central amygdala and decreases operant…. J Neurosci. 2013 Jun 12;33(24):10132-42. doi: 10.1523/JNEUROSCI.4742-12.2013.