PTIQ

• CAT Number: R036112
• CAS Number: 1032822-42-6
• Molecular Formula: C13H17NO3
• Molecular Weight: 235.28
• Purity: ≥95%
• IUPAC Name: 1-(7-hydroxy-6-methoxy-3,4-dihydro-1H-isoquinolin-2-yl)propan-1-one
• InChI: InChI=1S/C13H17NO3/c1-3-13(16)14-5-4-9-7-12(17-2)11(15)6-10(9)8-14/h6-7,15H,3-5,8H2,1-2H3
• SMILES: CCC(=O)N1CCC2=CC(=C(C=C2C1)O)OC

Brain penetrating neuroprotectant that attenuates MPTP induced motor deficits, prevents neurodegeneration and suppresses microglial activation in the substantia nigra. Mechanistically, PTIQ effectively suppresses expression of MMP-3 (IC50 value 60 nM in stressed dopaminergic cells), and NO production (IC50 value <100 µM in LPS stimulated BV-2 cells). PTIQ also inhibits IL-1β, TNF-α (IC50 value 6.5 µM) and COX-2 (IC50 value 9.3 µM) and blocked nuclear translocation of NF-κB, yet it shows no inhibition of hERG channels or CYP isozyme activities.

Reference

H.J. Son et al. A novel compound PTIQ protects the nigral dopaminergic neurones in an animal model of Parkinson’s disease induced by MPTP. Br J Pharmacol. 2012 Apr;165(7):2213-27.

 

J.W. Seo et al. Syntheses of tetrahydroisoquinoline derivatives that inhibit NO production in activated BV-2 microglial cells. Eur J Med Chem. 2008 Jun;43(6):1160-70.