Publications by authors named "Hirofumi Omura"
The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives.
Bioorg Med Chem Lett
June 2008
Article Synopsis
- Scientists found new compounds called benzimidazolone derivatives that work specifically on a receptor in the body called CB2.
- They studied these compounds to make them stronger and last longer in the body.
- One compound, called Compound 39, showed great results by lasting long when tested and helping with pain in rats that had a specific condition.
Previous studies have shown that cannabinoid 2 (CB(2))-receptor agonists might have analgesic effects on visceral hypersensitivity. To extend these results, we have determined the pharmacological characteristics of a newly designed CB(2) ligand, N-[(1S)-1-(aminocarbonyl)-2,2-dimethylpropyl]-3-(3-hydroxy-3-methylbutyl)-2-oxo-2,3-dihydro-1H-benzimidazole-1-carboxamide (PF-03550096), in vitro and in vivo. PF-03550096 showed high affinity to human (K(i) = 7.
View Article and Find Full Text PDFA novel potent NMDA-NR2B selective antagonist without the reactive metabolites formation issue was identified. Through this study, a close correlation between reactive metabolites formation and calculated HOMO energies of parent compounds was found.
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