Publications by authors named "Naoya Makita"
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.
From hit compounds identified by high throughput screening (HTS), we have found compound 1 as a lead TRPV1 antagonist and confirmed its potential as a treatment for pain. Compound 1 has led to potent TRPV1 antagonistic benzamide derivatives ((+/-)-2: human IC(50)=23 nM, (+/-)-3: human IC(50)=14 nM in the capsaicin-induced calcium influx assay) containing indole and naphthyl moieties, obtained by elaboration of the tryptamine scaffold or via bioisosteric replacements.
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