BMT-090605 is a potent, selective AAK1 inhibitor, with an IC50 of 0.6 nM. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 45 and 60 nM, respectively[1]. BMT-090605 shows antinociceptiveactivity
DPI-3290 is a specific agonist of opioid receptors (Ki: 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively) with potent antinociceptiveactivity. DPI-3290 is one of a series of novel centrally acting agents.
FR64822(N-(4-pyridylcarbamoyl)amino 1,2,3,6,-tetrahydropyridine), a novel non-opioid antinociceptive compound, displays antinociceptive activities in a variety of assays with mice and rats. It has a strong antinociceptiveactivity in the acetic acid writh
M-5011 is a non-steroidal anti-inflammatory drug and immunomodulator potentially for the treatment of inflammation and pain. M-5011 had an effective antinociceptiveactivity (ED50 value) of 0.63 mg kg. M-5011 partially inhibits the generalized bone loss a
20-HEPE is a metabolite of eicosapentaenoic acid that is formed via ω-oxidation of EPA by cytochrome P450 (CYP) ω-oxidases, including human CYP4F3B. It activates peroxisome proliferator-activated receptor α (PPARα) in COS-7 cells expressing a luciferase reporter when used at a concentration of 10 μM. 20-HEPE also activates murine transient receptor potential vanilloid receptor 1 (mTRPV1) in vitro but lacks antinociceptiveactivity in rats.
Hodgkinsine B is an alkaloid and isomer of hodgkinsine that has analgesic activity.1It increases the latency to tail withdrawal in the tail-flick test in mice when administered at a dose of 10 mg kg. 1.Kodanko, J.J., Hiebert, S., Peterson, E.A., et al.Synthesis of all low-energy stereoisomers of the tris(pyrrolidinoindoline) alkaloid hodgkinsine and preliminary assessment of their antinociceptiveactivityJ. Org. Chem.72(21)7909-7914(2007)