TMPH is an inhibitor of nAChR and inhibits nAChRs lacking α5, α6, or β3 subunits. TMPH can be used in studies about nAChR dysfunction or neurological disorders.
TMPH (100 nM) inhibits nAChR with an inhibition rate of 90% in Xenopus oocytes and suppresses AChR subtypes with IC50s of 1.0-390 nM[1].
In the nicotine-induced mice model, nAChR-IN-1 (20 mg/kg; s.c.) increases locomotor activity without effects on body temperature. In the tail-flick and hot-plate mice model, nAChR-IN-1(0, 0.1, 1, 5 mg/kg; s.c.) blocks the antinociceptive effect of nicotine in the hot-plate and blocks antinociception in a time-dependent manner[1].