Potent agonist of the nociceptin (ORL1) receptor, demonstrated both in vitro and in vivo. Selective, competitive antagonism at the nociceptin receptor has also been reported (pA2 = 7.02 and 6.75 in the guinea pig ileum and mouse vas deferens respectively)
Ac-hMCH(6-16)-NH2 shows non-selective agonist activity towards both MCH-1R and MCH-2R, which are human MCH receptors in the brain. The compound effectively binds to and activates these receptors, with IC 50 values of 0.16 nM and 2.7 nM for MCH-1R and MCH-2R, respectively.
Apamin TFA (Apamine TFA) is a toxin found in bee venom. It is a potent blocker of small conductance Ca2+-activated K+ (SK, KCa2) channels that is more effective at SK2 than SK1 and SK3.