anti-hyperalgesia

PNU-120596 (NSC-216666) is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.

AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg/kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg/kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg/kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.

(R)-Mirtazapine ((R)-Org3770) is the R(-)-enantiomer of Mirtazapine, exhibiting anti-injury sensory properties in an animal model of acute thermal hyperalgesia. It functions as a 5-HT3 receptor antagonist and serves as a potential analgesic.

1,7-Dihydroxy-2,3-methylenedioxyxanthone exhibits antiulcerogenic, anti-oxidation, and antihyperalgesic activities and can inhibit carrageenan-induced hyperalgesia.

J-2156 TFA is a selective SST4 receptor (somatostatin receptor type 4) agonist with IC50 values of 0.05 nM and 0.07 nM for human and rat SST4 receptors respectively. It exhibits anti-inflammatory and analgesic effects while reducing pERK levels.