anti-hyperalgesia

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 and potent growth inhibitor receptor type 4 (SST4) agonist that acts on the human SST4 receptor (IC50: 0.05 nM) and rat SST4 receptor (IC50: 0.07 nM). J-2156 TFA exhibited anti-inflammatory activity and was able to alleviate mechanical abnormal pain and mechanical hyperalgesia in the rat ipsilateral hind paw.

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