A-836339

A-836339 is a selective CB2 receptor agonist, with Ki values of 0.4 nM and 0.8 nM in humans and rats, respectively. A-836339 exhibits multiple effects such as analgesia, gastric protection, anti-inflammation, and antioxidant activity. A-836339 produces antinociceptive and analgesic activities by activating CB2 receptors in the dorsal root ganglia and spinal cord. A-836339 can also exert gastric protective effects through anti-inflammatory mechanisms (reducing TNF-α and IL-1β) and antioxidant mechanisms (enhancing the activities of CAT and SOD, and reducing H₂O₂). Radioactively labeled A-836339 can serve as a CB2-specific radioligand for autoradiography and PET imaging. A-836339 can be used in research on inflammatory pain, neuropathic pain, gastric ulcers, cerebral ischemia, etc^{[1][2][3][4][5]}. In Vitro:A-836339 (20 µM; 20 min; brain sections) decreases [11C]A-836339 binding in the ipsilateral hemisphere after LPS and AMPA injection^[4]. In Vivo:A-836339 (5 mg/kg; oral) demonstrates co-localization of CB2 receptors and COX-2 in gastric tissue of EtOH-induced ulcer model in mice^[3].
A-836339 (0.3 µmol/kg; i.t.) reverses neuropathic pain by acting at spinal cord sites^[1].
A-836339 (0.3 µmol/kg; intra-DRG) reverses inflammatory pain by acting at dorsal root ganglion sites^[1].
A-836339 (0.3 µmol/kg; intra-DRG) reverses neuropathic pain by acting at dorsal root ganglion sites^[1].
A-836339 (1-10 µmol/kg; IP) reverses inflammatory pain by acting through CB2 receptors^[1].
A-836339 (3-30 µmol/kg; IP) reverses neuropathic pain in the CCI model via CB2 receptor activation and without opioid dependency^[1].
A-836339 (1-5 mg/kg; oral) reduces ulcer index and ULI in EtOH-induced gastric ulcer model in mice by enhancing gastroprotection and reversing histological damage, reduces TNF-α levels, and enhances antioxidant defense mechanisms by increasing CAT and SOD activities and reducing H2O2 levels^[3].
A-836339 (1-5 mg/kg; oral) reduces ulcer index and ULI in NSAID-induced gastric ulcer model in mice, enhances CAT activity, and reduces H2O2 levels, while also reducing TNF-α levels^[3].