chronic constriction injury

GW406381 is a highly selective inhibitor of cyclooxygenase-2 (COX-2). GW406381 also attenuates spontaneous ectopic discharge in the sural nerves of rats following chronic constriction injury.

LP-935509 is a selective, brain-permeable, small molecule competitive inhibitor of articulin-2-associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM. LP-935509 is a potent inhibitor of BIKE (IC50 of 14 nM) and a moderate inhibitor of GAK (IC50 of 320±40 nM).

Kv7.2 Kv7.3 agonist 1 (Compound 16) is an orally effective agonist for the KV7.2 7.3 channels (KV7.2 7.3 channel KCNQ2 3) with an EC50 of 1.03 μM. This compound demonstrates analgesic effects in mouse models of chronic constriction injury (CCI) and Streptozotocin-induced diabetic peripheral neuropathy (DPNP), with ED50 values of 12.02 mg kg and 9.63 mg kg, respectively.

ASP8477 is a potent and selective FAAH inhibitor. It increases anandamide levels in the brain when administered orally. In rat models of neuropathic and osteoarthritic pain, ASP8477 demonstrates significant efficacy without causing motor coordination issues. A single oral dose of ASP8477 improves thermal hyperalgesia and cold allodynia in rats with chronic constriction nerve injury. Moreover, ASP8477 restores the decreased muscle pressure threshold in a myalgia model induced by reserpine. Research indicates that ASP8477 possesses analgesic effects effective for alleviating neuropathic and functional pain, making its pharmacological properties suitable for chronic pain treatment.

GeX-2 is a truncated analogue of αO-conotoxin. It has the ability to activate GABAB receptors and inhibit α9α10nAChR as well as CaV2.2 channels. Additionally, GeX-2 is effective in alleviating pain in a rat model of chronic constriction injury.