spinal nerve ligation

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).

5-HT6 inverse agonist 1 (Compound 33) is an antagonist of the 5-HT6 receptor with a Ki of 23 nM and a Kb of 6.62 nM. This compound can inhibit 5-HT6R-mediated Cdk5 and mTOR signaling pathways and reduce tactile allodynia induced by spinal nerve ligation (SNL) in rat models.

δ14-Triamcinolone acetonide is a potential impurity found in commercial preparations of triamcinolone acetonide. Triamcinolone acetonide is a synthetic corticosteroid. It decreases cytokine levels, the firing rate of sensory neurons, and mechanical hypersensitivity in a rat spinal nerve ligation model when used at a dose of 1.5 mg/kg prior to and following surgery for three days. Triamcinolone acetonide also decreases outflow facility in a mouse model of steroid-induced glaucoma when 20 μl of a 40 mg/ml suspension is administered subconjunctivally. Formulations containing triamcinolone acetonide are used in the treatment of diabetic macular edema.

JHU-58 is a novel dipeptide MrgC agonist. JHU-58 inhibited both mechanical and heat hypersensitivity in rats after an L5 spinal nerve ligation (SNL). JHU58 attenuated the evoked excitatory postsynaptic currents in substantia gelatinosa (SG) neurons in wild-type mice, but not in Mrg knockout mice, after peripheral nerve injury.

Dermorphin is agonist of μ-opioid receptor (MOR) agonist.

Dermorphin TFA is a new class of opioids-like peptides

AC-099 (compound 3) serves as a selective full agonist at NPFF2R (EC50 = 1189 nM) and a partial agonist at NPFF1R (EC50 = 2370 nM). It has been shown to mitigate hypersensitivity induced by spinal nerve ligation in rats [1] [2].