UKH-1114 is a selective TMEM97 (a sigma-2 receptor) agonist with a K i values of 1279 and 46 nM for σ1R and σ2R/ TMEM97, respectively. UKH-1114 exhibits exceptional selectivity with negligible affinity for over 50 other receptors and channels. UKH-1114 effectively relieves spared nerve injury (SNI)-induced mechanical hypersensitivity with a long-lasting duration and without motor impairment. UKH-1114 can be used for neuropathic pain research [1].
In Vivo, UKH-1114 (10 µg, i.t. once, lasting for 1-72 h) elicits pronounced and sustained antinociceptive effects, by acting as an agonist at σ2R/Tmem97 in the SNI mice model[1]. UKH-1114 (10 mg/kg, i.v., once, lasting for 0-164 h) alleviates neuropathic pain without motor impairment in the SNI mice model[1].
References:
[1]. Sahn JJ, et al. Sigma 2 Receptor/Tmem97 Agonists Produce Long Lasting Antineuropathic Pain Effects in Mice. ACS Chem Neurosci. 2017 Aug 16;8(8):1801-1811.
In Vivo, UKH-1114 (10 µg, i.t. once, lasting for 1-72 h) elicits pronounced and sustained antinociceptive effects, by acting as an agonist at σ2R/Tmem97 in the SNI mice model[1]. UKH-1114 (10 mg/kg, i.v., once, lasting for 0-164 h) alleviates neuropathic pain without motor impairment in the SNI mice model[1].
References:
[1]. Sahn JJ, et al. Sigma 2 Receptor/Tmem97 Agonists Produce Long Lasting Antineuropathic Pain Effects in Mice. ACS Chem Neurosci. 2017 Aug 16;8(8):1801-1811.