RPI-GLYT2-82 is a reversible, blood-brain barrier-permeable allosteric inhibitor of GlyT2 with an IC50 value of 554 nM. RPI-GLYT2-82 also exhibits inhibitory activity against 5-HT2AR and SERT, with IC50 values of 1.9 μM and 4.7 μM, respectively. RPI-GLYT2-82 inhibits pain signals and alleviates allodynia, shows no target-related side effects at the maximum analgesic dose, and has no addictive potential. RPI-GLYT2-82 can be used for the research of neuropathic pain [1].
In Vivo, RPI-GLYT2-82 (50-150 mg/kg, i.p., single administration) produces dose-dependent analgesic effects in mouse chronic constriction injury (CCI) and partial sciatic nerve ligation (PSNL) neuropathic pain models[1].
References:
[1]. Cantwell Chater RP, et al. A reversible allosteric inhibitor of GlyT2 alleviates neuropathic pain without on-target side effects. bioRxiv [Preprint]. 2025 Nov 20:2025.04.21.649698.
In Vivo, RPI-GLYT2-82 (50-150 mg/kg, i.p., single administration) produces dose-dependent analgesic effects in mouse chronic constriction injury (CCI) and partial sciatic nerve ligation (PSNL) neuropathic pain models[1].
References:
[1]. Cantwell Chater RP, et al. A reversible allosteric inhibitor of GlyT2 alleviates neuropathic pain without on-target side effects. bioRxiv [Preprint]. 2025 Nov 20:2025.04.21.649698.