J-2156

J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC₅₀s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats^[1][2]. IC50 & Target: IC50: 0.05 nM (human SST4) and 0.07 nM (rat SST4)^[1] In Vitro: J-2156 binds with nanomolar affinity to the human somatostatin receptor subtype 4 (h sst4: K_i=1.2 nM) and is over 400-fold subtype-selective against the other somatostatin receptors (h sst1: K_i=1.2 nM; h sst2: K_i>5000 nM; h sst3: K_i=1400 nM; h sst5: K_i=540 nM) in Chinese hamster ovary (CHO) cells^[2]. In Vivo: J-2156 (1-10?mg/kg; i.p.; for 3 hours) of single bolus doses has anti-allodynic effect on ipsilateral and contralateral in BCIBP-rats^[1].