J-2156 是一种高效，选择性的生长抑素受体 4 型 (SST4 受体) 激动剂，对于人和大鼠 SST4 受体的 IC50 分别为 0.05 nM 和 0.07 nM[1]。 J-2156 用于缓解大鼠同侧后爪的机械性异常性疼痛和机械性痛觉过敏的 ED50 分别为 3.7 mg/kg 和 8.0 mg/kg。
CAS：848647-56-3
分子式：C24H28N4O4S
分子量：468.57
纯度：98%
存储：Store at -20°C

Background:

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. The ED50 of J-2156 in rats for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws was 3.7 and 8.0 mg/kg, respectively[1]. IC50: 0.05 nM (human SST4) and 0.07 nM (rat SST4)[1]

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]. Animal Model: BCIBP-rats[1]

[1]. Shenoy PA, et al. The Somatostatin Receptor-4 Agonist J-2156 Alleviates Mechanical Hypersensitivity in a Rat Model of Breast Cancer Induced Bone Pain. Front Pharmacol. 2018 May 15;9:495.