sst4

Pasireotide (SOM230) acetate是长效的环己肽生长激素抑制素类似物，具有抗分泌、抗增殖和促凋亡活性。Pasireotide (SOM230) acetate可抑制 GH、IGF-I 和 ACTH 的分泌，可用于研究肢端肥大症和库欣病。Pasireotide (SOM230) acetate还可以提高生长抑素受体的激动剂活性，对sst1、2、3、4、5的pKi 分别为 8.2、9.0、9.1、小于7.0 和 9.9。

L-803087 是一种具有高效性和选择性的生长抑素 sst4 受体激动剂，对 sst4 的 Ki 值为 0.7 nM，比其他生长抑素受体的选择性高 280 倍以上。L-803087 在体外诱导 AMPA 介导的海马突触反应，在体内增加了海藻酸盐促使的小鼠癫痫发作。

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. J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC5

SSTR4agonist-1 (Compound 47) 是一种选择性激活生长抑素受体 4 (SSTR4) 的激动剂，EC50为 4.7 nM，并且在人体肝微粒体中的半衰期超过 130 分钟。

SSTR4 agonist5 (Compound 5) 是一种口服有效的生长抑素受体 4 (SSTR4) 激动剂，EC50为 0.228 nM。在人和大鼠肝微粒体中，SSTR4 agonist5 显示出良好的稳定性，并且能够在大鼠模型中抑制机械痛觉过敏。

Cortistatin-29 is a neuropeptide that is structurally similar to somatostatin-28. It is produced by cleavage of preprocortistatin to procortistatin, which is cleaved at dibasic amino acids to form cortistatin-29 and cortistatin-14 as well as other partial cleavage products. Cortistatin mRNA is expressed in the human brain and in interneurons of the rat hippocampus and cerebral cortex. Cortistatin-29 binds to somatostatin (SST) receptors with IC50 values of 2.8, 7.1, 0.2, 3, and 13.7 nM for SST1-5, respectively. Cortistatin-29 is found at similar levels as cortistatin-14 in mouse AtT20 cells but is secreted at a lower level. Cortistatin-29 corresponds to residues 85-112 of the rat peptide sequence.

PRL 2915 是一种有效的人类生长抑素亚型 2 受体拮抗剂 (hsst2)，其Ki 为 12 nM。

PRL 3195 是一种somatostatin receptor 拮抗剂，对人生长抑素受体 sst5、sst2、sst3、sst1和 sst4的Ki 分别为 6、17、66、1000 和 1000 nM。

Veldoreotide (DG3173) TFA，一种生长抑素类似物，能够结合并激活SSTR 2/4/5。其在腺瘤中抑制生长激素分泌的效果相较于Octreotide更为显著。此外，Veldoreotide亦展现出作为镇痛剂的潜力。

Veldoreotide, also known as Somatoprim, is a unique somatostatin receptor subtypes 2-, 4- and 5-selective analogue which effectively reduces GH secretion in human GH-secreting pituitary adenomas, even in Octreotide non-responsive tumours.

sst1/sst4 somatostatin receptors agonist

Pasireotide pamoate is a stable cyclohexapeptide somatostatin mimic. Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.

Pasireotide is a stable cyclohexapeptide somatostatin mimic.

Somatostatin sst4 receptor agonist

L-796,778 acetate 是一种选择性生长抑素受体激动剂，对 sst3的IC50为24nM，对sst1、sst2、sst4和sst5的IC50大于1000nM。

L-803087 TFA is a highly potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM. It displays a remarkable selectivity, being over 280-fold more preferential for the sst4 receptor compared to other somatostatin receptors. Furthermore, L-803087 TFA promotes AMPA-mediated synaptic responses in hippocampal preparations and enhances kainate-induced seizures in mice.

J-2156 TFA 是一种选择性的、高效的生长抑素受体 4 型 (SST4) 激动剂，能够作用于人 SST4 受体 (IC50: 0.05 nM) 和大鼠 SST4 受体 (IC50: 0.07 nM)。J-2156 TFA 表现出抗炎活性，能够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。

CYN 154806 TFA(183658-72-2 free base) 是一种环状八肽，是一种有效的选择性生长抑素 sst2 受体拮抗剂。对于重组 sst2、sst1、sst3、sst4 和 sst5 受体，pIC50 值分别为 8.58、5.41、6.07、5.76 和 6.48。

CYN 154806 is a potent and selective somatostatin sst2 receptor antagonist, The pIC50 values are 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.

Potent somatostatin receptor 1 (sst1) agonist; displays selectivity for sst1 (IC50 values are 30.9 nM, 345 nM, > 1 μM, > 10 μM and > 10μM for human sst1, sst3, sst4, sst2 and sst5 respectively). Attenuates somatostatin release in the rat nucleus accumbens

Peptide agonist for sst2 and sst5 somatostatin receptors. IC50/Kd values (nM) at cloned human somatostatin receptors are: > 1000 (sst1), 0.2 - 1.5 (sst2), 27 - 36 (sst3), > 127 (sst4), and 0.06 - 23 (sst5).