sstr4

(1R,5S,6r)-N-(2-methyl-1-((3-methylpyridin-2-yl)oxy)propan-2-yl)-3-azabicyclo[3.1.0]hexane-6-carboxamide L(+)-Tartaric acid 是一种潜在的SSTR4激动剂。

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。

SSTR4 agonist 2 是有效的生长抑素受体亚型 4 (SSTR4) 激动剂，在 SSTR4 相关的医学疾病研究中具有潜力。SSTR4 通路抑制痛觉和炎症。

SSTR4 agonist 4 是一种有效的SSTR4激动剂，具有用于疼痛研究的潜力。SSTR4 激动剂在与急性和慢性相关的抗外周伤害感受和抗炎活性相关疼痛的啮齿动物模型中有效。SSTR4 在海马和新皮质、记忆和学习区域以及阿尔茨海默病病理学中的表达水平相对较高。

SSTR4 agonist 3 is a potent compound that activates the SSTR4 receptor. The SSTR4 receptor is highly expressed in the hippocampus and neocortex, which are regions associated with memory, learning, and Alzheimer's disease pathology. SSTR4 agonists demonstrate strong efficacy in rodent models of pain, both acute and chronic, by reducing peripheral nociception and inflammation. Considering its potential application in pain research, SSTR4 agonist 3 is of interest[1].

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.

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.

Cortistatin 29，一种具备高亲和力结合至所有生长抑素(SS)受体亚型的神经肽，其对SSTR1、SSTR2、SSTR3、SSTR4、SSTR5的IC50值分别为2.8, 7.1, 0.2, 3.0, 13.7 nM。该化合物不仅能减轻神经性疼痛，还表现出抗纤维化作用。

(D-Phe5,Cys6,11,N-Me-D-Trp8)-Somatostatin-14 (5-12) amide (Compound 4) 是一种生长抑素类似物，对 SSTR5、SSTR3、SSTR2、SSTR1和 SSTR4的Kd 分别为 0.61、11.05、23.5、1200 和 >1000 nM。