somatostatin receptor agonist

Octreotide (SMS 201-995) 是一种有效的生长激素、胰高血糖素和胰岛素抑制剂。它主要与生长抑素 2、3 和 5 亚型受体结合，可增强 Gi 活性，降低胞内 cAMP 的产生。

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

Branosotine (compound 1-1) 作为一种高效的生长抑素受体 (somatostatin receptor (SSTR2)) 激动剂，其EC50 值低于 0.1 nM。

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。

somatostatin sst2 receptor agonist

somatostatin sst5 receptor agonist

Somatostatin sst4 receptor agonist

TC-G1003 is an effective agonist of the somatostatin sst2 receptor.

L-779,976 is an agonist of somatostatin receptor.

L-797,591 is a selective agonist of somatostatin receptor subtype 1.

Seglitide acetate (MK-678) 是一种选择性的 sst2生长抑素受体激动剂。

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。

Neuromedin C is a bombesin-like neuropeptide that stimulates uterine smooth muscle contraction and the release of gastrin , somatostatin, and amylase in rats. Neuromedin C is a truncated form of gastrin-releasing peptide corresponding to the GRP amino acids 18-27. It inhibits GRP and bombesin binding to rat pancreatic membranes (IC50s = 0.4 and 2.2 nM, respectively), which can be reduced by sodium chloride and guanylyl imidodiphosphate . Neuromedin C induces scratching and mast cell degranulation in mice when administered intradermally at doses ranging from 1 to 300 nmol site, which is inhibited by the BB2 bombesin receptor agonist RC-3095 and reduced in mast cell-deficient mice. Neuromedin C (3.2 nmol kg, i.p.) reduces rat glucose consumption by approximately 50% for up to one hour.

Urotensin II is a peptide vasoconstrictor and agonist of the urotensin (UT) receptor (Ki= 2.06 nM for the human recombinant receptor expressed in HEK293 cells).1It stimulates intracellular calcium mobilization in HEK293 cells expressing human and rat UT (EC50s = 0.47 and 0.78 nM, respectively) but decreases intracellular calcium concentration in goby (G. mirabilis) enterocytes when used at a concentration of 500 nM.2Urotensin II (20 mU/ml) stimulates active sodium and chloride absorption across isolated goby posterior intestine in 5% seawater-adapted solution.3In vivo, urotensin II (1.5-150 nmol/kg) decreases diastolic blood pressure and increases heart rate in anesthetized rats.4It also reduces the pressor responses to sympathetic nerve stimulation, norepinephrine , and vasopressin in pithed rats when administered at a dose of 150 nmol/kg. 1.Ames, R.S., Sarau, H.M., Chambers, J.K., et al.Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14Nature401(6750)282-286(1999) 2.Loretz, C.A., and Assad, J.A.Urotensin II lowers cytoplasmic free calcium concentration in goby enterocytes: Measurements using quin2Gen. Comp. Endocrinol.64(3)355-361(1986) 3.Loretz, C.A., Freel, R.W., and Bern, H.A.Specificity of response of intestinal ion transport systems to a pair of natural peptide hormone analogs: Somatostatin and urotensin IIGen. Comp. Endocrinol.52(2)198-206(1983) 4.Gibson, A., Wallace, P., and Bern, H.A.Cardiovascular effects of urotensin II in anesthetized and pithed ratsGen. Comp. Endocrinol.64(3)435-439(1986)

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.

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。

Paltusotine, also known as CRN00808, is a somatostatin receptor agonist.

Pasireotide (SOM230) diaspartate 是一种长效的环己肽生长激素抑制素类似物，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 <7.0 9.9。Pasireotide diaspartate 具有抗分泌、抗增殖和促凋亡活性。

Cyclic SSTR agonist octreotide 是一种 Octreotide ，可作为生长抑素受体 (SSTR) 的激动剂。

BIM-23027为高选择性sst2受体激动剂（EC50=0.32 nM），其功能效果类似生长抑素（SRIF，环状十四肽）。该化合物可促进多巴胺的释放，此过程通过Glu依赖的机制进行调控。

Zavolosotine (Compound 1) 是一种通过口服途径有效的生长抑素受体 5 型 (SST5) 激动剂，其EC50值小于1 nM。Zavolosotine 能够抑制胰岛素和胰高血糖素的分泌，并提高大鼠模型中血液的胰高血糖素水平。

Paltusotine 是一种口服有效的，非肽选择性生长抑素 2 型受体激动剂。在长效生长抑素受体配体作用后，Paltusotine 仍可维持 GH 和 IGF-1 水平。

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