sstr4

SSTR4agonist-1 (Compound 47) is a selective agonist of the somatostatin receptor 4 (SSTR4), with an EC50 of 4.7 nM. It has a half-life of over 130 minutes in human liver microsomes.

SSTR4 agonist5 (Compound 5) is an orally active agonist of the somatostatin receptor 4 (SSTR4) with an EC50 of 0.228 nM. It demonstrates good stability in human rat liver microsomes and can inhibit mechanical hyperalgesia in rat models.

SSTR4 agonist 2 is a potent somatostatin receptor subtype 4 (SSTR4) agonist with potential applications in research on SSTR4-related medical disorders. The SSTR4 pathway inhibits nociceptive and inflammatory processes [1].

SSTR4 agonist 4 is a potent SSTR4 agonist with potential applications in pain research. SSTR4 agonists demonstrate efficacy in rodent models of pain associated with acute and chronic anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, regions involved in memory and learning, and in Alzheimer's disease pathology [1].

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

(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 is a potential SSTR4 agonist.

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.

Cortistatin 29, a neuropeptide, alleviates neuropathic pain and exhibits anti-fibrotic effects. It binds with high affinity to all somatostatin (SS) receptor subtypes, displaying IC 50 values of 2.8 nM for SSTR1, 7.1 nM for SSTR2, 0.2 nM for SSTR3, 3.0 nM for SSTR4, and 13.7 nM for SSTR5, respectively [1] [2] [3] [4].

'(D-Phe5,Cys6,11,N-Me-D-Trp8)-Somatostatin-14 (5-12) amide (Compound 4) is a somatostatin analogue exhibiting varying affinity for somatostatin receptors, with dissociation constants (Kd) of 0.61 nM for SSTR5, 11.05 nM for SSTR3, 23.5 nM for SSTR2, 1200 nM for SSTR1, and >1000 nM for SSTR4, respectively [1].'

Veldoreotide (DG3173) TFA, a somatostatin analogue, effectively binds to and activates somatostatin receptors (SSTR) 2, 4, and 5. This compound demonstrates a higher efficacy in inhibiting growth hormone (GH) secretion in adenomas than Octreotide, showcasing its potential as a pain modulating agent [1].

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.