sstr3

MK-4256 is an effective and selective SSTR3 antagonist (IC50s: 0.66 nM and 0.36 nM in human and mouse receptor binding assays, respectively).

BIM 23056 Acetate is a  potent and surmountable human recombinant sst5 receptor antagonist.

BN-81,674 is a bioactive chemical.

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.

MK-1421 is a potent and selective sstr3 antagonist.

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.