sst4

Pasireotide (SOM230) acetate is a long-acting cyclohexapeptide growth hormone inhibitory hormone analog with antisecretory, antiproliferative, and proapoptotic activities.Pasireotide (SOM230) acetate inhibits the secretion of GH, IGF-I, and ACTH, and can be used in the study of acromegaly and Cushing's disease. Pasireotide (SOM230) acetate also enhances the agonist activity of growth inhibitory receptors, with pKi of 8.2, 9.0, 9.1, <7.0 and 9.9 for sst1, 2, 3, 4 and 5, respectively.

L-803087 is a potent and selective agonist of the growth inhibitor sst4 receptor with a Ki value of 0.7 nM for sst4, demonstrating over 280-fold selectivity compared to other growth inhibitory receptors. L-803087 induces AMPA-mediated synaptic responses in the hippocampus in vitro and increases seizures in alginate-induced seizure-busting mice in vivo.

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

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

Pasireotide is a stable cyclohexapeptide somatostatin mimic.

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.

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.

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 is a selective SST4 receptor (somatostatin receptor type 4) agonist with IC50 values of 0.05 nM and 0.07 nM for human and rat SST4 receptors respectively. It exhibits anti-inflammatory and analgesic effects while reducing pERK levels.

PRL 2915 is a potent antagonist of the human somatostatin subtype 2 receptor (hsst 2), exhibiting a binding affinity (K_i) of 12 nM [1].

PRL 3195 is a somatostatin receptor antagonist with K i values of 6, 17, 66, 1000, and 1000 nM for human somatostatin receptors sst 5, sst 2, sst 3, sst 1, and sst 4, 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.

Somatostatin sst4 receptor agonist

sst1/sst4 somatostatin receptors agonist

L-796,778 acetate is a slective somatostatin receptor agonist with IC50 of 24nM for sst3, for sst1, sst2, sst4 and sst5, IC50 is >1000nM.

CYN 154806 TFA is a cyclic octapeptide and an effective selective somatostatin sst2 receptor antagonist. For the recombinant sst2, sst1, sst3, sst4 and sst5 receptors, the pIC50 values are 8.58, 5.41, 6.07, 5.76 and 6.48, respectively.

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).

L803 is a selective somatostatin receptor type 4 (SST4) agonist that can inhibit L-type calcium channel currents (ICa). It holds potential for research into degenerative diseases of retinal ganglion cells (RGC), such as glaucoma.