sst1

L-797,591 hydrochloride is active for somatostatin receptor isoform 1 (SSTR1). L-797,591 hydrochloride is commonly used in combination with AG1478 to enhance p-ERK5 expression in SSTR1 cells. L-797,591 hydrochloride significantly enhanced p38 phosphorylation in cotransfected cells, and this effect was reversed in combination with AG1478.

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.

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.

Cortistatin-14, a neuropeptide structurally similar to growth inhibitor-14, has anticonvulsant and neuroprotective effects and impairs recognition memory consolidation in mice through activation of sst(2), growth hormone-releasing peptide, and GABA(A B) receptor, which can be used to study sepsis-induced cognitive impairment.

sst1/sst4 somatostatin receptors agonist

Pasireotide L-aspartate salt is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1 2 3 4 5, pKi=8.2 9.0 9.1 <7.0 9.9 respectively).

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

Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1 2 3 4 5, pKi=8.2 9.0 9.1 <7.0 9.9 respectively).

Pasireotide is a stable cyclohexapeptide somatostatin mimic.

SRA880 is a non-peptide antagonist of somatostatin sst1-receptor. SRA880 displayed significantly lower affinity for the other human recombinant somatostatin receptors ( pK(d) < or = 6.0). SRA880 shows a certain binding affinity to the human dopamine D4 re

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.

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.

Pasireotide diaspartate (SOM230), a long-acting cyclohexapeptide and somatostatin analog, enhances agonist activity across somatostatin receptor subtypes (sst1 2 3 4 5, with pK i values of 8.2, 9.0, 9.1, <7.0, and 9.9, respectively). This compound demonstrates antisecretory, antiproliferative, and proapoptotic activities [1] [2].

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].

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.

Cortistatin-14 acetate, a neuropeptide have structural similarity to somatostatin-14, binds and exerts its function via the somatostatin receptors (sst1-sst5). Cortistatin-14 acetate shows anticonvulsive, neuroprotective effect and remarkable anti-inflammatory properties

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).