sstr

Octreotide (SMS 201-995) is a potent inhibitor of growth hormone, glucagon, and insulin.

Octreotide Acetate (Sandostatin) is a potent, long-acting synthetic somatostatin octapeptide analog that inhibits secretion of growth hormone.

Paltusotine is a nonpeptide, small molecule somatostatin type 2 (SST2) receptor agonist with high oral bioavailability. Paltusotine maintains GH and IGF-1 levels in acromegaly patients

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.

Octreotide, a cyclic SSTR agonist, serves as the cyclic Somatostatin Receptor SSTR agonist [1].

SSTR5 antagonist 1 is a selective, and orally available antagonist of somatostatin receptor subtype 5 (SSTR5)(IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively).

SSTR5 antagonist 2 is a highly potent, oral active and selective antagonist of somatostatin (receptor) subtype 5 (SSTR5),with potential to treat type 2 diabetes mellitus (T2DM).

SSTR5 antagonist 2 TFA is a highly potent, oral active and selective antagonist of somatostatin (receptor) subtype 5 (SSTR5), with potential to treat type 2 diabetes mellitus (T2DM).

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].

SSTR5 antagonist 2 hydrochloride is a potent, orally active, selective antagonist of the growth hormone inhibitory hormone (receptor) subtype 5 (SSTR5), with potential for investigation in type 2 diabetes.

SSTR5 antagonist 3 (Compound 23) serves as a potent somatostatin receptor subtype 5 (SSTR5) antagonist, demonstrating oral activity and minimal hERG inhibition. It shows significant efficacy, with IC50 values of 2.8 nM in humans and 1.4 nM in mice. This compound is utilized in gallstone research [1].

SSTR5 antagonist 6, an orally active antagonist specific to the somatostatin receptor subtype 5 (SSTR5), exhibits an IC50 value of 24 nM. This compound is utilized in researching type 2 diabetes [1].

212Pb-DOTAMTATE is a bifunctional ligand used to prepare Pb212-complex and serves as a targeted alpha radiation therapy for metastatic neuroendocrine tumors that express SSTR. It may have significant clinical implications when used alone or in combination with chemotherapeutic compounds.

DOTA-LM3 TFA is a somatostatin receptor (SSTR) antagonist with the molecular structure p-Cl-Phe-cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr-NH2, used for in vivo tumor tracing via isotopic labeling, such as 177Lu-DOTA-LM3 TFA and 68Ga-DOTA-LM3 TFA. The 68Ga-labeled compound shows favorable biodistribution, high tumor uptake, good tumor retention, and minimal safety concerns, while the 177Lu-labeled variant targets DOTATOC-negative liver metastases, including pancreatic NET and extensive tumor thrombosis [1] [2].

DOTA-LM3 is a somatostatin receptor (SSTR) antagonist, with LM3 denoting the peptide sequence p-Cl-Phe-cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr-NH2. It is utilized in the isotopic labeling of tumors for in vivo tracing, notably with 177Lu-DOTA-LM3 and 68Ga-DOTA-LM3. The derivative 68Ga-DOTA-LM3 exhibits promising biodistribution, high tumor uptake, efficient tumor retention, and minimal safety concerns, while 177Lu-DOTA-LM3 is applied in research on DOTATOC-negative liver metastases including pancreatic NET and extensive tumor thrombosis [1] [2].

NODAGA-LM3, when labeled with ^68Ga, serves as a PET imaging agent. As an SSTR2 antagonist, ^68Ga-NODAGA-LM3 is utilized for the visualization of SSTR-positive paragangliomas [1] [2].

NODAGA-LM3 TFA, a SSTR2 antagonist, can be radiolabeled with ^68Ga for PET imaging applications, particularly in the visualization of SSTR-positive paragangliomas [1] [2].

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].

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