We have discovered a novel compound, J-2156 [(1'S, 2S)-4-amino-N-(1'-carbamoyl-2'-phenylethyl)-2-(4''-methyl-1''-naphthalenesulfonylamino)butanamide], that belongs to a new class of somatostatin receptor ligands. J-2156 binds with nanomolar affinity to the human somatostatin receptor subtype 4 and is over 400-fold subtype-selective against the other somatostatin receptors. When evaluated in a [...

The peptide hormone somatostatin (SST) and its five G protein-coupled receptors (SSTR1-5) were described to be present in the skin, but their cutaneous function(s) and skin-specific signalling mechanisms are widely unknown. By using receptor specific agonists we show here that the SSTRs expressed in keratinocytes are functionally coupled to the inhibition of adenylate cyclase. In addition, trea...

OBJECTIVE Scintigraphy with a radiolabeled somatostatin analog ((111)In-diethylenetriaminepenta-acetic acid octreotide) detects the somatostatin receptors that are found in vitro in all meningiomas. Previous studies have proved the benefit of radioimmunoguided surgery, with a hand-held gamma probe, for the assessment and removal of neuroendocrine tumors. We conducted a study to determine whethe...

introduction: somatostatin receptors expressed on a wide range of human tumors, are potential targets for the peptide receptor radionuclide therapy (prrt). in this study, 177lu-[dota-dphe1, tyr3]octreotide (177lu-dotatoc) as an agent for prrt was prepared and its biodistribution was studied in rats. methods:the best condition for the preparation of the 177lu-dotatoc radiolabeled complex was det...

Carcinoid is a neuroendocrine neoplasm derived from primitive stem cells, occurring most frequently in the alimentary tract. Somatostatin-receptor scintigraphy with indium-111 pentetreotide is a sensitive and noninvasive technique for imaging carcinoid and its metastatic spread. However, nontumoral lesions such as sarcoidosis may also express somatostatin receptors, which may present a diagnost...

Although many aspects of the regulation of acid secretion at the cellular level among different species remains controversial, certain concepts have emerged that span the differences between species, model systems and investigators. The paracrine, endocrine, neural and autocrine pathways mediate acid secretion by acting both directly on the parietal cell and indirectly via modulation of mucosal...

British Journal of DermatologyVolume 184, Issue 2 p. e32-e32 PLAIN LANGUAGE SUMMARYFree Access Somatostatin receptors: an alternative treatment target for advanced Merkel cell carcinoma First published: 05 February 2021 https://doi.org/10.1111/bjd.19723AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text full-text accessPlease revie...

BACKGROUND Neuroendocrine cells have been found in all stages of prostate cancer. Neuroendocrine differentiation of prostate adenocarcinoma is a possible target for therapeutic strategies, such as administration of GH analogs (e.g., somatostatin), especially in patients with hormone-refractory prostate cancer (HRPC). The presence of receptors for these drugs in tumor cells and tissues is essent...