Drug intelligence / Profile preview

cyclosomatostatin

Development stage
Preclinical
Modality
Peptides, Small Molecules
Administration
In Vitro (laboratory Research), Not For Clinical Use
01

Overview

Cyclosomatostatin is a **synthetic, non-selective antagonist of somatostatin receptors (sst receptors)**, primarily used as a research tool in laboratory settings. It blocks the effects of endogenous somatostatin, interfering with signaling through somatostatin receptor subtypes, especially SSTR1, but also the broader class of somatostatin receptors. Its antagonism affects functions such as inhibition of hormone release (e.g., growth hormone, insulin, glucagon), neurotransmitter release, and some gastrointestinal and endocrine pathways. In certain cell lines (e.g., SH-SY5Y neuroblastoma), it has paradoxically exhibited partial agonist/agonist-like effects. Cyclosomatostatin has also demonstrated opioid receptor agonist activity in specific experimental models, highlighting possible off-target consequences. It is not an approved therapeutic agent and is used only in experimental models to investigate the physiological and pathophysiological role of somatostatin signaling[1][2][3][4][5][6].

Other names
cyclo-(7-aminoheptanoyl-Phe-D-Trp-Lys-Thr[Bzl])cyclo-somatostatinCyclosomatostatin Acetate
02

Targets

MOR (Mu opioid receptor)SSTR1 (Somatostatin Receptor Type 1)

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