SSTR4 Agonist

Mazisotine (CNTX-0290) is an orally active, non-opioid somatostatin receptor 4 (SSTR4) agonist with an EC₅₀ of 4.7 nM. Mazisotine exerts significant analgesic effects in various nociceptive (inflammatory, osteoarthritic) and neuropathic pain models. Mazisotine can be used for pain research.

TT-232 (CAP-232), a somatostatin derivative, is a peptide SSTR1/SSTR4 agonist. TT-232 inhibits cancer cell proliferation and induces apoptosis. TT-232 is also a broad-spectrum anti-inflammatory and analgesic agent.

Veldoreotide (DG3173) TFA a somatostatin analogue, binds to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide TFA inhibits growth hormone (GH) secretion in adenomas compared with Octreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent

SSTR4 agonist 6 (Compound 1) is a SSTR4 agonist. SSTR4 agonist 6 can be used for pain research.

L803 is a selective Somatostatin Receptor Subtype 4 (SST4) agonist. L803 inhibits L-type calcium channel currents (I_Ca). L803 is promising for research of retinal ganglion cell (RGC) degenerative diseases (e.g., glaucoma).

SSTR4 agonist 5 (Compound 5) is the orally active agonist for somatostatin receptor 4 (SSTR4) with an EC₅₀ of 0.228 nM. SSTR4 agonist 5 exhibits good stability in human/rat liver microsomes. SSTR4 agonist 5 inhibits mechanical hyperalgesia in rat models.