1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. Somatostatin Receptor
  4. SSTR4 Isoform

SSTR4

SSTR4 (somatostatin receptor subtype 4) is a member of the somatostatin receptor family and belongs to the class A G protein-coupled receptor (GPCR) superfamily with seven transmembrane domains, mediating cellular responses to somatostatin signaling.[1][2] Mechanistically, SSTR4 regulates intracellular signaling through inhibition of adenylate cyclase activity and activation of downstream kinase pathways, including phosphoinositide-3 kinase (PI3K) and extracellular signal-regulated kinase (ERK)/MAPK signaling, thereby linking receptor activation to neuronal and cellular responses.[3][4] Consistent with its prominent expression in the central nervous system, SSTR4 has been implicated in the regulation of neuronal excitability, and receptor activation couples to the M-current to modulate seizure susceptibility in experimental models.[5] Disease-related studies further demonstrate that selective SSTR4 activation produces analgesic effects in preclinical pain models, where the highly selective agonist J-2156 reverses pain-like behaviors and reduces spinal ERK phosphorylation associated with central sensitization.[6] Compared with other somatostatin receptor isoforms, SSTR4 has attracted particular interest because it mediates analgesic, anti-inflammatory, and antidepressant actions without the endocrine effects commonly associated with other receptor subtypes, supporting efforts to achieve subtype-selective pharmacology.[7] For experimental applications, selective agonists including J-2156 and other SSTR4-preferring ligands are widely used to investigate receptor-specific signaling, neurobiology, and therapeutic mechanisms while minimizing off-target activation of related somatostatin receptor isoforms.[6][7]

SSTR4 Related Products (13):

Cat. No. Product Name Effect Purity
  • HY-P1932
    Cortistatin-14
    99.98%
    Cortistatin-14 is a neuropeptide that shares structural similarities with somatostatin, working by binding to somatostatin receptors (sst1-sst5). Cortistatin-14 (TFA) has anticonvulsant, neuroprotective effects, and significant anti-inflammatory properties.
  • HY-139347
    Mazisotine
    Agonist 99.54%
    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.
  • HY-105172
    TT-232
    Agonist 98.72%
    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.
  • HY-P4452
    PRL 2915
    Antagonist 99.92%
    PRL 2915 is a potent human somatostatin subtype 2 receptor (hsst2) antagonist with a Ki of 12 nM.
  • HY-P0024A
    Veldoreotide TFA
    Agonist 98.97%
    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
  • HY-W1117589
    SSTR4 agonist 6
    Agonist
    SSTR4 agonist 6 (Compound 1) is a SSTR4 agonist. SSTR4 agonist 6 can be used for pain research.
  • HY-P0024
    Veldoreotide
    Activator
    Veldoreotide (DG3173) a somatostatin analogue, binds to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide inhibits growth hormone (GH) secretion in adenomas compared withOctreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent
  • HY-P3618
    Cortistatin-29 (reduced)
    98.12%
    Cortistatin-29 is a neuropeptide. Cortistatin-29 alleviates neuropathic pain. Cortistatin-29 binds all somatostatin (SS) receptor subtypes with high affinity and shows IC50 values of 2.8 nM, 7.1 nM, 0.2 nM, 3.0 nM, 13.7 nM for SSTR1, SSTR2, SSTR3, SSTR4, SSTR5, respectively. Cortistatin-29 shows anti-fibrotic effects.
  • HY-P4469
    PRL 3195
    Antagonist
    PRL 3195 is a somatostatin receptor antagonist with Kis of 6, 17, 66, 1000 and 1000 nM for human somatostatin receptors (sst5, sst2, sst3, sst1 and sst4, respectively).
  • HY-142701
    SSTR4 agonist 4
    Activator
    SSTR4 agonist 4 is a somatostatin receptor 4 (SSTR4) agonist. SSTR4 agonist 4 functionally activates SSTR4. SSTR4 agonist 4 has the potential for the research of pain.
  • HY-P1384
    L803
    Agonist
    L803 is a selective Somatostatin Receptor Subtype 4 (SST4) agonist. L803 inhibits L-type calcium channel currents (ICa). L803 is promising for research of retinal ganglion cell (RGC) degenerative diseases (e.g., glaucoma).
  • HY-172147
    SSTR4 agonist 5
    Agonist
    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.
  • HY-P2150
    Cortistatin-29 (rat)
    Cortistatin-29 is a neuropeptide. Cortistatin-29 alleviates neuropathic pain. Cortistatin-29 binds all somatostatin (SS) receptor subtypes with high affinity and shows IC50 values of 2.8 nM, 7.1 nM, 0.2 nM, 3.0 nM, 13.7 nM for SSTR1, SSTR2, SSTR3, SSTR4, SSTR5, respectively. Cortistatin-29 shows anti-fibrotic effects.