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J-2156
Identifiers
	IUPAC name (2S)-4-amino-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-2-[(4-methylnaphthalen-1-yl)sulfonylamino]butanamide;
CAS Number	848647-56-3;
PubChem CID	11442741;
IUPHAR/BPS	10115;
ChemSpider	9617604;
UNII	H35JAI9M2X;
ChEMBL	ChEMBL4451852;
PDB ligand	I8B (PDBe, RCSB PDB);
Chemical and physical data
Formula	C24H28N4O4S
Molar mass	468.57 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=CC=C(C2=CC=CC=C12)S(=O)(=O)N[C@@H](CCN)C(=O)N[C@@H](CC3=CC=CC=C3)C(=O)N;
	InChI InChI=1S/C24H28N4O4S/c1-16-11-12-22(19-10-6-5-9-18(16)19)33(31,32)28-20(13-14-25)24(30)27-21(23(26)29)15-17-7-3-2-4-8-17/h2-12,20-21,28H,13-15,25H2,1H3,(H2,26,29)(H,27,30)/t20-,21-/m0/s1; Key:VTNCZBXJSGKDLS-SFTDATJTSA-N;

J-2156 is a chemical compound which was one of the first compounds developed that acts as an agonist at somatostatin receptor 4. It has analgesic and anti-hyperalgesic effects and is widely used in research into the role of SST4 receptors in pain perception and other neurological functions.^[1]^[2]^[3]^[4]^[5]^[6]^[7]^[8]^[9]^[10]

References

↑ Engström M, Tomperi J, El-Darwish K, Ahman M, Savola JM, Wurster S (January 2005). "Superagonism at the human somatostatin receptor subtype 4". The Journal of Pharmacology and Experimental Therapeutics. 312 (1): 332–338. doi:10.1124/jpet.104.075531. PMID 15333679.
↑ Sándor K, Elekes K, Szabó A, Pintér E, Engström M, Wurster S, et al. (June 2006). "Analgesic effects of the somatostatin sst4 receptor selective agonist J-2156 in acute and chronic pain models". European Journal of Pharmacology. 539 (1–2): 71–75. doi:10.1016/j.ejphar.2006.03.082. PMID 16697366.
↑ Elekes K, Helyes Z, Kereskai L, Sándor K, Pintér E, Pozsgai G, et al. (January 2008). "Inhibitory effects of synthetic somatostatin receptor subtype 4 agonists on acute and chronic airway inflammation and hyperreactivity in the mouse". European Journal of Pharmacology. 578 (2–3): 313–322. doi:10.1016/j.ejphar.2007.09.033. hdl:2437/78619. PMID 17961545.
↑ Scheich B, Gaszner B, Kormos V, László K, Ádori C, Borbély É, et al. (February 2016). "Somatostatin receptor subtype 4 activation is involved in anxiety and depression-like behavior in mouse models". Neuropharmacology. 101: 204–215. doi:10.1016/j.neuropharm.2015.09.021. PMID 26387439.
↑ Shenoy PA, Kuo A, Khan N, Gorham L, Nicholson JR, Corradini L, et al. (2018). "The Somatostatin Receptor-4 Agonist J-2156 Alleviates Mechanical Hypersensitivity in a Rat Model of Breast Cancer Induced Bone Pain". Frontiers in Pharmacology. 9 495. doi:10.3389/fphar.2018.00495. PMC 5962878. PMID 29867498.
↑ Park TS, Khan N, Kuo A, Nicholson JR, Corradini L, Smith MT (September 2019). "J-2156, a somatostatin receptor type 4 agonist, alleviates mechanical hyperalgesia in a rat model of chronic low back pain". Biomedicine & Pharmacotherapy = Biomedecine & Pharmacotherapie. 117 109056. doi:10.1016/j.biopha.2019.109056. PMID 31181441.
↑ Kecskés A, Pohóczky K, Kecskés M, Varga ZV, Kormos V, Szőke É, et al. (October 2020). "Characterization of Neurons Expressing the Novel Analgesic Drug Target Somatostatin Receptor 4 in Mouse and Human Brains". International Journal of Molecular Sciences. 21 (20): 7788. doi:10.3390/ijms21207788. PMC 7589422. PMID 33096776.
↑ Szőke É, Bálint M, Hetényi C, Markovics A, Elekes K, Pozsgai G, et al. (November 2020). "Small molecule somatostatin receptor subtype 4 (sst₄) agonists are novel anti-inflammatory and analgesic drug candidates". Neuropharmacology. 178 108198. doi:10.1016/j.neuropharm.2020.108198. PMID 32739276.
↑ Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, et al. (August 2022). "Structural insights into ligand recognition and selectivity of somatostatin receptors". Cell Research. 32 (8): 761–772. doi:10.1038/s41422-022-00679-x. PMC 9343605. PMID 35739238.
↑ Kuo A, Imam MZ, Li R, Lin L, Raboczyj A, Bohmer AE, et al. (2024). "J-2156, a small molecule somatostatin type 4 receptor agonist, alleviated hindpaw hypersensitivity in the streptozotocin-induced rat model of painful diabetic neuropathy but with a 2-fold decrease in potency at an advanced stage in the model, mimicking morphine". Frontiers in Pharmacology. 15 1346801. doi:10.3389/fphar.2024.1346801. PMC 10839067. PMID 38318132.

[1] Engström M, Tomperi J, El-Darwish K, Ahman M, Savola JM, Wurster S (January 2005). "Superagonism at the human somatostatin receptor subtype 4". The Journal of Pharmacology and Experimental Therapeutics. 312 (1): 332–338. doi:10.1124/jpet.104.075531. PMID 15333679.

[2] Sándor K, Elekes K, Szabó A, Pintér E, Engström M, Wurster S, et al. (June 2006). "Analgesic effects of the somatostatin sst4 receptor selective agonist J-2156 in acute and chronic pain models". European Journal of Pharmacology. 539 (1–2): 71–75. doi:10.1016/j.ejphar.2006.03.082. PMID 16697366.

[3] Elekes K, Helyes Z, Kereskai L, Sándor K, Pintér E, Pozsgai G, et al. (January 2008). "Inhibitory effects of synthetic somatostatin receptor subtype 4 agonists on acute and chronic airway inflammation and hyperreactivity in the mouse". European Journal of Pharmacology. 578 (2–3): 313–322. doi:10.1016/j.ejphar.2007.09.033. hdl:2437/78619. PMID 17961545.

[4] Scheich B, Gaszner B, Kormos V, László K, Ádori C, Borbély É, et al. (February 2016). "Somatostatin receptor subtype 4 activation is involved in anxiety and depression-like behavior in mouse models". Neuropharmacology. 101: 204–215. doi:10.1016/j.neuropharm.2015.09.021. PMID 26387439.

[5] Shenoy PA, Kuo A, Khan N, Gorham L, Nicholson JR, Corradini L, et al. (2018). "The Somatostatin Receptor-4 Agonist J-2156 Alleviates Mechanical Hypersensitivity in a Rat Model of Breast Cancer Induced Bone Pain". Frontiers in Pharmacology. 9 495. doi:10.3389/fphar.2018.00495. PMC 5962878. PMID 29867498.

[6] Park TS, Khan N, Kuo A, Nicholson JR, Corradini L, Smith MT (September 2019). "J-2156, a somatostatin receptor type 4 agonist, alleviates mechanical hyperalgesia in a rat model of chronic low back pain". Biomedicine & Pharmacotherapy = Biomedecine & Pharmacotherapie. 117 109056. doi:10.1016/j.biopha.2019.109056. PMID 31181441.

[7] Kecskés A, Pohóczky K, Kecskés M, Varga ZV, Kormos V, Szőke É, et al. (October 2020). "Characterization of Neurons Expressing the Novel Analgesic Drug Target Somatostatin Receptor 4 in Mouse and Human Brains". International Journal of Molecular Sciences. 21 (20): 7788. doi:10.3390/ijms21207788. PMC 7589422. PMID 33096776.

[8] Szőke É, Bálint M, Hetényi C, Markovics A, Elekes K, Pozsgai G, et al. (November 2020). "Small molecule somatostatin receptor subtype 4 (sst₄) agonists are novel anti-inflammatory and analgesic drug candidates". Neuropharmacology. 178 108198. doi:10.1016/j.neuropharm.2020.108198. PMID 32739276.

[9] Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, et al. (August 2022). "Structural insights into ligand recognition and selectivity of somatostatin receptors". Cell Research. 32 (8): 761–772. doi:10.1038/s41422-022-00679-x. PMC 9343605. PMID 35739238.

[10] Kuo A, Imam MZ, Li R, Lin L, Raboczyj A, Bohmer AE, et al. (2024). "J-2156, a small molecule somatostatin type 4 receptor agonist, alleviated hindpaw hypersensitivity in the streptozotocin-induced rat model of painful diabetic neuropathy but with a 2-fold decrease in potency at an advanced stage in the model, mimicking morphine". Frontiers in Pharmacology. 15 1346801. doi:10.3389/fphar.2024.1346801. PMC 10839067. PMID 38318132.

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See also

References