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Miricorilant

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Miricorilant
Clinical data
Other namesCORT-118335
Legal status
Legal status
  • Investigational
Identifiers
  • trans-6-(4-phenylcyclohexyl)-5-[[3-(trifluoromethyl)phenyl]methyl]-1H-pyrimidine-2,4-dione
CAS Number
PubChemCID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC24H23F3N2O2
Molar mass428.455 g·mol−1
3D model (JSmol)
  • C1CC(CCC1C2=CC=CC=C2)C3=C(C(=O)NC(=O)N3)CC4=CC(=CC=C4)C(F)(F)F
  • InChI=1/C24H23F3N2O2/c25-24(26,27)19-8-4-5-15(13-19)14-20-21(28-23(31)29-22(20)30)18-11-9-17(10-12-18)16-6-2-1-3-7-16/h1-8,13,17-18H,9-12,14H2,(H2,28,29,30,31)/t17-,18-
  • Key:GVVUZBSCYAVFTI-IYARVYRRNA-N

Miricorilant (CORT-118335) is a small molecule that works as aselective glucocorticoid receptor modulator andmineralcorticoid receptor antagonist.[1][2][3][4] It was developed by Corcept Therapeutics fornonalcoholic steatohepatitis[5] and weight gain associated withatypical antipsychotics.[6]

See also

[edit]

References

[edit]
  1. ^Hunt, Hazel J.; Ray, Nicholas C.; Hynd, George; Sutton, Jon; Sajad, Mohammed; o'Connor, Elizabeth; Ahmed, Shahadat; Lockey, Peter; Daly, Steve; Buckley, Gerry; Clark, Robin D.; Roe, Robert; Blasey, Christine; Belanoff, Joe (2012). "Discovery of a novel non-steroidal GR antagonist with in vivo efficacy in the olanzapine-induced weight gain model in the rat".Bioorganic & Medicinal Chemistry Letters.22 (24):7376–7380.doi:10.1016/j.bmcl.2012.10.074.PMID 23131342.
  2. ^Mammi, C.; Marzolla, V.; Armani, A.; Feraco, A.; Antelmi, A.; Maslak, E.; Chlopicki, S.; Cinti, F.; Hunt, H.; Fabbri, A.; Caprio, M. (June 2016)."A novel combined glucocorticoid-mineralocorticoid receptor selective modulator markedly prevents weight gain and fat mass expansion in mice fed a high-fat diet".International Journal of Obesity.40 (6):964–972.doi:10.1038/ijo.2016.13.ISSN 1476-5497.PMID 26830012.S2CID 19751493.
  3. ^Nguyen, Elizabeth T.; Berman, Sarah; Streicher, Joshua; Estrada, Christina M.; Caldwell, Jody L.; Ghisays, Valentina; Ulrich-Lai, Yvonne; Solomon, Matia B. (1 August 2019). "Effects of combined glucocorticoid/mineralocorticoid receptor modulation (CORT118335) on energy balance, adiposity, and lipid metabolism in male rats".American Journal of Physiology. Endocrinology and Metabolism.317 (2):E337 –E349.doi:10.1152/ajpendo.00018.2019.PMID 31112405.S2CID 162170330.
  4. ^Nguyen, Elizabeth T.; Caldwell, Jody L.; Streicher, Joshua; Ghisays, Valentina; Balmer, Nikolaus J.; Estrada, Christina M.; Solomon, Matia B. (January 2018). "Differential effects of imipramine and CORT118335 (Glucocorticoid receptor modulator/mineralocorticoid receptor antagonist) on brain-endocrine stress responses and depression-like behavior in female rats".Behavioural Brain Research.336:99–110.doi:10.1016/j.bbr.2017.08.045.PMID 28866130.S2CID 5511661.
  5. ^Koorneef, Lisa L; van den Heuvel, José K; Kroon, Jan; Boon, Mariëtte R; ’t Hoen, Peter A C; Hettne, Kristina M; van de Velde, Nienke M; Kolenbrander, Kelsey B; Streefland, Trea C M; Mol, Isabel M; Sips, Hetty C M; Kielbasa, Szymon M; Mei, Hailiang; Belanoff, Joseph K; Pereira, Alberto M; Oosterveer, Maaike H; Hunt, Hazel; Rensen, Patrick C N; Meijer, Onno C (12 October 2018)."Selective glucocorticoid receptor modulation prevents and reverses non-alcoholic fatty liver disease in male mice".Endocrinology.159 (12):3925–3936.doi:10.1210/en.2018-00671.hdl:1887/79939.PMID 30321321.S2CID 53501584.
  6. ^Hunt, Hazel J.; Donaldson, Kirsteen; Strem, Mark; Tudor, Iulia Cristina; Sweet-Smith, Suzanne; Sidhu, Sharan (November–December 2021)."Effect of Miricorilant, a Selective Glucocorticoid Receptor Modulator, on Olanzapine-Associated Weight Gain in Healthy Subjects: A Proof-of-Concept Study".Journal of Clinical Psychopharmacology.41 (6):632–637.doi:10.1097/JCP.0000000000001470.ISSN 1533-712X.PMC 8575171.PMID 34369902.
GRTooltip Glucocorticoid receptor
Agonists
Mixed
(SEGRMsTooltip Selective glucocorticoid receptor agonists)
Antagonists
Others
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