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Monlunabant

From Wikipedia, the free encyclopedia
(Redirected fromINV-202)
Chemical compound
Pharmaceutical compound
Monlunabant
Clinical data
Other namesINV-202, MRI-1891
Legal status
Legal status
  • Investigational
Identifiers
  • N-[(E)-N′-[(Z)-C-[(4S)-5-(4-Chlorophenyl)-4-phenyl-3,4-dihydropyrazol-2-yl]-N-[4-(trifluoromethyl)phenyl]sulfonylcarbonimidoyl]carbamimidoyl]acetamide
CAS Number
PubChemCID
ChemSpider
UNII
Chemical and physical data
FormulaC26H22ClF3N6O3S
Molar mass591.01 g·mol−1
3D model (JSmol)
  • CC(=O)N/C(=N/C(=N/S(=O)(=O)C1=CC=C(C=C1)C(F)(F)F)/N2C[C@@H](C(=N2)C3=CC=C(C=C3)Cl)C4=CC=CC=C4)/N
  • InChI=1S/C26H22ClF3N6O3S/c1-16(37)32-24(31)33-25(35-40(38,39)21-13-9-19(10-14-21)26(28,29)30)36-15-22(17-5-3-2-4-6-17)23(34-36)18-7-11-20(27)12-8-18/h2-14,22H,15H2,1H3,(H3,31,32,33,35,37)/t22-/m1/s1
  • Key:GYJPQNPVIJXXTA-JOCHJYFZSA-N

Monlunabant (INV-202, MRI-1891, or S-MRI-1891) is aperipherally selectivecannabinoid receptor 1inverse agonist, discovered as a β-arrestin-2-biased cannabinoid receptor 1 antagonist by Dr George Kunos, Dr Resat Cinar, and Dr Malliga Iyer at theNational Institutes of Health.[1] It was developed as aweight loss drug by Inversago Pharma.[2][3][4]

Novo Nordisk’s obesity drug monlunabant showed only modest weight loss in a Phase 2a trial.[5] The drug was associated with higher rates of mild to moderate neuropsychiatric side effects like anxiety and sleep disturbances.[6] Suicidal ideations were not reported.

See also

[edit]

References

[edit]
  1. ^Liu, Ziyi; Iyer, Malliga R.; Godlewski, Grzegorz; Jourdan, Tony; Liu, Jie; Coffey, Nathan J.; Zawatsky, Charles N.; Puhl, Henry L.; Wess, Jürgen; Meister, Jaroslawna; Liow, Jeih-San; Innis, Robert B.; Hassan, Sergio A.; Lee, Yong Sok; Kunos, George; Cinar, Resat (11 June 2021)."Functional Selectivity of a Biased Cannabinoid-1 Receptor (CB 1 R) Antagonist".ACS Pharmacology & Translational Science.4 (3):1175–1187.doi:10.1021/acsptsci.1c00048.PMC 8204328.PMID 34151207.</
  2. ^Crater, Glenn D.; Ravenelle, Francois; Lalonde, Karine; DespréS, Jean-Pierre (20 June 2023). "431-P: Effects of CB1 Antagonist INV-202 in Patients with Metabolic Syndrome—A Randomized, Placebo-Controlled, Double-Blind Phase 1B Study".Diabetes.72 (Supplement_1).doi:10.2337/db23-431-P.S2CID 259384475.
  3. ^Morris, C.R.; Chandrasekaran, R.; Butzirius, I.; Daphtary, N.; Aliyeva, M.; Bates, J.H.T.; Anathy, V.; Crater, G.D.; Gaucher, G.; Dixon, A.E. (May 2023). "Cannabinoid Receptor 1 Inverse Agonist, INV-202, Induces Weight Loss and Reduces Airway Hyperreactivity in a Mouse Model of Obese Asthma".B15. Asthma: Hot off the Press from the Bench to the Clinic. pp. A2759.doi:10.1164/ajrccm-conference.2023.207.1_MeetingAbstracts.A2759.S2CID 258446002.
  4. ^Crater, Glenn D.; Lalonde, Karine; Ravenelle, François; Harvey, Michael; Després, Jean-Pierre (8 November 2023)."Effects of CB1R inverse agonist, INV -202, in patients with features of metabolic syndrome. A randomized, placebo-controlled, double-blind phase 1b study".Diabetes, Obesity and Metabolism.26 (2):642–649.doi:10.1111/dom.15353.PMID 37941317.
  5. ^Chen, Elaine (2024-09-20)."Novo's new obesity drug shows modest results, raises concerns of psychiatric side effects".STAT. Retrieved2024-09-21.
  6. ^"News Details".Novo Nordisk. Retrieved2024-09-21.
Receptor
(ligands)
CB1Tooltip Cannabinoid receptor type 1
Agonists
(abridged,
full list)
Inverse agonists
Antagonists
CB2Tooltip Cannabinoid receptor type 2
Agonists
Antagonists
NAGly
(GPR18)
Agonists
Antagonists
GPR55
Agonists
Antagonists
GPR119
Agonists
Transporter
(modulators)
eCBTsTooltip Endocannabinoid transporter
Enzyme
(modulators)
FAAHTooltip Fatty acid amide hydrolase
MAGL
ABHD6
ABHD12
Others
  • Others:2-PG(directly potentiates activity of 2-AG at CB1 receptor)
  • ARN-272(FAAH-like anandamide transporter inhibitor)
See also
Receptor/signaling modulators
Cannabinoids (cannabinoids by structure)
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