Monlunabant Explained

Legal Status:Investigational
Synonyms:INV-202, MRI-1891
Pubchem:164888943
Unii:4G8X27X87A
Iupac Name:N-[(''E'')-''{{prime|N}}''-[(''Z'')-''C''-[(4''S'')-5-(4-Chlorophenyl)-4-phenyl-3,4-dihydropyrazol-2-yl]-N-[4-(trifluoromethyl)phenyl]sulfonylcarbonimidoyl]carbamimidoyl]acetamide
C:26
H:22
Cl:1
F:3
N:6
O:3
S:1

Monlunabant (INV-202, MRI-1891, or S-MRI-1891) is a peripherally selective cannabinoid receptor 1 inverse agonist, discovered as a β-arrestin-2-biased cannabinoid receptor 1 antagonist by the National Institutes of Health.[1] It was developed as a weight loss drug by Inversago Pharma.[2] [3] [4]

Notes and References

  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 . Functional Selectivity of a Biased Cannabinoid-1 Receptor (CB 1 R) Antagonist . ACS Pharmacology & Translational Science . 11 June 2021 . 4 . 3 . 1175–1187 . 10.1021/acsptsci.1c00048. free . 8204328 .
  2. Crater . Glenn D. . Ravenelle . Francois . Lalonde . Karine . DespréS . Jean-Pierre . 431-P: Effects of CB1 Antagonist INV-202 in Patients with Metabolic Syndrome—A Randomized, Placebo-Controlled, Double-Blind Phase 1B Study . Diabetes . 20 June 2023 . 72 . Supplement_1 . 10.2337/db23-431-P. 259384475 .
  3. Book: 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. . B15. Asthma: Hot off the Press from the Bench to the Clinic . Cannabinoid Receptor 1 Inverse Agonist, INV-202, Induces Weight Loss and Reduces Airway Hyperreactivity in a Mouse Model of Obese Asthma . May 2023 . A2759 . 10.1164/ajrccm-conference.2023.207.1_MeetingAbstracts.A2759. 258446002 .
  4. Crater . Glenn D. . Lalonde . Karine . Ravenelle . François . Harvey . Michael . Després . Jean-Pierre . 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 . 8 November 2023 . 10.1111/dom.15353. 37941317 . free .