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. 2021 Aug 31;22(17):9472. doi: 10.3390/ijms22179472

Table 9.

Examples of peripheral CB1R antagonists and their therapeutic windows.

CB1R Antagonists Biological Effect(s) and/or Mechanism of Action Reference
i. SR141716A (Rimonabant)—the first developed CB1R antagonist.
Now discontinued due to unwanted side effects such as depression, anxiety, and suicidal thoughts.
  • -

    Obesity possibly via inducing loss of appetite or increase in metabolic rate (loss of fat mass) via interaction with corticotropin-releasing hormone (CRH), a known anorexigenic

  • -

    Rimonabant inhibits CB1R activation which is responsible for lipogenesis

  • -

    Tobacco addiction

  • -

    Inhibition of cannabinoid-induced heroin-seeking behaviour in rats

 [6,136,372,373]
ii. AM251
  • -

    Attenuates mechanical allodynia

  • -

    Attenuates thermal hyperalgesia

  • -

    Anti-nociceptive

  • -

    Anti-depressive effects

  • -

    Improves recognition memory in murine model

  • -

    Anti-cancer/modulation of tumour growth in mice

 [374,375,376]
iii. SLV-326 (Solvay)
  • -

    May have anti-obesity, anti-addiction, anti-depressant, and anxiolytic effects

 [136]
iv. LY320135 (Lilly)
  • -

    May have anti-obesity, anti-addiction, anti-depressant, and anxiolytic effects

 [136,372,377]
Neutral Antagonists
v. AM4113
  • -

    Prevents opioid addiction (self-administration) in rodent model

  • -

    Anti-depressant

  • -

    Anxiolytic

  • -

    Prevents relapse to nicotine-seeking behaviour in rats

  • -

    Anti-obesity via suppression of appetite

  • -

    Regulate body weight in rats

  • -

    Anti-nauseant

 [136,378,379,380,381,382]
vi. O-2654 (Organix)
  • -

    May have anti-obesity, anti-addiction, anti-depressant, and anxiolytic effects

 [136]
vii. AM5171 (University of Connecticut)
  • -

    May have anti-obesity, anti-addiction, anti-depressant, and anxiolytic effects

 [6,136,272,338,373]