CB1 inverse agonist
CB1 cannabinoid receptor inverse agonist
- Inverse agonist at CB1 → suppresses constitutive endocannabinoid signaling
- Appetite suppression and weight loss
- Loss of central endocannabinoid tone → depression/suicidality
- None currently available
- removed from European market due to psychiatric adverse effects (↑ suicidality)
Drugs with this mechanism (1)
- Rimonabant — CB1 antagonist weight-loss drug withdrawn for depression and suicidality.
Self-check
- What psychiatric risk follows loss of central endocannabinoid tone with CB1 blockade?
Depression or suicidality. - What weight effect accompanies CB1 blockade?
Weight loss.
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