Review Article
Pharmacotherapies for Obesity: Past, Current, and Future Therapies
Table 2
Central mechanisms of action of anti-obesity pharmacotherapies.
| | Central Subsystem | Drugs targets | Possible receptor subtypes involved |
| | Monoamine system (indirect agonists and subtype selective receptor antagonists) | Single therapies | | | (i) Dex/fenfluramine (WD), fluoxetine | (i) 5HT | | (ii) Phentermine/Diethylpropion (ST) | (ii) DA, NA | | (iii) Sibutramine | (iii) α 1, β 1, β 3 adrenergic and 5HT2B/C | | (iv) Bupropion | (iv) DA, NA | | (v) Tesofensine | (v) DA, NA, 5HT | | (vi) Lorcaserin | (vi) 5HT2C |
| | Opioid system (μ-opioid receptor antagonist) | (i) Naltrexone | (i) μ-opioid | | (ii) Topiramate | (ii) AMPA/kainite glutamate* | | (iii) Zonisamide | (iii) 5HT, DA∗ |
| | Cannabinoid system | Single therapies: | | | (i) Rimonabant (WD) | (i) CB1 | | (ii) Taranabant (DC) | (ii) CB1 |
| | Monoamine/Opioid system | Bupropion/naltrexone | (i) DA, NA/μ-opioid | | Bupropion/zonisamide | (ii) DA, NA/5HT, DA∗ |
| | Neuropeptide Y/Agouti-related peptide system | Pramlintide/metreleptin | (i) Calcitonin receptor∗/Leptin receptor |
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5HT: serotonergic, DA: dopaminergic, NA: noradrenergic, WD:withdrawn; DC: phase III trials discontinued; ST: short term;∗: unknown; AMPA: α-amino-3-hydroxyl-5-methyl-4-isoxazole-propionate.
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