Mesulergine
Template:Short description Template:Drugbox
Mesulergine (INN) (developmental code name CU-32085) is a drug of the ergoline group which was never marketed.[1][2]
Pharmacology
Pharmacodynamics
| Target | Affinity (Ki, nM) | Species |
|---|---|---|
| 5-HT1A | 195–398 | Human |
| 5-HT1B | 631–1,288 | Human |
| 5-HT1D | 1,700–>10,000 | Human |
| 5-HT1E | ND | ND |
| 5-HT1F | >10,000 | Human |
| 5-HT2A | 19.5–151 | Human |
| 5-HT2B | 1.44–3.62 | Human |
| 5-HT2C | 1.12–48.5 | Human |
| 5-HT3 | >10,000 | Rat |
| 5-HT4 | ND | ND |
| 5-HT5A | 1,000 | Rat |
| 5-HT5B | 1,000 | Rat |
| 5-HT6 | 776–3,800 | Human |
| 5-HT7 | 7.9–31.6 | Human |
| D2 | 8–12 | Rat |
| Notes: The smaller the value, the more avidly the drug binds to the site. All proteins are human unless otherwise specified. Refs: [3][4][5][6] | ||
Mesulergine acts on serotonin and dopamine receptors.[7][8][9] Specifically, it is an agonist of dopamine D2-like receptors and serotonin 5-HT6 receptors and an antagonist of serotonin 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7 receptors.[9]Template:Additional citation needed It also has affinity for the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1F, and 5-HT5A receptors.[10][9]
Research
Mesulergine had entered clinical trials for the treatment of Parkinson's disease; however, further development was halted due to adverse histological abnormalities in rats.[11] It was also investigated for the treatment of hyperprolactinemia (high prolactin levels).[12]
See also
References
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- ↑ National Institute of Mental Health. PDSD Ki Database (Internet). ChapelHill (NC): University of North Carolina. Available from: Script error: No such module "citation/CS1".
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Template:Dopamine receptor modulators
Template:Serotonin receptor modulators
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