Facinicline
Discontinued drug for Alzheimer's Disease and Schizophrenia
From Wikipedia, the free encyclopedia
Facinicline (development code RG3487) is a α7 nicotinic acetylcholine receptor partial agonist and antagonist to serotonin-3 receptors (5-HT3). It demonstrated initial efficacy for treating cognitive impairment in Alzheimer's disease in a phase 2a trial, but development was discontinued following the conclusion of a later phase 2 trial.[1]
| Names | |
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| IUPAC name
N-[(3S)-1-Azabicyclo[2.2.2]octan-3-yl]-1H-indazole-3-carboxamide | |
| Other names
RG3487 | |
| Identifiers | |
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| Properties | |
| C15H18N4O | |
| Molar mass | 270.336 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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A later study evaluating the effects of facinicline on cognitive deficits in schizophrenia failed to demonstrate an effect on its primary endpoints, although post-hoc analysis showed improvements in patients with high negative PANSS scores.[1][2]
Pharmacology
Facinicline is an a7 nicotinic partial agonist and 5-HT3 antagonist.[3][4] Facinicline shares much of its structure with tropesitron, another α7 and 5HT3 agonist/antagonist.
