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]

Quick facts Names, Identifiers ...
Facinicline
Names
IUPAC name
N-[(3S)-1-Azabicyclo[2.2.2]octan-3-yl]-1H-indazole-3-carboxamide
Other names
RG3487
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
UNII
  • InChI=1S/C15H18N4O/c20-15(14-11-3-1-2-4-12(11)17-18-14)16-13-9-19-7-5-10(13)6-8-19/h1-4,10,13H,5-9H2,(H,16,20)(H,17,18)/t13-/m1/s1
    Key: TXCYUSKWBHUVEP-CYBMUJFWSA-N
  • C1CN2CCC1[C@@H](C2)NC(=O)C3=NNC4=CC=CC=C43
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).
Close

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.

References

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