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Draft:RG3487

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Chemical structure of RG3487

RG3487 is a selective α7 nicotinic acetylcholine receptor partial agonist and antagonist to serotonin-3 receptors (5HT3). It demonstrated initial efficacy in a proof-of-concept phase I trial in 80 Alzheimer's patients but its development was later discontinued following the conclusion of a later phase II trial without published results.[1] A later study evaluating the effects of RG3487 on cognitive deficits associated with schizophrenia failed to find an effect, although post-hoc analysis revealed improvements in patients with high negative PANSS scores.[1]

Pharmacology

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RG3487 is a combined a7 nicotinic agonist and 5HT3 antagonist, a trait it shares with tropesitron.[2]



References

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  1. ^ a b "RG3487 | ALZFORUM". www.alzforum.org. Retrieved 2023-12-23.
  2. ^ Terry Jr., Alvin V.; Callahan, Patrick M.; Hernandez, Caterina M. (2015-10-15). "Nicotinic ligands as multifunctional agents for the treatment of neuropsychiatric disorders". Biochemical Pharmacology. Nicotinic Acetylcholine Receptors as Therapeutic Targets: Emerging Frontiers in Basic Research and Clinical Science (Satellite to the 2015 Meeting of the Society for Neuroscience) Oct 14-15, Chicago, IL USA. 97 (4): 388–398. doi:10.1016/j.bcp.2015.07.027. ISSN 0006-2952.