Rivanicline (TC-2403, RJR-2403, (E)-metanicotine) is a drug which acts as a
partial agonist at neural
nicotinic acetylcholine receptors. It is subtype-selective, binding primarily to the
α4β2subtype. It has
nootropic effects and was originally developed as a potential treatment for
Alzheimer's disease,[1][2][3] but a second action that was subsequently found was that it inhibits the production of
Interleukin-8 and thus produces an
antiinflammatory effect, and so it has also been developed as a potential treatment for
ulcerative colitis.[4] Rivanicline also has
stimulant and
analgesic actions which are thought to be mediated through stimulation of
noradrenaline release,[5] and so it could also have other applications. It has been identified as constituent of tobacco as well.[6][7]
^Jang J, Sin KS, Park H (December 2001). "Synthesis of (+/-)-methyl-(1-aryl-4-pyridin-3-yl-but-3-enyl)-amines". Archives of Pharmacal Research. 24 (6): 503–7.
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10.1007/bf02975153.
PMID11794523.
S2CID19502452.
^Sapronov NS, Fedotova YO, Kuznetsova NN (December 2006). "Antiamnestic effect of alpha7-nicotinic receptor agonist RJR-2403 in middle-aged ovariectomized rats with Alzheimer type dementia". Bulletin of Experimental Biology and Medicine. 142 (6): 700–2.
doi:
10.1007/s10517-006-0455-y.
PMID17603674.
S2CID7186817.
^Spoettl T, Paetzel C, Herfarth H, Bencherif M, Schoelmerich J, Greinwald R, et al. (March 2007). "(E)-metanicotine hemigalactarate (TC-2403-12) inhibits IL-8 production in cells of the inflamed mucosa". International Journal of Colorectal Disease. 22 (3): 303–12.
doi:
10.1007/s00384-006-0135-4.
PMID16715250.
S2CID11135872.
^Stedman RL (April 1968). "The chemical composition of tobacco and tobacco smoke". Chemical Reviews. 68 (2). American Chemical Society (ACS): 153–207.
doi:
10.1021/cr60252a002.
PMID4868017.