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Rivanicline

Rivanicline
Skeletal formula
Ball-and-stick model of rivanicline
Clinical data
ATC code
  • none
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
Chemical and physical data
FormulaC10H14N2
Molar mass162.232 g·mol−1
3D model (JSmol)
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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 α4β2 subtype. It has nootropic effects and was originally developed as a potential treatment for Alzheimer's disease,[1][2] 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.[3] Rivanicline also has stimulant and analgesic actions which are thought to be mediated through stimulation of noradrenaline release,[4] and so it could also have other applications.

References

  1. ^ 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. doi:10.1007/bf02975153. PMID 11794523.
  2. ^ 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. PMID 17603674.
  3. ^ 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. PMID 16715250.
  4. ^ Li X, Eisenach JC (June 2002). "Nicotinic acetylcholine receptor regulation of spinal norepinephrine release". Anesthesiology. 96 (6): 1450–6. doi:10.1097/00000542-200206000-00026. PMID 12170059.