Rivanicline

Drugbox
IUPAC_name = (E)-N-Methyl-4-(3-pyridinyl)-3-butene-1-amine


width= 240
CAS_number= 538-79-4
ATC_prefix=
ATC_suffix=
PubChem= 5310967
DrugBank=
C=10 | H=14 | N=2
molecular_weight = 162.232
smiles = CNCCC=CC1=CN=CC=C1
bioavailability=
metabolism =
elimination_half-life=
excretion =
pregnancy_category =
legal_status =
routes_of_administration=

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, [Jang J, Sin KS, Park H. Synthesis of (+/-)-methyl-(1-aryl-4-pyridin-3-yl-but-3-enyl)-amines. "Archives of Pharmacal Research". 2001 Dec;24(6):503-7. PMID 11794523] [Sapronov NS, Fedotova YO, Kuznetsova NN. Antiamnestic effect of alpha7-nicotinic receptor agonist RJR-2403 in middle-aged ovariectomized rats with Alzheimer type dementia. "Bulletin of Experimental Biology and Medicine". 2006 Dec;142(6):700-2. PMID 17603674] 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. [Spoettl T, Paetzel C, Herfarth H, Bencherif M, Schoelmerich J, Greinwald R, Gatto GJ, Rogler G. (E)-metanicotine hemigalactarate (TC-2403-12) inhibits IL-8 production in cells of the inflamed mucosa. "International Journal of Colorectal Disease". 2007 Mar;22(3):303-12. PMID 16715250] Rivanicline also has stimulant and analgesic actions which are thought to be mediated through stimulation of noradrenaline release, [Li X, Eisenach JC. Nicotinic acetylcholine receptor regulation of spinal norepinephrine release. "Anesthesiology". 2002 Jun;96(6):1450-6. PMID 12170059] and so it could potentially also have other applications.

References


Wikimedia Foundation. 2010.

Look at other dictionaries:

  • Phencyclidine — Systematic (IUPAC) name …   Wikipedia

  • Nicotine — This article is about the chemical compound. For other uses, see Nicotine (disambiguation). Nicotine Systematic (IUPAC) name …   Wikipedia

  • Aminorex — Systematic (IUPAC) name (RS) 5 phenyl 4,5 dihydro 1,3 oxazol 2 amine Clinical data Pregnancy cat.  …   Wikipedia

  • Benzydamine — Systematic (IUPAC) name 3 (1 benzyl 1H indazol 3 yloxy) N,N dimethylpropan 1 amine Clinical data AHFS/ …   Wikipedia

  • Cytisine — Not to be confused with cytosine, cysteine, or cystine. Cytisine IUPAC name …   Wikipedia

  • Varenicline — Systematic (IUPAC) name 7,8,9,10 tetrahydro 6,10 methano 6H pyrazino (2,3 h)(3) benzazepine Clinical data Trade names …   Wikipedia

  • Diphenylpyraline — Systematic (IUPAC) name 4 benzhydryloxy 1 methyl piperidine Clinical data AHFS/Drugs.com …   Wikipedia

  • Nicotinic agonist — A nicotinic agonist is a drug which enhances the action at the nicotinic acetylcholine receptor (nAChR). Examples include: nicotine (by definition the nicotinic acetylcholine receptor is named for its affinity for nicotine) acetylcholine, the… …   Wikipedia

  • Cyprodenate — Systematic (IUPAC) name 2 dimethylaminoethyl 3 cyclohexylpropanoate Clinical data AHFS/Drugs.com …   Wikipedia

  • Dianicline — Systematic (IUPAC) name (5aS,8S,10aR) 5a,6,9,10 Tetrahydro,7H,11H 8,10a methanopyrido[2 ,3 :5,6]pyrano[2,3 d]azepine Clinical data Pregnancy cat …   Wikipedia


Share the article and excerpts

Direct link
Do a right-click on the link above
and select “Copy Link”

We are using cookies for the best presentation of our site. Continuing to use this site, you agree with this.