Dianicline

Chemical compound
  • none
Identifiers
  • (5aS,8S,10aR)-5a,6,9,10-Tetrahydro,7H,11H-8,10a-methanopyrido[2',3':5,6]pyrano[2,3-d]azepine
CAS Number
  • 292634-27-6 checkY
PubChem CID
  • 9816447
ChemSpider
  • 8352269 ☒N
UNII
  • Y0SNM34C6O
ChEMBL
  • ChEMBL187927 ☒N
Chemical and physical dataFormulaC13H16N2OMolar mass216.284 g·mol−13D model (JSmol)
  • Interactive image
  • C1CN2CC[C@@]3(C2)[C@H]1OC4=C(C3)N=CC=C4
InChI
  • InChI=1S/C13H16N2O/c1-2-11-10(14-5-1)8-13-4-7-15(9-13)6-3-12(13)16-11/h1-2,5,12H,3-4,6-9H2/t12-,13+/m0/s1 ☒N
  • Key:SUPRUPHAEXPGPF-QWHCGFSZSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Dianicline (SSR-591,813) is a drug developed by Sanofi-Aventis which acts as a partial agonist at neural nicotinic acetylcholine receptors. It is subtype-selective, binding primarily to the α4β2 subtype. It is being developed as a medication for the treatment of nicotine dependence to assist in smoking cessation.[1] Dianicline is very similar to the already marketed drug varenicline and it is unclear what advantages it will have over the older drug, although it may have an improved side effect profile. It has been through human trials up to Phase II, although results have not yet been reported. Drug development has been discontinued after reporting of unfavourable results during Phase III trials.[2][3][4]

References

  1. ^ Cohen C, Bergis OE, Galli F, Lochead AW, Jegham S, Biton B, et al. (July 2003). "SSR591813, a novel selective and partial alpha4beta2 nicotinic receptor agonist with potential as an aid to smoking cessation". The Journal of Pharmacology and Experimental Therapeutics. 306 (1): 407–20. doi:10.1124/jpet.103.049262. PMID 12682217. S2CID 37543790.
  2. ^ Fagerström K, Balfour DJK. Neuropharmacology and potential efficacy of new treatments for tobacco dependence. Expert Opinion on Investigational Drugs. 2006; 15(2):107-116.
  3. ^ Efficacy and Safety of Dianicline Versus Placebo as an Aid to Smoking Cessation
  4. ^ "Sanofi Pipeline" (PDF). Archived from the original (PDF) on 2008-12-04. Retrieved 2009-06-24.
  • v
  • t
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Stimulants
AdamantanesAdenosine antagonistsAlkylaminesAmpakinesArylcyclohexylaminesBenzazepinesCathinonesCholinergicsConvulsantsEugeroicsOxazolinesPhenethylamines
PhenylmorpholinesPiperazinesPiperidinesPyrrolidinesRacetamsTropanesTryptaminesOthers
  • v
  • t
  • e
Treatment of drug dependence (N07B)
Nicotine dependence
Alcohol dependence
Opioid dependence
Benzodiazepine dependence
  • v
  • t
  • e
nAChRsTooltip Nicotinic acetylcholine receptors
Agonists
(and PAMsTooltip positive allosteric modulators)
Antagonists
(and NAMsTooltip negative allosteric modulators)
Precursors
(and prodrugs)
See also
Receptor/signaling modulators
Muscarinic acetylcholine receptor modulators
Acetylcholine metabolism/transport modulators