CC4, a dimer of cytisine, is a selective partial agonist at α4β2/α6β2 nAChR with improved selectivity for tobacco smoking cessation

@article{Sala2013CC4AD,
  title={CC4, a dimer of cytisine, is a selective partial agonist at α4β2/α6β2 nAChR with improved selectivity for tobacco smoking cessation},
  author={M. Sala and D. Braida and Luca Pucci and I. Manfredi and M. Marks and C. R. Wageman and S. Grady and Barbara Loi and Sergio Fucile and F. Fasoli and M. Zoli and B. Tasso and F. Sparatore and F. Clementi and C. Gotti},
  journal={British Journal of Pharmacology},
  year={2013},
  volume={168}
}
  • M. Sala, D. Braida, +12 authors C. Gotti
  • Published 2013
  • Chemistry, Medicine
  • British Journal of Pharmacology
    • Many of the addictive and rewarding effects of nicotine are due to its actions on the neuronal nicotinic ACh receptor (nAChR) subtypes expressed in dopaminergic mesocorticolimbic cells. The partial agonists, cytisine and varenicline, are helpful smoking cessation aids. These drugs have a number of side effects that limit their usefulness. The aim of this study was to investigate the preclinical pharmacology of the cytisine dimer1,2‐bisN‐cytisinylethane (CC4). 
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    26 Citations
    Background Citations
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    Methods Citations
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    References

    SHOWING 1-10 OF 75 REFERENCES
    Pre‐clinical properties of the α4β2 nicotinic acetylcholine receptor partial agonists varenicline, cytisine and dianicline translate to clinical efficacy for nicotine dependence
    • 130
    Varenicline: An α4β2 Nicotinic Receptor Partial Agonist for Smoking Cessation
    • 753
    • Highly Influential
    • PDF
    Rationale, pharmacology and clinical efficacy of partial agonists of α4β2 nACh receptors for smoking cessation
    • 185
    • Highly Influential
    • PDF
    Varenicline Is a Partial Agonist at α4β2 and a Full Agonist at α7 Neuronal Nicotinic Receptors
    • 467
    • PDF
    Nicotinic receptor partial agonists as novel compounds for the treatment of smoking cessation.
    • P. Tutka
    • Medicine
    • Expert opinion on investigational drugs
    • 2008
    • 12
    Pharmacological profile of the α4β2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid
    • 456
    • Highly Influential
    Synthesis and preliminary pharmacological evaluation of some cytisine derivatives.
    • 69
    Cytisine derivatives as ligands for neuronal nicotine receptors and with various pharmacological activities.
    • 82
    Rationale, pharmacology and clinical efficacy of partial agonists of alpha4beta2 nACh receptors for smoking cessation.
    • 103
    • Highly Influential
    Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors.
    • 217