Display options
Cite
Singh J, Budhiraja S. Partial nicotinic acetylcholine (alpha4beta2) agonists as promising new medications for smoking cessation. Indian J Pharmacol. 2008;40(5):191-6doi: 10.4103/0253-7613.44150.
Singh, J., & Budhiraja, S. (2008). Partial nicotinic acetylcholine (alpha4beta2) agonists as promising new medications for smoking cessation. Indian journal of pharmacology, 40(5), 191-6. https://doi.org/10.4103/0253-7613.44150
Singh, J, and Budhiraja, Salil. "Partial nicotinic acetylcholine (alpha4beta2) agonists as promising new medications for smoking cessation." Indian journal of pharmacology vol. 40,5 (2008): 191-6. doi: https://doi.org/10.4103/0253-7613.44150
Singh J, Budhiraja S. Partial nicotinic acetylcholine (alpha4beta2) agonists as promising new medications for smoking cessation. Indian J Pharmacol. 2008 Oct;40(5):191-6. doi: 10.4103/0253-7613.44150. PMID: 20040957; PMCID: PMC2792622.
Copy Download .nbib Format: NLM
Share it on

Indian J Pharmacol. 2008 Oct;40(5):191-6. doi: 10.4103/0253-7613.44150.

Partial nicotinic acetylcholine (alpha4beta2) agonists as promising new medications for smoking cessation.

Indian journal of pharmacology

J Singh, Salil Budhiraja

Affiliations

  1. Department of Pharmacology, Pt. B. D. Sharma PGIMS, Haryana, India.

PMID: 20040957 PMCID: PMC2792622 DOI: 10.4103/0253-7613.44150

Abstract

OBJECTIVE: To review the pharmacology, clinical efficacy and safety of partial agonists of alpha4beta2 nicotinic acetylcholine receptor.

DATA SOURCES: Primary literature and review articles were obtained via a PUBMED search (1988-August 2006) using the key terms smoking cessation, partial agonist alpha4beta2 nicotinic acetylcholine receptor, varenicline, cytisine and SSR591813. Additional studies and abstracts were identified from the bibliographies of reviewed literature.

STUDY SELECTION AND DATA EXTRACTION: Studies and review articles related to varenicline, cytisine and the partial agonist alpha4beta2 nicotinic acetylcholine receptor were reviewed.

DATA SYNTHESIS: Smoking is widely recognized as a serious health problem. Smoking cessation has major health benefits. According to the US Public Health Services, all patients attempting to quit smoking should be encouraged to use one or more effective pharmacotherapy. Currently, along with nicotine replacement therapy, bupropion, nortriptyline and clonidine, are the mainstay of pharmacotherapy. More than (3/4) of patients receiving treatment for smoking cessation return to smoking within the first year. Nicotine, through stimulating alpha4beta2 nAChR, releases dopamine in the reward pathway. Partial agonist of alpha4beta2 nAChR elicits moderate and sustained release of dopamine, which is countered during the cessation attempts; it simultaneously blocks the effects of nicotine by binding with alpha4beta2 receptors during smoking. Recently, varenicline, a partial agonist at alpha4beta2 nAChR, has been approved by the FDA (Food and Drug Administration) for smoking cessation.

CONCLUSION: Partial agonist alpha4beta2 nAChR appears to be a promising target in smoking cessation. Varenicline of this group is approved for treatment of smoking cessation by the FDA in May 2006.

Keywords: Cytisine; SSR591813; partial agonist α4β2 nAChR; smoking cessation; varenicline

References

  1. Int J Clin Pract. 2006 May;60(5):571-6 - PubMed
  2. Bioorg Med Chem Lett. 2005 Jun 15;15(12):2974-9 - PubMed
  3. Trends Neurosci. 2003 Apr;26(4):184-92 - PubMed
  4. Proc Natl Acad Sci U S A. 1988 Jul;85(14):5274-8 - PubMed
  5. BMC Public Health. 2006 Dec 11;6:300 - PubMed
  6. Trends Pharmacol Sci. 2002 Mar;23(3):130-6 - PubMed
  7. JAMA. 2006 Jul 5;296(1):56-63 - PubMed
  8. JAMA. 2006 Jul 5;296(1):47-55 - PubMed
  9. Neuron. 2006 Jun 15;50(6):911-21 - PubMed
  10. Psychopharmacology (Berl). 1994 Jan;113(3-4):445-52 - PubMed
  11. Behav Pharmacol. 1999 Nov;10(6-7):559-80 - PubMed
  12. Behav Pharmacol. 2002 Sep;13(5-6):451-63 - PubMed
  13. Pharmacol Biochem Behav. 2001 Dec;70(4):551-9 - PubMed
  14. J Psychiatr Res. 2006 Aug;40(5):404-18 - PubMed
  15. JAMA. 2006 Jul 5;296(1):64-71 - PubMed
  16. J Med Chem. 2005 May 19;48(10):3474-7 - PubMed
  17. Arch Intern Med. 2006 Aug 14-28;166(15):1561-8 - PubMed
  18. J Neurobiol. 2002 Dec;53(4):606-17 - PubMed
  19. Psychopharmacology (Berl). 1992;107(2-3):285-9 - PubMed
  20. Br J Pharmacol. 2006 Feb;147(4):379-90 - PubMed
  21. Clin Ther. 2007 Jun;29(6):1040-56 - PubMed
  22. Mol Pharmacol. 1994 Jan;45(1):142-9 - PubMed
  23. J Am Chem Soc. 1948 Oct;70(10):3472-4 - PubMed
  24. Lancet. 2003 Sep 13;362(9387):847-52 - PubMed
  25. Methods Enzymol. 1992;207:319-39 - PubMed
  26. Drug Alcohol Rev. 2006 Jan;25(1):59-71 - PubMed
  27. Neuropsychopharmacology. 1992 Aug;7(1):7-14 - PubMed
  28. FDA Consum. 2006 Jul-Aug;40(4):29 - PubMed
  29. Arch Intern Med. 2006 Aug 14-28;166(15):1571-7 - PubMed
  30. Addiction. 1994 Nov;89(11):1461-70 - PubMed
  31. Pharmacol Rep. 2006 Nov-Dec;58(6):777-98 - PubMed
  32. J Pharmacol Exp Ther. 2003 Jul;306(1):407-20 - PubMed
  33. Drug Discov Today. 2003 Nov 15;8(22):1025-34 - PubMed
  34. Clin Ther. 2007 Jun;29(6):1027-39 - PubMed
  35. Drug Metab Dispos. 2006 Jan;34(1):121-30 - PubMed
  36. Pharmacol Biochem Behav. 1999 Apr;62(4):743-51 - PubMed
  37. J Pharmacol Exp Ther. 2006 Jul;318(1):381-8 - PubMed
  38. Nature. 1998 Jan 8;391(6663):173-7 - PubMed
  39. J Mol Neurosci. 2006;30(1-2):181-4 - PubMed
  40. Biol Psychiatry. 2006 Jun 1;59(11):1065-70 - PubMed
  41. Jpn J Pharmacol. 2002 Feb;88(2):133-8 - PubMed
  42. J Pharmacol Exp Ther. 1997 Nov;283(2):566-73 - PubMed
  43. Curr Med Res Opin. 2007 Apr;23(4):793-801 - PubMed
  44. Clin Pharmacol Ther. 1994 Jul;56(1):86-99 - PubMed
  45. Neuropharmacology. 2007 Mar;52(3):985-94 - PubMed
  46. J Neurosci. 2000 Oct 15;20(20):RC102 - PubMed

Publication Types