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Structural characterization of binding mode of smoking cessation drugs to nicotinic acetylcholine receptors through study of ligand complexes with acetylcholine-binding protein.

Rucktooa P, Haseler CA, van Elk R, Smit AB, Gallagher T, Sixma TK.

J Biol Chem. 2012 Jul 6;287(28):23283-93. doi: 10.1074/jbc.M112.360347. Epub 2012 May 2.


Differential modulation of brain nicotinic acetylcholine receptor function by cytisine, varenicline, and two novel bispidine compounds: emergent properties of a hybrid molecule.

Peng C, Stokes C, Mineur YS, Picciotto MR, Tian C, Eibl C, Tomassoli I, Guendisch D, Papke RL.

J Pharmacol Exp Ther. 2013 Nov;347(2):424-37. doi: 10.1124/jpet.113.206904. Epub 2013 Aug 19.


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

Sala M, Braida D, Pucci L, Manfredi I, Marks MJ, Wageman CR, Grady SR, Loi B, Fucile S, Fasoli F, Zoli M, Tasso B, Sparatore F, Clementi F, Gotti C.

Br J Pharmacol. 2013 Feb;168(4):835-49. doi: 10.1111/j.1476-5381.2012.02204.x.


In silico characterization of cytisinoids docked into an acetylcholine binding protein.

Abin-Carriquiry JA, Zunini MP, Cassels BK, Wonnacott S, Dajas F.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3683-7. doi: 10.1016/j.bmcl.2010.04.092. Epub 2010 May 6.


Synthesis, binding, and modeling studies of new cytisine derivatives, as ligands for neuronal nicotinic acetylcholine receptor subtypes.

Tasso B, Canu Boido C, Terranova E, Gotti C, Riganti L, Clementi F, Artali R, Bombieri G, Meneghetti F, Sparatore F.

J Med Chem. 2009 Jul 23;52(14):4345-57. doi: 10.1021/jm900225j.


Pre-clinical properties of the alpha4beta2 nicotinic acetylcholine receptor partial agonists varenicline, cytisine and dianicline translate to clinical efficacy for nicotine dependence.

Rollema H, Shrikhande A, Ward KM, Tingley FD 3rd, Coe JW, O'Neill BT, Tseng E, Wang EQ, Mather RJ, Hurst RS, Williams KE, de Vries M, Cremers T, Bertrand S, Bertrand D.

Br J Pharmacol. 2010 May;160(2):334-45. doi: 10.1111/j.1476-5381.2010.00682.x. Epub 2010 Mar 22.


Structural and functional studies of the modulator NS9283 reveal agonist-like mechanism of action at α4β2 nicotinic acetylcholine receptors.

Olsen JA, Ahring PK, Kastrup JS, Gajhede M, Balle T.

J Biol Chem. 2014 Sep 5;289(36):24911-21. doi: 10.1074/jbc.M114.568097. Epub 2014 Jun 30.


Molecular actions of smoking cessation drugs at α4β2 nicotinic receptors defined in crystal structures of a homologous binding protein.

Billen B, Spurny R, Brams M, van Elk R, Valera-Kummer S, Yakel JL, Voets T, Bertrand D, Smit AB, Ulens C.

Proc Natl Acad Sci U S A. 2012 Jun 5;109(23):9173-8. doi: 10.1073/pnas.1116397109. Epub 2012 May 22.


7-Azaindole derivatives as potential partial nicotinic agonists.

Stoit AR, den Hartog AP, Mons H, van Schaik S, Barkhuijsen N, Stroomer C, Coolen HK, Reinders JH, Adolfs TJ, van der Neut M, Keizer H, Kruse CG.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):188-93. Epub 2007 Nov 1.


Pharmacological and molecular studies on the interaction of varenicline with different nicotinic acetylcholine receptor subtypes. Potential mechanism underlying partial agonism at human α4β2 and α3β4 subtypes.

Arias HR, Feuerbach D, Targowska-Duda K, Kaczor AA, Poso A, Jozwiak K.

Biochim Biophys Acta. 2015 Feb;1848(2):731-41. doi: 10.1016/j.bbamem.2014.11.003. Epub 2014 Dec 2.


Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation.

Coe JW, Brooks PR, Vetelino MG, Wirtz MC, Arnold EP, Huang J, Sands SB, Davis TI, Lebel LA, Fox CB, Shrikhande A, Heym JH, Schaeffer E, Rollema H, Lu Y, Mansbach RS, Chambers LK, Rovetti CC, Schulz DW, Tingley FD 3rd, O'Neill BT.

J Med Chem. 2005 May 19;48(10):3474-7.


C3-halogenation of cytisine generates potent and efficacious nicotinic receptor agonists.

Abin-Carriquiry JA, Voutilainen MH, Barik J, Cassels BK, Iturriaga-Vásquez P, Bermudez I, Durand C, Dajas F, Wonnacott S.

Eur J Pharmacol. 2006 Apr 24;536(1-2):1-11. Epub 2006 Mar 6.


Nicotinic receptor antagonists as treatments for nicotine abuse.

Crooks PA, Bardo MT, Dwoskin LP.

Adv Pharmacol. 2014;69:513-51. doi: 10.1016/B978-0-12-420118-7.00013-5. Review.


Impact of genetic variability in nicotinic acetylcholine receptors on nicotine addiction and smoking cessation treatment.

Russo P, Cesario A, Rutella S, Veronesi G, Spaggiari L, Galetta D, Margaritora S, Granone P, Greenberg DS.

Curr Med Chem. 2011;18(1):91-112. Review.


Ligand specificity of nicotinic acetylcholine receptors in rat spinal cord: studies with nicotine and cytisine.

Khan IM, Yaksh TL, Taylor P.

J Pharmacol Exp Ther. 1994 Jul;270(1):159-66.


Nicotinic receptor partial agonists as novel compounds for the treatment of smoking cessation.

Tutka P.

Expert Opin Investig Drugs. 2008 Oct;17(10):1473-85. doi: 10.1517/13543784.17.10.1473 . Review.


Pharmacological profile of the alpha4beta2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid.

Rollema H, Chambers LK, Coe JW, Glowa J, Hurst RS, Lebel LA, Lu Y, Mansbach RS, Mather RJ, Rovetti CC, Sands SB, Schaeffer E, Schulz DW, Tingley FD 3rd, Williams KE.

Neuropharmacology. 2007 Mar;52(3):985-94. Epub 2006 Dec 8.


Molecular recognition of neonicotinoid insecticides: the determinants of life or death.

Tomizawa M, Casida JE.

Acc Chem Res. 2009 Feb 17;42(2):260-9. doi: 10.1021/ar800131p. Review.


Electrophysiological perspectives on the therapeutic use of nicotinic acetylcholine receptor partial agonists.

Papke RL, Trocmé-Thibierge C, Guendisch D, Al Rubaiy SA, Bloom SA.

J Pharmacol Exp Ther. 2011 May;337(2):367-79. doi: 10.1124/jpet.110.177485. Epub 2011 Feb 1.

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