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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.


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.


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.


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.


The effects of nicotine, varenicline, and cytisine on schedule-controlled responding in mice: differences in α4β2 nicotinic receptor activation.

Cunningham CS, McMahon LR.

Eur J Pharmacol. 2011 Mar 1;654(1):47-52. doi: 10.1016/j.ejphar.2010.12.003. Epub 2010 Dec 21.


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 is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors.

Mihalak KB, Carroll FI, Luetje CW.

Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9.


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.


Activation and inhibition of mouse muscle and neuronal nicotinic acetylcholine receptors expressed in Xenopus oocytes.

Papke RL, Wecker L, Stitzel JA.

J Pharmacol Exp Ther. 2010 May;333(2):501-18. doi: 10.1124/jpet.109.164566. Epub 2010 Jan 25.


Cytisine-based nicotinic partial agonists as novel antidepressant compounds.

Mineur YS, Eibl C, Young G, Kochevar C, Papke RL, Gündisch D, Picciotto MR.

J Pharmacol Exp Ther. 2009 Apr;329(1):377-86. doi: 10.1124/jpet.108.149609. Epub 2009 Jan 22.


The contribution of α4β2 and non-α4β2 nicotinic acetylcholine receptors to the discriminative stimulus effects of nicotine and varenicline in mice.

de Moura FB, McMahon LR.

Psychopharmacology (Berl). 2017 Mar;234(5):781-792. doi: 10.1007/s00213-016-4514-4. Epub 2016 Dec 27.


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.


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.


Pharmacologic characterization of a nicotine-discriminative stimulus in rhesus monkeys.

Cunningham CS, Javors MA, McMahon LR.

J Pharmacol Exp Ther. 2012 Jun;341(3):840-9. doi: 10.1124/jpet.112.193078. Epub 2012 Mar 21.


Multiple nicotine training doses in mice as a basis for differentiating the effects of smoking cessation aids.

Cunningham CS, McMahon LR.

Psychopharmacology (Berl). 2013 Jul;228(2):321-33. doi: 10.1007/s00213-013-3037-5. Epub 2013 Mar 14.


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.


Long-term exposure to the new nicotinic antagonist 1,2-bisN-cytisinylethane upregulates nicotinic receptor subtypes of SH-SY5Y human neuroblastoma cells.

Riganti L, Matteoni C, Di Angelantonio S, Nistri A, Gaimarri A, Sparatore F, Canu-Boido C, Clementi F, Gotti C.

Br J Pharmacol. 2005 Dec;146(8):1096-109.


Varenicline and cytisine: two nicotinic acetylcholine receptor ligands reduce ethanol intake in University of Chile bibulous rats.

Sotomayor-Zárate R, Gysling K, Busto UE, Cassels BK, Tampier L, Quintanilla ME.

Psychopharmacology (Berl). 2013 May;227(2):287-98. doi: 10.1007/s00213-013-2974-3. Epub 2013 Jan 24.


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.

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