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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.


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.


α4β2 nicotinic acetylcholine receptor partial agonists with low intrinsic efficacy have antidepressant-like properties.

Mineur YS, Einstein EB, Seymour PA, Coe JW, O'neill BT, Rollema H, Picciotto MR.

Behav Pharmacol. 2011 Aug;22(4):291-9. doi: 10.1097/FBP.0b013e328347546d.


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.


Dissociation between duration of action in the forced swim test in mice and nicotinic acetylcholine receptor occupancy with sazetidine, varenicline, and 5-I-A85380.

Caldarone BJ, Wang D, Paterson NE, Manzano M, Fedolak A, Cavino K, Kwan M, Hanania T, Chellappan SK, Kozikowski AP, Olivier B, Picciotto MR, Ghavami A.

Psychopharmacology (Berl). 2011 Sep;217(2):199-210. doi: 10.1007/s00213-011-2271-y.


Molecular determinants of subtype-selective efficacies of cytisine and the novel compound NS3861 at heteromeric nicotinic acetylcholine receptors.

Harpsøe K, Hald H, Timmermann DB, Jensen ML, Dyhring T, Nielsen EØ, Peters D, Balle T, Gajhede M, Kastrup JS, Ahring PK.

J Biol Chem. 2013 Jan 25;288(4):2559-70. doi: 10.1074/jbc.M112.436337.


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.


Antidepressant-like effects of nicotinic acetylcholine receptor antagonists, but not agonists, in the mouse forced swim and mouse tail suspension tests.

Andreasen JT, Olsen GM, Wiborg O, Redrobe JP.

J Psychopharmacol. 2009 Sep;23(7):797-804. doi: 10.1177/0269881108091587.


Role of neuronal nicotinic acetylcholine receptors (nAChRs) on learning and memory in zebrafish.

Braida D, Ponzoni L, Martucci R, Sparatore F, Gotti C, Sala M.

Psychopharmacology (Berl). 2014 May;231(9):1975-85. doi: 10.1007/s00213-013-3340-1.


Expression of the 5-HT1A serotonin receptor in the hippocampus is required for social stress resilience and the antidepressant-like effects induced by the nicotinic partial agonist cytisine.

Mineur YS, Einstein EB, Bentham MP, Wigestrand MB, Blakeman S, Newbold SA, Picciotto MR.

Neuropsychopharmacology. 2015 Mar;40(4):938-46. doi: 10.1038/npp.2014.269.


Nicotinic receptor partial agonists alter catecholamine homeostasis and response to nicotine in PC12 cells.

Turcanu DS, Kirtok N, Eibl C, Guendisch D, LaGamma EF, Nankova BB.

Neurosci Lett. 2012 May 16;516(2):212-6. doi: 10.1016/j.neulet.2012.03.088.


The nicotinic acetylcholine receptor as a target for antidepressant drug development.

Philip NS, Carpenter LL, Tyrka AR, Price LH.

ScientificWorldJournal. 2012;2012:104105. doi: 10.1100/2012/104105. Review.


In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.

Coe JW, Vetelino MG, Bashore CG, Wirtz MC, Brooks PR, Arnold EP, Lebel LA, Fox CB, Sands SB, Davis TI, Schulz DW, Rollema H, Tingley FD 3rd, O'Neill BT.

Bioorg Med Chem Lett. 2005 Jun 15;15(12):2974-9.


Varenicline and cytisine diminish the dysphoric-like state associated with spontaneous nicotine withdrawal in rats.

Igari M, Alexander JC, Ji Y, Qi X, Papke RL, Bruijnzeel AW.

Neuropsychopharmacology. 2014 Jan;39(2):455-65. doi: 10.1038/npp.2013.216.


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.


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.

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