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Items: 1 to 20 of 239

1.

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.

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.

PMID:
15887955
3.

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.

PMID:
17157884
4.

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.

5.

Ligands selective for alpha4beta2 but not alpha3beta4 or alpha7 nicotinic receptors generalise to the nicotine discriminative stimulus in the rat.

Smith JW, Mogg A, Tafi E, Peacey E, Pullar IA, Szekeres P, Tricklebank M.

Psychopharmacology (Berl). 2007 Feb;190(2):157-70. Epub 2006 Nov 18.

PMID:
17115136
6.

The alpha4beta2 nicotinic acetylcholine-receptor partial agonist varenicline inhibits both nicotine self-administration following repeated dosing and reinstatement of nicotine seeking in rats.

O'Connor EC, Parker D, Rollema H, Mead AN.

Psychopharmacology (Berl). 2010 Feb;208(3):365-76. doi: 10.1007/s00213-009-1739-5. Epub 2009 Dec 5.

PMID:
19967529
7.

Molecular dissection of tropisetron, an alpha7 nicotinic acetylcholine receptor-selective partial agonist.

Papke RL, Schiff HC, Jack BA, Horenstein NA.

Neurosci Lett. 2005 Apr 22;378(3):140-4. Epub 2005 Jan 5.

PMID:
15781147
8.

The nicotinic alpha 4 beta 2 receptor selective agonist, TC-2559, increases dopamine neuronal activity in the ventral tegmental area of rat midbrain slices.

Chen Y, Sharples TJ, Phillips KG, Benedetti G, Broad LM, Zwart R, Sher E.

Neuropharmacology. 2003 Sep;45(3):334-44.

PMID:
12871651
9.

An unusual pattern of ligand-receptor interactions for the α7 nicotinic acetylcholine receptor, with implications for the binding of varenicline.

Van Arnam EB, Blythe EE, Lester HA, Dougherty DA.

Mol Pharmacol. 2013 Aug;84(2):201-7. doi: 10.1124/mol.113.085795. Epub 2013 May 16.

10.

Diverse actions of neonicotinoids on chicken alpha7, alpha4beta2 and Drosophila-chicken SADbeta2 and ALSbeta2 hybrid nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes.

Ihara M, Matsuda K, Otake M, Kuwamura M, Shimomura M, Komai K, Akamatsu M, Raymond V, Sattelle DB.

Neuropharmacology. 2003 Jul;45(1):133-44.

PMID:
12814666
12.
13.

Rationale, pharmacology and clinical efficacy of partial agonists of alpha4beta2 nACh receptors for smoking cessation.

Rollema H, Coe JW, Chambers LK, Hurst RS, Stahl SM, Williams KE.

Trends Pharmacol Sci. 2007 Jul;28(7):316-25. Epub 2007 Jun 18. Review.

PMID:
17573127
14.

Effects of the alpha4beta2 partial agonist varenicline on brain activity and working memory in abstinent smokers.

Loughead J, Ray R, Wileyto EP, Ruparel K, Sanborn P, Siegel S, Gur RC, Lerman C.

Biol Psychiatry. 2010 Apr 15;67(8):715-21. doi: 10.1016/j.biopsych.2010.01.016. Epub 2010 Mar 6.

PMID:
20207347
15.

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.

16.

The high-affinity nAChR partial agonists varenicline and sazetidine-A exhibit reinforcing properties in rats.

Paterson NE, Min W, Hackett A, Lowe D, Hanania T, Caldarone B, Ghavami A.

Prog Neuropsychopharmacol Biol Psychiatry. 2010 Dec 1;34(8):1455-64. doi: 10.1016/j.pnpbp.2010.07.037. Epub 2010 Aug 11.

PMID:
20708056
17.

Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, selectively decreases ethanol consumption and seeking.

Steensland P, Simms JA, Holgate J, Richards JK, Bartlett SE.

Proc Natl Acad Sci U S A. 2007 Jul 24;104(30):12518-23. Epub 2007 Jul 11.

18.

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.

19.

JN403, in vitro characterization of a novel nicotinic acetylcholine receptor alpha7 selective agonist.

Feuerbach D, Nozulak J, Lingenhoehl K, McAllister K, Hoyer D.

Neurosci Lett. 2007 Apr 6;416(1):61-5. Epub 2007 Jan 25.

PMID:
17314009
20.

Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro.

Obach RS, Reed-Hagen AE, Krueger SS, Obach BJ, O'Connell TN, Zandi KS, Miller S, Coe JW.

Drug Metab Dispos. 2006 Jan;34(1):121-30. Epub 2005 Oct 12.

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