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Computational neural network analysis of the affinity of lobeline and tetrabenazine analogs for the vesicular monoamine transporter-2.

Zheng F, Zheng G, Deaciuc AG, Zhan CG, Dwoskin LP, Crooks PA.

Bioorg Med Chem. 2007 Apr 15;15(8):2975-92. Epub 2007 Feb 11.


Design, synthesis and interaction at the vesicular monoamine transporter-2 of lobeline analogs: potential pharmacotherapies for the treatment of psychostimulant abuse.

Crooks PA, Zheng G, Vartak AP, Culver JP, Zheng F, Horton DB, Dwoskin LP.

Curr Top Med Chem. 2011;11(9):1103-27. Review.


Pyrrolidine analogues of lobelane: relationship of affinity for the dihydrotetrabenazine binding site with function of the vesicular monoamine transporter 2 (VMAT2).

Vartak AP, Nickell JR, Chagkutip J, Dwoskin LP, Crooks PA.

J Med Chem. 2009 Dec 10;52(23):7878-82. doi: 10.1021/jm900770h.


Pyrrolidine analogs of GZ-793A: synthesis and evaluation as inhibitors of the vesicular monoamine transporter-2 (VMAT2).

Penthala NR, Ponugoti PR, Nickell JR, Deaciuc AG, Dwoskin LP, Crooks PA.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3342-5. doi: 10.1016/j.bmcl.2013.03.092. Epub 2013 Apr 2.


Defunctionalized lobeline analogues: structure-activity of novel ligands for the vesicular monoamine transporter.

Zheng G, Dwoskin LP, Deaciuc AG, Norrholm SD, Crooks PA.

J Med Chem. 2005 Aug 25;48(17):5551-60.


Synthesis and biological evaluation of 3-alkyl-dihydrotetrabenazine derivatives as vesicular monoamine transporter-2 (VMAT2) ligands.

Zheng P, Lieberman BP, Choi SR, Plöessl K, Kung HF.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3435-8. doi: 10.1016/j.bmcl.2011.03.113. Epub 2011 Apr 5.


Vesicular monoamine transporter 2: role as a novel target for drug development.

Zheng G, Dwoskin LP, Crooks PA.

AAPS J. 2006 Nov 10;8(4):E682-92. Review.


Phenyl ring-substituted lobelane analogs: inhibition of [³H]dopamine uptake at the vesicular monoamine transporter-2.

Nickell JR, Zheng G, Deaciuc AG, Crooks PA, Dwoskin LP.

J Pharmacol Exp Ther. 2011 Mar;336(3):724-33. doi: 10.1124/jpet.110.172882. Epub 2010 Sep 28.


Lobelane inhibits methamphetamine-evoked dopamine release via inhibition of the vesicular monoamine transporter-2.

Nickell JR, Krishnamurthy S, Norrholm S, Deaciuc G, Siripurapu KB, Zheng G, Crooks PA, Dwoskin LP.

J Pharmacol Exp Ther. 2010 Feb;332(2):612-21. doi: 10.1124/jpet.109.160275. Epub 2009 Oct 23.


Lobeline analogs with enhanced affinity and selectivity for plasmalemma and vesicular monoamine transporters.

Miller DK, Crooks PA, Zheng G, Grinevich VP, Norrholm SD, Dwoskin LP.

J Pharmacol Exp Ther. 2004 Sep;310(3):1035-45. Epub 2004 Apr 30.


The vesicular monoamine transporter-2: an important pharmacological target for the discovery of novel therapeutics to treat methamphetamine abuse.

Nickell JR, Siripurapu KB, Vartak A, Crooks PA, Dwoskin LP.

Adv Pharmacol. 2014;69:71-106. doi: 10.1016/B978-0-12-420118-7.00002-0. Review.


The novel pyrrolidine nor-lobelane analog UKCP-110 [cis-2,5-di-(2-phenethyl)-pyrrolidine hydrochloride] inhibits VMAT2 function, methamphetamine-evoked dopamine release, and methamphetamine self-administration in rats.

Beckmann JS, Siripurapu KB, Nickell JR, Horton DB, Denehy ED, Vartak A, Crooks PA, Dwoskin LP, Bardo MT.

J Pharmacol Exp Ther. 2010 Dec;335(3):841-51. doi: 10.1124/jpet.110.172742. Epub 2010 Aug 30.


Novel N-1,2-dihydroxypropyl analogs of lobelane inhibit vesicular monoamine transporter-2 function and methamphetamine-evoked dopamine release.

Horton DB, Siripurapu KB, Zheng G, Crooks PA, Dwoskin LP.

J Pharmacol Exp Ther. 2011 Oct;339(1):286-97. doi: 10.1124/jpet.111.184770. Epub 2011 Jul 21.


Improving the inhibitory activity of arylidenaminoguanidine compounds at the N-methyl-D-aspartate receptor complex from a recursive computational-experimental structure-activity relationship study.

Ring JR, Zheng F, Haubner AJ, Littleton JM, Crooks PA.

Bioorg Med Chem. 2013 Apr 1;21(7):1764-74. doi: 10.1016/j.bmc.2013.01.051. Epub 2013 Jan 31.


GZ-793A, a lobelane analog, interacts with the vesicular monoamine transporter-2 to inhibit the effect of methamphetamine.

Horton DB, Nickell JR, Zheng G, Crooks PA, Dwoskin LP.

J Neurochem. 2013 Oct;127(2):177-86. doi: 10.1111/jnc.12371. Epub 2013 Aug 19.


Lobeline esters as novel ligands for neuronal nicotinic acetylcholine receptors and neurotransmitter transporters.

Hojahmat M, Horton DB, Norrholm SD, Miller DK, Grinevich VP, Deaciuc AG, Dwoskin LP, Crooks PA.

Bioorg Med Chem. 2010 Jan 15;18(2):640-9. doi: 10.1016/j.bmc.2009.12.002. Epub 2009 Dec 6.


Synthesis and evaluation of 2-amino-dihydrotetrabenzine derivatives as probes for imaging vesicular monoamine transporter-2.

Zhu L, Liu J, Kung HF.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5026-8. doi: 10.1016/j.bmcl.2009.07.048. Epub 2009 Jul 24.


Predictive QSAR modeling of HIV reverse transcriptase inhibitor TIBO derivatives.

Mandal AS, Roy K.

Eur J Med Chem. 2009 Apr;44(4):1509-24. doi: 10.1016/j.ejmech.2008.07.020. Epub 2008 Jul 24.


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