Published in Bioorg Med Chem Lett on October 14, 2008
Pyrrolidine analogues of lobelane: relationship of affinity for the dihydrotetrabenazine binding site with function of the vesicular monoamine transporter 2 (VMAT2). J Med Chem (2009) 1.30
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. J Pharmacol Exp Ther (2010) 1.00
Design, synthesis and interaction at the vesicular monoamine transporter-2 of lobeline analogs: potential pharmacotherapies for the treatment of psychostimulant abuse. Curr Top Med Chem (2011) 0.93
Pyrrolidine analogs of GZ-793A: synthesis and evaluation as inhibitors of the vesicular monoamine transporter-2 (VMAT2). Bioorg Med Chem Lett (2013) 0.89
Quinlobelane: a water-soluble lobelane analogue and inhibitor of VMAT2. Bioorg Med Chem Lett (2010) 0.87
Exploring the effect of N-substitution in nor-lobelane on the interaction with VMAT2: discovery of a potential clinical candidate for treatment of methamphetamine abuse. Medchemcomm (2013) 0.79
Stereocontrolled synthesis and pharmacological evaluation of cis-2,6-diphenethyl-1-azabicyclo[2.2.2]octanes as lobelane analogues. J Org Chem (2009) 0.76
Lobelane analogues containing 4-hydroxy and 4-(2-fluoroethoxy) aromatic substituents: Potent and selective inhibitors of [(3)H]dopamine uptake at the vesicular monoamine transporter-2. Bioorg Med Chem Lett (2016) 0.75
Synthesis of Lobeline, Lobelane and their Analogues. A Review. Org Prep Proced Int (2015) 0.75
Defunctionalized lobeline analogues: structure-activity of novel ligands for the vesicular monoamine transporter. J Med Chem (2005) 3.32
A novel mechanism of action and potential use for lobeline as a treatment for psychostimulant abuse. Biochem Pharmacol (2002) 2.51
Lobeline and nicotine evoke [3H]overflow from rat striatal slices preloaded with [3H]dopamine: differential inhibition of synaptosomal and vesicular [3H]dopamine uptake. J Pharmacol Exp Ther (1997) 2.14
Lobelane decreases methamphetamine self-administration in rats. Eur J Pharmacol (2007) 1.82
Vesicular monoamine transporter 2: role as a novel target for drug development. AAPS J (2006) 1.78
Lobeline displaces [3H]dihydrotetrabenazine binding and releases [3H]dopamine from rat striatal synaptic vesicles: comparison with d-amphetamine. J Neurochem (1998) 1.76
Easily prepared air- and moisture-stable Pd-NHC (NHC=N-heterocyclic carbene) complexes: a reliable, user-friendly, highly active palladium precatalyst for the Suzuki-Miyaura reaction. Chemistry (2006) 1.55
Lobelane analogues as novel ligands for the vesicular monoamine transporter-2. Bioorg Med Chem (2005) 1.38
A user-friendly, all-purpose Pd-NHC (NHC=N-heterocyclic carbene) precatalyst for the negishi reaction: a step towards a universal cross-coupling catalyst. Chemistry (2006) 1.10
Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands. Bioorg Med Chem Lett (2005) 1.06
Defunctionalized lobeline analogues: structure-activity of novel ligands for the vesicular monoamine transporter. J Med Chem (2005) 3.32
Novel substituted (Z)-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-one and (Z)-(+/-)-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-ol derivatives as potent thermal sensitizing agents. Bioorg Med Chem Lett (2007) 3.14
NADPH oxidase activity is essential for Keap1/Nrf2-mediated induction of GCLC in response to 2-indol-3-yl-methylenequinuclidin-3-ols. Cancer Res (2003) 3.02
Aminoparthenolides as novel anti-leukemic agents: Discovery of the NF-kappaB inhibitor, DMAPT (LC-1). Bioorg Med Chem Lett (2009) 2.77
A novel mechanism of action and potential use for lobeline as a treatment for psychostimulant abuse. Biochem Pharmacol (2002) 2.51
An orally bioavailable parthenolide analog selectively eradicates acute myelogenous leukemia stem and progenitor cells. Blood (2007) 2.14
Chemical genomic screening reveals synergism between parthenolide and inhibitors of the PI-3 kinase and mTOR pathways. Blood (2010) 1.92
Lobeline analogs with enhanced affinity and selectivity for plasmalemma and vesicular monoamine transporters. J Pharmacol Exp Ther (2004) 1.83
Lobelane decreases methamphetamine self-administration in rats. Eur J Pharmacol (2007) 1.82
Vesicular monoamine transporter 2: role as a novel target for drug development. AAPS J (2006) 1.78
Lobeline does not serve as a reinforcer in rats. Psychopharmacology (Berl) (2002) 1.63
Lobelane inhibits methamphetamine-evoked dopamine release via inhibition of the vesicular monoamine transporter-2. J Pharmacol Exp Ther (2009) 1.49
N,N'-Alkane-diyl-bis-3-picoliniums as nicotinic receptor antagonists: inhibition of nicotine-evoked dopamine release and hyperactivity. J Pharmacol Exp Ther (2008) 1.44
Melampomagnolide B: a new antileukemic sesquiterpene. Bioorg Med Chem (2011) 1.40
Lobelane analogues as novel ligands for the vesicular monoamine transporter-2. Bioorg Med Chem (2005) 1.38
Subtype-selective nicotinic receptor antagonists: potential as tobacco use cessation agents. Bioorg Med Chem Lett (2004) 1.36
Prefrontal cortex and drug abuse vulnerability: translation to prevention and treatment interventions. Brain Res Rev (2010) 1.34
The effects of a novel nicotinic receptor antagonist N,N-dodecane-1,12-diyl-bis-3-picolinium dibromide (bPiDDB) on acute and repeated nicotine-induced increases in extracellular dopamine in rat nucleus accumbens. Neuropharmacology (2006) 1.32
Environmental enrichment decreases cell surface expression of the dopamine transporter in rat medial prefrontal cortex. J Neurochem (2005) 1.32
Novel chemical enhancers of heat shock increase thermal radiosensitization through a mitotic catastrophe pathway. Cancer Res (2007) 1.32
Effect of bupropion on nicotine self-administration in rats. Psychopharmacology (Berl) (2003) 1.30
Pyrrolidine analogues of lobelane: relationship of affinity for the dihydrotetrabenazine binding site with function of the vesicular monoamine transporter 2 (VMAT2). J Med Chem (2009) 1.30
3-(2-Amino-1-methyl-4-oxo-4,5-dihydro-1H-imidazol-5-yl)-3-hydroxy-indolin-2-one monohydrate. Acta Crystallogr Sect E Struct Rep Online (2009) 1.29
Environmental enrichment enhances sensitization to GBR 12935-induced activity and decreases dopamine transporter function in the medial prefrontal cortex. Behav Brain Res (2004) 1.27
Extending the analysis of nicotinic receptor antagonists with the study of alpha6 nicotinic receptor subunit chimeras. Neuropharmacology (2008) 1.25
Targeting aberrant glutathione metabolism to eradicate human acute myelogenous leukemia cells. J Biol Chem (2013) 1.25
(Z)-3-(Benzo[b]thiophen-2-yl)-2-(3,4,5-trimethoxyphenyl)acrylonitrile and (E)-3-(benzo[b]thiophen-2-yl)-2-(3,4-dimethoxyphenyl)acrylonitrile. [corrected]. Acta Crystallogr C (2007) 1.23
Lobeline attenuates locomotor stimulation induced by repeated nicotine administration in rats. Pharmacol Biochem Behav (2003) 1.22
Novel substituted (Z)-5-((N-benzyl-1H-indol-3-yl)methylene)imidazolidine-2,4-diones and 5-((N-benzyl-1H-indol-3-yl)methylene)pyrimidine-2,4,6(1H,3H,5H)-triones as potent radio-sensitizing agents. Bioorg Med Chem Lett (2009) 1.19
A NADPH oxidase-dependent redox signaling pathway mediates the selective radiosensitization effect of parthenolide in prostate cancer cells. Cancer Res (2010) 1.18
The pharmacological activity of nicotine and nornicotine on nAChRs subtypes: relevance to nicotine dependence and drug discovery. J Neurochem (2007) 1.18
bis-Azaaromatic quaternary ammonium analogues: ligands for alpha4beta2* and alpha7* subtypes of neuronal nicotinic receptors. Bioorg Med Chem Lett (2002) 1.17
Molecular pathway for thymoquinone-induced cell-cycle arrest and apoptosis in neoplastic keratinocytes. Anticancer Drugs (2004) 1.17
Synthesis and evaluation of a series of benzothiophene acrylonitrile analogs as anticancer agents. Medchemcomm (2013) 1.17
Antileukemic activity of aminoparthenolide analogs. Bioorg Med Chem Lett (2008) 1.14
Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release. Bioorg Med Chem Lett (2004) 1.13
N-n-alkylnicotinium analogs, a novel class of nicotinic receptor antagonists: interaction with alpha4beta2* and alpha7* neuronal nicotinic receptors. J Pharmacol Exp Ther (2003) 1.13
(Z)-2-(1-Phenylsulfonyl-1H-indol-3-ylmethylene)-1-azabicyclo[2.2.2]octan-3-one and (Z)-(S)-2-(1-phenylsulfonyl-1H-indol-3-ylmethylene)-1-azabicyclo[2.2.2]octan-3-ol. Acta Crystallogr C (2004) 1.13
Bupropion inhibits nicotine-evoked [(3)H]overflow from rat striatal slices preloaded with [(3)H]dopamine and from rat hippocampal slices preloaded with [(3)H]norepinephrine. J Pharmacol Exp Ther (2002) 1.13
N-n-alkylpyridinium analogs, a novel class of nicotinic receptor antagonists: selective inhibition of nicotine-evoked [3H] dopamine overflow from superfused rat striatal slices. J Pharmacol Exp Ther (2003) 1.12
(Z)-3-(1H-Indol-3-yl)-2-(3-thienyl)acrylonitrile and (Z)-3-[1-(4-tert-butylbenzyl)-1H-indol-3-yl]-2-(3-thienyl)acrylonitrile. Acta Crystallogr C (2005) 1.11
Novel N-1,2-dihydroxypropyl analogs of lobelane inhibit vesicular monoamine transporter-2 function and methamphetamine-evoked dopamine release. J Pharmacol Exp Ther (2011) 1.10
(Z)-2-[(1-Phenylsulfonyl-1H-indol-3-yl)methylene]-1-azabicyclo[2.2.2]octan-3-one semicarbazone. Acta Crystallogr C (2007) 1.10
A pilot study of plasma caffeine concentrations in a US sample of smoker and nonsmoker volunteers. Prog Neuropsychopharmacol Biol Psychiatry (2003) 1.09
Nicotinic receptor-based therapeutics and candidates for smoking cessation. Biochem Pharmacol (2009) 1.09
Transdermal delivery of naltrexol and skin permeability lifetime after microneedle treatment in hairless guinea pigs. J Pharm Sci (2010) 1.09
The effect of a novel VMAT2 inhibitor, GZ-793A, on methamphetamine reward in rats. Psychopharmacology (Berl) (2011) 1.08
Pharmacokinetics of the novel nicotinic receptor antagonist N,N'-dodecane-1,12-diyl-bis-3-picolinium dibromide in the rat. Drug Metab Dispos (2008) 1.07
Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands. Bioorg Med Chem Lett (2005) 1.06
rac-2-(2-Amino-4-oxo-4,5-dihydro-1,3-thia-zol-5-yl)-2-hydroxy-indane-1,3-dione. Acta Crystallogr Sect E Struct Rep Online (2009) 1.06
Carrier-mediated transport of the quaternary ammonium neuronal nicotinic receptor antagonist n,n'-dodecylbispicolinium dibromide at the blood-brain barrier. J Pharmacol Exp Ther (2007) 1.06
N-n-alkylnicotinium analogs, a novel class of nicotinic receptor antagonist: inhibition of S(-)-nicotine-evoked [(3)H]dopamine overflow from superfused rat striatal slices. J Pharmacol Exp Ther (2002) 1.05
Modeling multiple species of nicotine and deschloroepibatidine interacting with alpha4beta2 nicotinic acetylcholine receptor: from microscopic binding to phenomenological binding affinity. J Am Chem Soc (2005) 1.05
Microwave assisted synthesis and in vitro cytotoxicities of substituted (Z)-2-amino-5-(1-benzyl-1H-indol-3-yl)methylene-1-methyl-1H-imidazol-4(5H)-ones against human tumor cell lines. Bioorg Med Chem Lett (2009) 1.05
Synthesis and in vitro evaluation of N-alkyl-3-hydroxy-3-(2-imino-3-methyl-5-oxoimidazolidin-4-yl)indolin-2-one analogs as potential anticancer agents. Bioorg Med Chem Lett (2010) 1.05
(Z)-4-[3-(2,5-Dioxoimidazolidin-4-ylidenemeth-yl)-1H-indol-1-ylmeth-yl]benzonitrile. Acta Crystallogr Sect E Struct Rep Online (2008) 1.04
3-(2-Amino-1-methyl-4-oxo-4,5-dihydro-1H-imidazol-5-yl)-5-fluoro-3-hydr-oxy-1-methyl-indolin-2-one methanol hemisolvate. Acta Crystallogr Sect E Struct Rep Online (2009) 1.04
The radiosensitization effect of parthenolide in prostate cancer cells is mediated by nuclear factor-kappaB inhibition and enhanced by the presence of PTEN. Mol Cancer Ther (2007) 1.03
Enhancement of transdermal delivery of 6-beta-naltrexol via a codrug linked to hydroxybupropion. J Control Release (2006) 1.03
Transdermal delivery of naltrexone and its active metabolite 6-beta-naltrexol in human skin in vitro and guinea pigs in vivo. J Pharm Sci (2005) 1.03
Active transport of high-affinity choline and nicotine analogs into the central nervous system by the blood-brain barrier choline transporter. J Pharmacol Exp Ther (2003) 1.02
Methylphenidate treatment in adolescent rats with an attention deficit/hyperactivity disorder phenotype: cocaine addiction vulnerability and dopamine transporter function. Neuropsychopharmacology (2010) 1.02
Effects of norketamine enantiomers in rodent models of persistent pain. Pharmacol Biochem Behav (2008) 1.02
Flux across [corrected] microneedle-treated skin is increased by increasing charge of naltrexone and naltrexol in vitro. Pharm Res (2008) 1.01
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. J Pharmacol Exp Ther (2010) 1.00
Tris-azaaromatic quaternary ammonium salts: Novel templates as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release. Bioorg Med Chem Lett (2007) 1.00
In vitro permeation of a pegylated naltrexone prodrug across microneedle-treated skin. J Control Release (2010) 1.00
Mecamylamine, dihydro-beta-erythroidine, and dextromethorphan block conditioned responding evoked by the conditional stimulus effects of nicotine. Pharmacol Biochem Behav (2009) 1.00
Targeting reward-relevant nicotinic receptors in the discovery of novel pharmacotherapeutic agents to treat tobacco dependence. Nebr Symp Motiv (2009) 1.00