S. Mascarella

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Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity.

F Ivy Carroll, S Wayne Mascarella, J. L. Howard, 2010, Journal of medicinal chemistry.

Structure of the human kappa opioid receptor in complex with JDTic

Bryan L. Roth, Raymond C. Stevens, Vadim Cherezov, 2012, Nature.

Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.

F I Carroll, S W Mascarella, James B. Thomas, 2001, Journal of medicinal chemistry.

Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.

James B. Thomas, S. Mascarella, F. Carroll, 2003, Journal of medicinal chemistry.

Design, Synthesis, and Biological Evaluation of (3R)-1,2,3,4-Tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) Analogues: In Vitro Pharmacology and ADME Profile

James B. Thomas, S. Runyon, L. Brieaddy, 2014, Journal of medicinal chemistry.

Synthesis and Evaluation of Metabotropic Glutamate Receptor Subtype 5 Antagonists Based on Fenobam().

S. Mascarella, H. Navarro, F. Carroll, 2011, ACS medicinal chemistry letters.

A comparison of (-)-deoxybenzomorphans devoid of opiate activity with their dextrorotatory phenolic counterparts suggests role of sigma 2 receptors in motor function.

W. Bowen, S. L. Patrick, J. Walker, 1993, European journal of pharmacology.

Bupropion and bupropion analogs as treatments for CNS disorders.

R. Lukas, S. Mascarella, H. Navarro, 2014, Advances in pharmacology.

Effect of the 3- and 4-Methyl Groups on the Opioid Receptor Properties of N-Substituted trans-3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines

James B. Thomas, S. Runyon, L. Brieaddy, 2014, Journal of medicinal chemistry.

Synthesis, Nicotinic Acetylcholine Receptor Binding, and Antinociceptive Properties of 2′-Fluoro-3′-(substituted pyridinyl)-7-deschloroepibatidine Analogues

S. Mascarella, H. Navarro, F. Carroll, 2014, Journal of medicinal chemistry.

Synthesis and nicotinic acetylcholine receptor in vitro and in vivo pharmacological properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues of 2'-fluoro-3'-(4-nitrophenyl)deschloroepibatidine.

S. Mascarella, H. Navarro, F. Carroll, 2012, Journal of medicinal chemistry.

Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.

S. Mascarella, F. Carroll, J. B. Thomas, 1998, Journal of medicinal chemistry.

Synthesis of bridged analogs of epibatidine. 3-Chloro-5,7,8,9,9a,10-hexahydro-7,10-methanopyrrolo[1,2-b]-2,6-naphthyridine and 2-chloro-5,5a,6,7,8,10-hexahydro-5,8-methanopyrrolo[2,1-b]-1,7-naphthyridine

L. Brieaddy, S. Mascarella, H. Navarro, 2001 .

Designer drugs: a medicinal chemistry perspective (II)

S. Mascarella, F. Carroll, A. Lewin, 2020, Annals of the New York Academy of Sciences.

Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation.

R. Lukas, S. Mascarella, H. Navarro, 2009, Journal of medicinal chemistry.

A novel asymmetric synthesis of 3-benzyl-1,2,3,4,5,6-hexahydro-11-alkyl-2,6-methano-3-benzazocines

W. Bowen, S. Mascarella, F. Carroll, 1994 .

Effects of sphingosine stereoisomers on P-glycoprotein phosphorylation and vinblastine accumulation in multidrug-resistant MCF-7 cells.

R. Fine, R. Bell, S. Mascarella, 1996, Biochemical pharmacology.

Emergence and properties of spice and bath salts: a medicinal chemistry perspective.

S. Mascarella, F. Carroll, A. Lewin, 2014, Life sciences.

Structure-activity correlations for beta-phenethylamines at human trace amine receptor 1.

S. Mascarella, H. Navarro, A. Lewin, 2008, Bioorganic & medicinal chemistry.

Potent and Selective Tetrahydroisoquinoline Kappa Opioid Receptor Antagonists of Lead Compound (3 R)-7-Hydroxy- N-[(1 S)-2-methyl-1-(piperidin-1-ylmethyl)propyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (PDTic).

T. Fennell, R. Snyder, James B. Thomas, 2018, Journal of medicinal chemistry.

Design, Synthesis, and Biological Evaluation of Structurally Rigid Analogues of 4-(3-Hydroxyphenyl)piperidine Opioid Receptor Antagonists.

J. Deschamps, S. Runyon, S. Mascarella, 2016, The Journal of organic chemistry.

Discovery of N-{4-[(3-hydroxyphenyl)-3-methylpiperazin-1-yl]methyl-2-methylpropyl}-4-phenoxybenzamide analogues as selective kappa opioid receptor antagonists.

I. Carroll, James B. Thomas, S. Runyon, 2013, Journal of medicinal chemistry.

Importance of phenolic address groups in opioid kappa receptor selective antagonists.

James B. Thomas, S. Mascarella, F. Carroll, 2004, Journal of medicinal chemistry.

Nicotinic Acetylcholine Receptor Efficacy And Pharmacological Properties Of 3-(Substituted Phenyl)-2Ã”Â2-Substituted Tropanes

J. Lukáš, S. Mascarella, F. Carroll, 2021 .

Synthesis of 2-(substituted phenyl)-3,5,5-trimethylmorpholine analogues and their effects on monoamine uptake, nicotinic acetylcholine receptor function, and behavioral effects of nicotine.

R. Lukas, S. Mascarella, H. Navarro, 2011, Journal of medicinal chemistry.

Nicotinic acetylcholine receptor efficacy and pharmacological properties of 3-(substituted phenyl)-2β-substituted tropanes.

R. Lukas, S. Mascarella, H. Navarro, 2010, Journal of medicinal chemistry.

Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.

S. Mascarella, F. Carroll, J. B. Thomas, 1998, Journal of medicinal chemistry.

α-[Amino(4-aminophenyl)thio]methylene-2-(trifluoromethyl)benzeneacetonitrile; Configurational equilibria in solution.

J. Deschamps, L. Brieaddy, S. Mascarella, 2021, Bioorganic chemistry.

Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of the 3- and 4-methyl substituents.

James B. Thomas, S. Runyon, S. Mascarella, 2015, Bioorganic & medicinal chemistry.

Potent and Selective Tetrahydroisoquinoline Kappa Opioid Receptor Antagonists of Lead Compound (3 R)- N-[1 R)-1-(Cyclohexylmethyl)-2-methylpropyl]-7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (CDTic).

T. Fennell, R. Snyder, James B. Thomas, 2018, Journal of medicinal chemistry.

Structure of the human k-opioid receptor in complex with JDTic

R. Stevens, Xi-Ping Huang, B. Roth, 2012 .

Synthesis and in vitro opioid receptor functional antagonism of methyl-substituted analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic).

James B. Thomas, S. Mascarella, H. Navarro, 2009, Journal of medicinal chemistry.

N-Substituted 4β-Methyl-5-(3-hydroxyphenyl)-7α-amidomorphans Are Potent, Selective κ Opioid Receptor Antagonists

James B. Thomas, S. Mascarella, H. Navarro, 2006 .

Structure-activity analysis of anandamide analogs: relationship to a cannabinoid pharmacophore.

S. Mascarella, B. Thomas, R. Razdan, 1996, Journal of medicinal chemistry.

Conjugate addition―cycloacylation of acetylenic diesters: synthesis of highly functionalized cyclopentenones

S. Mascarella, M. Crimmins, Joe A. DeLoach, 1984 .

Enantiomeric N-substituted N-normetazocines: a comparative study of affinities at sigma, PCP, and mu opioid receptors.

S. Mascarella, F. Carroll, B. Martin, 1992, Journal of medicinal chemistry.

Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.

R. Lukas, S. Mascarella, H. Navarro, 2010, Journal of medicinal chemistry.

Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine.

S. Mascarella, H. Navarro, F. Carroll, 2007, Journal of medicinal chemistry.

Designer drugs: a medicinal chemistry perspective

F Ivy Carroll, Anita H Lewin, S Wayne Mascarella, 2012, Annals of the New York Academy of Sciences.

1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists.

James B. Thomas, S. Runyon, S. Mascarella, 2010, ACS medicinal chemistry letters.

Stimulation of rat striatal tyrosine hydroxylase activity following intranigral administration of sigma receptor ligands.

S. L. Patrick, J. Walker, S. Mascarella, 1995, European journal of pharmacology.

Synthesis and physicochemical characterization of (6S)-5-formiminotetrahydrofolate; a reference standard for metabolomics.

S. Mascarella, A. Lewin, H. Seltzman, 2018, Organic & biomolecular chemistry.

Synthesis and muscarinic receptor activity of ester derivatives of 2-substituted 2-azabicyclo[2.2.1]heptan-5-ol and -6-ol.

D J Triggle, F I Carroll, P Abraham, 1992, Journal of medicinal chemistry.

Synthesis of 3-halomethyl-2,3,4,5-tetrahydro-2,5-methano-1H-2-benzazepines and their rearrangement to 4-halo-1,2,3,4,5,6-hexahydro-2,6-methano-2-benzazocines

S. Mascarella, F. Carroll, B. Blough, 1993 .

Intramolecular photocycloadditions: synthesis of stericallycongested substituted [4.5.5.5] Fenestranes. Models for the total synthesis of laurenene and silphinene

S. Mascarella, M. Crimmins, L. D. Bredon, 1985 .

N-substituted cis-4a-(3-hydroxyphenyl)-8a-methyloctahydroisoquinolines are opioid receptor pure antagonists.

J. Deschamps, James B. Thomas, S. Mascarella, 2005, Journal of medicinal chemistry.

Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogues.

J. B. Pitner, D. Triggle, S. Mascarella, 1991, Journal of medicinal chemistry.

Conformationally constrained analogues of N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4- dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716): design, synthesis, computational analysis, and biological evaluations.

S. Mascarella, B. Thomas, M. Brackeen, 2008, Journal of medicinal chemistry.

Synthesis and monoamine transporter binding properties of 2,3-cyclo analogues of 3beta-(4'-aminophenyl)-2beta-tropanemethanol.

J. Deschamps, S. Mascarella, H. Navarro, 2006, Journal of medicinal chemistry.

Hydrolytic instability of the important orexin 1 receptor antagonist SB-334867: possible confounding effects on in vivo and in vitro studies.

S. Runyon, L. Brieaddy, S. Mascarella, 2012, Bioorganic & medicinal chemistry letters.

Synthesis and sigma binding properties of 1'- and 3'-halo- and 1',3'-dihalo-N-normetazocine analogues.

W. Bowen, S. Mascarella, F. Carroll, 1995, Journal of medicinal chemistry.

Synthesis of 9β-methyl-2-alkyl-7-oxo-5-arylmorphans

James B. Thomas, L. Brieaddy, S. Mascarella, 1998 .

N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.

C. George, J. Flippen-Anderson, S. Mascarella, 1998, Journal of medicinal chemistry.

Identification and Differentiation of Isomeric Methylated Derivatives of Oxygenation Products of Polycyclic Aromatic Hydrocarbons by Gas Chromatography - Mass Spectrometry

S. Mascarella, J. Patel, J. Laseter, 1979 .

Dopamine transporter uptake blockers: Structure-activity relationships

S. Mascarella, F. Carroll, A. Lewin, 1995 .

Synthesis, Ligand Binding, and Quantitative Structure−Activity Relationship Study of 3β-(4‘-Substituted phenyl)-2β-heterocyclic Tropanes: Evidence for an Electrostatic Interaction at the 2β-Position

M. Kuhar, S. Mascarella, F. Carroll, 1996 .

Synthesis and Ligand Binding Study of 3β-(4′-Substituted phenyl)- 2β-(heterocyclic)tropanes.

M. Kuhar, S. Mascarella, F. Carroll, 1995 .

Synthesis and ligand binding study of 3 beta-(4'-substituted phenyl)-2 beta-(heterocyclic)tropanes.

M. Kuhar, S. Mascarella, F. Carroll, 1995, Journal of medicinal chemistry.

Synthesis, ligand binding, and QSAR (CoMFA and classical) study of 3 beta-(3'-substituted phenyl)-, 3 beta-(4'-substituted phenyl)-, and 3 beta-(3',4'-disubstituted phenyl)tropane-2 beta-carboxylic acid methyl esters.

F I Carroll, P Abraham, S W Mascarella, 1994, Journal of medicinal chemistry.

Dopamine-Transporter Uptake Blockers

S. Mascarella, F. Carroll, A. Lewin, 1997 .

Synthesis, Nicotinic Acetylcholine Binding, and in Vitro and in Vivo Pharmacological Properties of 2'-Fluoro-(carbamoylpyridinyl)deschloroepibatidine Analogues.

M. Marks, S. Mascarella, H. Navarro, 2016, ACS chemical neuroscience.

(3S)-3-Hydroxyquinidine, the major biotransformation product of quinidine, synthesis and conformational studies. X-ray molecular structure of (3S)-3-hydroxyquinidine methanesulphonate

S. Mascarella, F. Carroll, P. Abraham, 1991 .

RTI‐4793‐14, a new ligand with high affinity and selectivity for the (+)‐MK801‐insensitive [3H]1‐[1‐(2 thienyl)cyclohexyl]piperidine binding site (PCP site 2) of guinea pig brain

J. Cadet, M. Rogawski, S. Mascarella, 1994, Synapse.

Organics in the water colümn and air-water interface samples of Mississippi river water

S. Mascarella, E. Overton, J. Laseter, 1980 .

In vitro and in vivo neuronal nicotinic receptor properties of (+)- and (-)-pyrido[3,4]homotropane [(+)- and (-)-PHT]: (+)-PHT is a potent and selective full agonist at α6β2 containing neuronal nicotinic acetylcholine receptors.

M. Marks, S. Mascarella, H. Navarro, 2015, ACS chemical neuroscience.

Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.

S. Mascarella, F. Carroll, J. B. Thomas, 1999, Bioorganic & medicinal chemistry letters.

(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.

S. Mascarella, F. Carroll, J. B. Thomas, 1999, Bioorganic & medicinal chemistry letters.

Use of D-erythro-sphingosine as a pharmacological inhibitor of protein kinase C in human platelets.

Y. Hannun, S. Mascarella, F. Carroll, 1990, The Biochemical journal.

A Perspective of Modern Methods in Computer‐Aided Drugc design

Lisa M. Balbes, S. Wayne Mascarella, Donald B. Boyds, 2007 .

Quantitative Signaling and Structure-Activity Analyses Demonstrate Functional Selectivity at the Nociceptin/Orphanin FQ Opioid Receptor

M. Bruchas, S. Mascarella, H. Navarro, 2015, Molecular Pharmacology.

Synthesis, Nicotinic Acetylcholine Receptor Binding, and in Vitro and in Vivo Pharmacological Properties of 2'-Fluoro-(substituted thiophenyl)deschloroepibatidine Analogues.

S. Mascarella, H. Navarro, F. Carroll, 2017, ACS chemical neuroscience.

Synthesis, absolute configuration, and molecular modeling study of etoxadrol, a potent phencyclidine-like agonist.

C. George, K. Rice, S. Mascarella, 1988, Journal of medicinal chemistry.

IDENTIFICATION OF PETROLEUM RESIDUE SOURCES AFTER A FIRE AND OIL SPILL

S. Mascarella, E. Overton, J. Laseter, 1981 .

Novel Synthesis and Pharmacological Characterization of NOP Receptor Agonist 8-[(1S,3aS)-2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (Ro 64-6198).

M. Bruchas, L. Brieaddy, S. Mascarella, 2015, ACS chemical neuroscience.

A stereoselective synthetic approach to N-alkyl-4β-methyl-5-phenylmorphans

James B. Thomas, S. Mascarella, F. Carroll, 1999 .

QSAR analysis of Delta(8)-THC analogues: relationship of side-chain conformation to cannabinoid receptor affinity and pharmacological potency.

S. Mascarella, B. Thomas, R. Razdan, 2000, Journal of medicinal chemistry.

Synthesis and sigma binding properties of 2'-substituted 5,9 alpha-dimethyl-6,7-benzomorphans.

W. Bowen, S. Mascarella, F. Carroll, 1995, Journal of medicinal chemistry.

4β-Methyl-5-(3-hydroxyphenyl)morphan opioid agonist and partial agonist derived from a 4β-methyl-5-(3-hydroxyphenyl)morphan pure antagonist.

B. Roth, James B. Thomas, S. Mascarella, 2013, Journal of medicinal chemistry.

Simple Tetrahydroisoquinolines Are Potent and Selective Kappa Opioid Receptor Antagonists.

James B. Thomas, S. Runyon, S. Mascarella, 2017, ACS medicinal chemistry letters.

Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides.

C. George, J. Flippen-Anderson, S. Mascarella, 2001, Journal of medicinal chemistry.

Discovery of the First N-Substituted 4β-Methyl-5-(3-hydroxyphenyl)morphan To Possess Highly Potent and Selective Opioid δ Receptor Antagonist Activity

James B. Thomas, S. Mascarella, H. Navarro, 2004 .

Intramolecular Photocycloaddition-Cyclobutane Fragmentation: Total Synthesis of (±)-Silphinene.

S. Mascarella, M. Crimmins, 1986 .

N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.

C. George, J. Flippen-Anderson, S. Mascarella, 1998, Bioorganic & medicinal chemistry letters.

4-[(8-Alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]-N,N-diethylbenzamides: high affinity, selective ligands for the delta opioid receptor illustrate factors important to antagonist activity.

James B. Thomas, S. Mascarella, F. Carroll, 2000, Bioorganic & medicinal chemistry letters.

Structure of the human kappa opioid receptor in complex with JDTic

R. Stevens, Xi-Ping Huang, B. Roth, 2012, Nature.

Synthesis, nicotinic acetylcholine receptor binding, in vitro and in vivo pharmacology properties of 3'-(substituted pyridinyl)-deschloroepibatidine analogs.

S. Mascarella, H. Navarro, F. Carroll, 2015, Bioorganic & Medicinal Chemistry.

Caged Naloxone: Synthesis, Characterization, and Stability of 3- O-(4,5-Dimethoxy-2-nitrophenyl)carboxymethyl Naloxone (CNV-NLX).

S. Mascarella, F. Carroll, A. Lewin, 2017, ACS chemical neuroscience.

Synthesis and physicochemical characterization of the one-carbon carrier 10-formyltetrahydrofolate; a reference standard for metabolomics

S. Mascarella, H. Seltzman, P. Silinski, 2017, Metabolomics.

Synthesis And Characterization Of In Vitro And In Vivo Profiles Of Synthesis And Characterization Of In Vitro And In Vivo Profiles Of Hydroxybupropion Analogues: Aids To Smoking Cessation Hydroxybupropion Analogues: Aids To Smoking Cessation

S. Mascarella, M. Damaj, S. Marxer-Miller, 2022 .

Synthesis of 2-(substituted phenyl)-3,5,5-trimethylmorpholine analogues and their effects on monoamine uptake, nicotinic acetylcholine receptor function, and behavioral effects of nicotine.

R. Lukas, S. Mascarella, H. Navarro, 2011, Journal of medicinal chemistry.