E. Burstein

发表

Low dose bexarotene treatment rescues dopamine neurons and restores behavioral function in models of Parkinson's disease.

K. Mcfarland, T. Spalding, D. Hubbard, 2013, ACS chemical neuroscience.

AC-186, a selective nonsteroidal estrogen receptor β agonist, shows gender specific neuroprotection in a Parkinson's disease rat model.

K. Mcfarland, D. Bonhaus, Jian-Nong Ma, 2013, ACS chemical neuroscience.

Identification of the Antiarrhythmic Drugs Amiodarone and Lorcainide as Potent H3 Histamine Receptor Inverse Agonists

F. Piu, Jian-Nong Ma, E. Burstein, 2014, The Journal of Pharmacology and Experimental Therapeutics.

Optimization of isochromanone based urotensin II receptor agonists.

U. Hacksell, K. Luthman, E. Currier, 2010, Bioorganic & medicinal chemistry.

Population study of triazolam pharmacokinetics.

D. Greenblatt, J. Harmatz, R. Shader, 1986, British journal of clinical pharmacology.

Guanine Nucleotide Dissociation Stimulators

I. Macara, E. Burstein, 1993 .

Constitutive activation of chimeric m2/m5 muscarinic receptors and delineation of G-protein coupling selectivity domains.

M. Brann, T. Spalding, E. Burstein, 1996, Biochemical pharmacology.

The role of M1 muscarinic receptor agonism of N-desmethylclozapine in the unique clinical effects of clozapine

A. Levey, H. Meltzer, U. Hacksell, 2004, Psychopharmacology.

Structural Requirements of Transmembrane Domain 3 for Activation by the M1 Muscarinic Receptor Agonists AC-42, AC-260584, Clozapine, and N-Desmethylclozapine: Evidence for Three Distinct Modes of Receptor Activation

M. Brann, T. Spalding, Jian-Nong Ma, 2006, Molecular Pharmacology.

Characterization of a guanine nucleotide-releasing factor and a GTPase-activating protein that are specific for the ras-related protein p25rab3A.

I. Macara, E. Burstein, Ian G. Macara, 1992, Proceedings of the National Academy of Sciences of the United States of America.

Characterization of Highly Efficacious Allosteric Agonists of the Human Calcium-Sensing Receptor

K. Schmelzer, Jian-Nong Ma, R. Olsson, 2011, Journal of Pharmacology and Experimental Therapeutics.

Discovery of a class of calcium sensing receptor positive allosteric modulators; 1-(benzothiazol-2-yl)-1-phenylethanols.

E. Currier, Jian-Nong Ma, R. Olsson, 2010, Bioorganic & medicinal chemistry letters.

Chiral Dihydrobenzofuran Acids Show Potent Retinoid X Receptor-Nuclear Receptor Related 1 Protein Dimer Activation.

C. Ottmann, M. Scheepstra, L. Brunsveld, 2016, Journal of medicinal chemistry.

Trazodone kinetics: Effect of age, gender, and obesity

D. Greenblatt, J. Harmatz, R. Shader, 1987, Clinical pharmacology and therapeutics.

Pharmacology of muscarinic receptor subtypes constitutively activated by G proteins.

M. Brann, T. Spalding, E. Burstein, 1997, Molecular pharmacology.

Functional Enhancement of AT1R Potency in the Presence of the TPαR Is Revealed by a Comprehensive 7TM Receptor Co-Expression Screen

D. Weiner, C. Lyngsø, J. L. Hansen, 2013, PloS one.

Discovery of potent and selective small-molecule PAR-2 agonists.

E. Currier, Jian-Nong Ma, R. Olsson, 2008, Journal of medicinal chemistry.

Regulation of the GTPase cycle of the neuronally expressed Ras-like GTP-binding protein Rab3A.

K. Kaibuchi, I. Macara, Y. Takai, 1993, Journal of Biological Chemistry.

Discovery of the first nonpeptide agonist of the GPR14/urotensin-II receptor: 3-(4-chlorophenyl)-3-(2- (dimethylamino)ethyl)isochroman-1-one (AC-7954).

U. Hacksell, D. Weiner, M. Brann, 2002, Journal of medicinal chemistry.

Lack of Evidence for AT1R/B2R Heterodimerization in COS-7, HEK293, and NIH3T3 Cells

T. Walther, D. Weiner, E. Kostenis, 2009, Journal of Biological Chemistry.

Regulation of the GTPase activity of the ras-like protein p25rab3A. Evidence for a rab3A-specific GAP.

I. Macara, Z. Lu, E. Burstein, 1991, The Journal of biological chemistry.

The ras-like protein p25rab3A is partially cytosolic and is expressed only in neural tissue

I. Macara, E. Burstein, 1989, Molecular and cellular biology.

Identification and characterization of novel small molecule Protease Activated Receptor 2 ( PAR 2 ) agonists

K. Schmelzer, J. Lameh, N. Nash, 2008 .

In Vitro Pharmacology of Clinically Used Central Nervous System-Active Drugs as Inverse H1 Receptor Agonists

R. Leurs, U. Hacksell, D. Weiner, 2007, Journal of Pharmacology and Experimental Therapeutics.

Molecular cloning and pharmacology of functionally distinct isoforms of the human histamine H3 receptor

D. Weiner, M. Brann, N. Nash, 2002, Neuropharmacology.

Homologous mutations near the junction of the sixth transmembrane domain and the third extracellular loop lead to constitutive activity and enhanced agonist affinity at all muscarinic receptor subtypes.

D. J. Ford, T. Spalding, E. Burstein, 2002, The Journal of pharmacology and experimental therapeutics.

Constitutive activation of muscarinic receptors by the G‐protein Gq

M. Brann, T. Spalding, E. Burstein, 1995, FEBS letters.

The human angiotensin AT(1) receptor supports G protein-independent extracellular signal-regulated kinase 1/2 activation and cellular proliferation.

D. Weiner, J. L. Hansen, S. Haunsø, 2008, European journal of pharmacology.

The Protease Activated Receptor 2 (PAR2) Polymorphic Variant F240S Constitutively Activates PAR2 Receptors and Potentiates Responses to Small-Molecule PAR2 Agonists

E. Burstein, Jian‐Nong Ma, 2013, The Journal of Pharmacology and Experimental Therapeutics.

The PAR2 polymorphic variant F240S constitutively activates PAR2 receptors and potentiates responses to small molecule PAR2 agonists.

E. Burstein, Jian‐Nong Ma, 2013 .

Mutants of Rab3A analogous to oncogenic Ras mutants. Sensitivity to Rab3A-GTPase activating protein and Rab3A-guanine nucleotide releasing factor.

I. Macara, W. Brondyk, E. Burstein, 1993, The Journal of biological chemistry.

G protein-coupled receptors and proliferative signaling.

M. Smit, E. Burstein, R. Bakker, 2002, Methods in enzymology.

Functional Importance of the Ala116–Pro136 Region in the Calcium-sensing Receptor

M. Brann, P. O'Hara, P. Krogsgaard‐Larsen, 2000, The Journal of Biological Chemistry.

Constitutive activation of the m5 muscarinic receptor by a series of mutations at the extracellular end of transmembrane 6.

J. W. Wells, M. Brann, T. Spalding, 1997, Biochemistry.

Pharmacological and behavioral profile of ACP-103, a novel 5-HT 2A receptor inverse agonist

Robert I. Davis, M. Geyer, D. Weiner, 2006 .

Amino acid residues in the Ras-like GTPase Rab3A that specify sensitivity to factors that regulate the GTP/GDP cycling of Rab3A.

I. Macara, W. Brondyk, E. Burstein, 1992, The Journal of biological chemistry.

Design of a Highly Selective and Potent Class of Non‐planar Estrogen Receptor β Agonists

A. Gustavsson, R. Olsson, E. Burstein, 2013, ChemMedChem.

The oncogenic protein p60v-src has competence activity but does not activate phosphatidylinositol turnover or protein kinase C in Balb/c 3T3 cells.

I. Macara, H. Sadowski, E. Burstein, 1990, Oncogene.

Amino Acid Side Chains That Define Muscarinic Receptor/G-protein Coupling

M. Brann, T. Spalding, E. Burstein, 1996, The Journal of Biological Chemistry.

Inverse agonists of the 5-HT2A receptor reduce nicotine withdrawal signs in rats

E. Burstein, D. Malin, Jian‐Nong Ma, 2019, Neuroscience Letters.

Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists.

F. Piu, K. Mcfarland, E. Currier, 2009, Journal of medicinal chemistry.

Structure-Function of Muscarinic Receptor Coupling to G Proteins

M. Brann, D. Hill-Eubanks, T. Spalding, 1995, The Journal of Biological Chemistry.

The impact of pimavanserin on psychotic phenotypes and tau phosphorylation in the P301L/COMT– and rTg(P301L)4510 mouse models of Alzheimer's disease

Eric H. Chang, L. Adrien, J. Koppel, 2022, Alzheimer's & dementia.

Identification of the Atypical L-Type Ca2+ Channel Blocker Diltiazem and Its Metabolites As Ghrelin Receptor Agonists

M. Brann, N. Nash, E. Currier, 2007, Molecular Pharmacology.

as Ghrelin receptor agonists

M. Brann, N. Nash, E. Currier, 2007 .

A subtype-specific neuropeptide FF receptor antagonist attenuates morphine and nicotine withdrawal syndrome in the rat

Caitlin A. Madison, E. Burstein, D. Malin, 2018, Neuroscience Letters.

Dronedarone Modulates M1 and M3 Muscarinic Receptors with Subtype Selectivity, Functional Selectivity, and Probe Dependence

E. Burstein, J. Ellis, G. M. Jayasuriya, 2016, Pharmacology.

Discovery of novel peptide/receptor interactions: identification of PHM-27 as a potent agonist of the human calcitonin receptor.

M. Brann, N. Nash, E. Currier, 2004, Biochemical pharmacology.

Structure/function relationships of a G-protein coupling pocket formed by the third intracellular loop of the m5 muscarinic receptor.

M. Brann, T. Spalding, E. Burstein, 1998, Biochemistry.

Interactions of Muscarinic Receptors with the Heterotrimeric G Proteins Gq and G12: Transduction of Proliferative Signals

B. Conklin, M. Brann, H. Bräuner‐Osborne, 1997, Journal of neurochemistry.

Should inverse agonists be defined by pharmacological mechanism or clinical effect?

E. Burstein, 2019, CNS Spectrums.

On the Discovery and Development of Pimavanserin: A Novel Drug Candidate for Parkinson’s Psychosis

U. Hacksell, R. Mills, K. Mcfarland, 2014, Neurochemical Research.

Preclinical PET Neuroimaging of [11C]Bexarotene

Steven H. Liang, N. Vasdev, J. Hooker, 2016, Molecular imaging.

Discovery of potential antipsychotic agents possessing pro-cognitive properties

F. Piu, K. Mcfarland, D. Bonhaus, 2012, Naunyn-Schmiedeberg's Archives of Pharmacology.

Bexarotene prodrugs: targeting through cleavage by NQO1 (DT-diaphorase).

R. Olsson, E. Burstein, A. Schäfer, 2014, Bioorganic & medicinal chemistry letters.

The Second Intracellular Loop of the m5 Muscarinic Receptor Is the Switch Which Enables G-protein Coupling*

M. Brann, T. Spalding, E. Burstein, 1998, The Journal of Biological Chemistry.

Constitutive Activity of Muscarinic Acetylcholine Receptors

T. Spalding, E. Burstein, 2006, Journal of receptor and signal transduction research.

Reversal of morphine tolerance by a compound with NPFF receptor subtype-selective actions

Caitlin A. Madison, E. Burstein, D. Malin, 2015, Neuroscience Letters.

Bromazepam pharmacokinetics: Influence of age, gender, oral contraceptives, cimetidine, and propranolol

D. Greenblatt, J. Harmatz, R. Shader, 1987, Clinical pharmacology and therapeutics.

Pharmacology of N-desmethylclozapine.

D. Weiner, D. Bonhaus, J. Lameh, 2007, Pharmacology & therapeutics.

Characterization of the Mas‐related gene family: structural and functional conservation of human and rhesus MrgX receptors

M. Brann, N. Nash, E. Burstein, 2006, British journal of pharmacology.

Discovery of an ectopic activation site on the M(1) muscarinic receptor.

U. Hacksell, M. Brann, E. Currier, 2002, Molecular pharmacology.

5-hydroxytryptamine2A receptor inverse agonists as antipsychotics.

M A Geyer, M. Geyer, K. Krebs-Thomson, 2001, The Journal of pharmacology and experimental therapeutics.

Identification of a Ligand-dependent Switch within a Muscarinic Receptor*

M. Brann, T. Spalding, E. Burstein, 1998, The Journal of Biological Chemistry.

Structure of a G-protein-coupling Domain of a Muscarinic Receptor Predicted by Random Saturation Mutagenesis (*)

M. Brann, D. Hill-Eubanks, H. Bräuner‐Osborne, 1996, The Journal of Biological Chemistry.

Studies of the Pharmacology, Localization, and Structure of Muscarinic Acetylcholine Receptors a

M. Brann, D. Hill-Eubanks, T. Spalding, 1993, Annals of the New York Academy of Sciences.

Simplified gas chromatographic analysis of ethanol in blood and tissue.

D. Greenblatt, E. Burstein, 1989, Journal of chromatography.

Pimavanserin, a 5HT2A receptor inverse agonist, rapidly suppresses Aβ production and related pathology in a mouse model of Alzheimer’s disease

J. Cirrito, E. Burstein, Clare E Wallace, 2020, Journal of neurochemistry.

I. In vivo evidence for partial agonist effects of (−)-OSU6162 and (+)-OSU6162 on 5-HT2A serotonin receptors

J. Rung, A. Carlsson, E. Burstein, 2011, Journal of Neural Transmission.

Design of a Highly Selective and Potent Class of Non‐planar Estrogen Receptor β Agonists.

A. Gustavsson, R. Olsson, E. Burstein, 2013 .

Pharmacology of polymorphic variants of the human 5-HT1A receptor.

U. Hacksell, D. Weiner, M. Brann, 2004, Biochemical pharmacology.

G-protein-coupled receptor-mediated activation of rap GTPases: characterization of a novel Gαi regulated pathway

E. Burstein, Anthony Essex, J. Weissman, 2004, Oncogene.

Identification and Characterization of Novel Small-Molecule Protease-Activated Receptor 2 Agonists

K. Schmelzer, J. Lameh, N. Nash, 2008, Journal of Pharmacology and Experimental Therapeutics.

Pharmacology of a constitutively active muscarinic receptor generated by random mutagenesis.

M. Brann, D. Hill-Eubanks, T. Spalding, 1995, The Journal of pharmacology and experimental therapeutics.

Ligand Dependent Switch from RXR Homo- to RXR-NURR1 Heterodimerization

C. Ottmann, M. Scheepstra, L. Brunsveld, 2017, ACS chemical neuroscience.

Triazolam Kinetics: Interaction with Cimetidine, Propranolol, and the Combination

D. Greenblatt, J. Harmatz, R. Shader, 1988, Journal of clinical pharmacology.

Clearance of the Antihistamine Doxylamine

D. Greenblatt, J. Harmatz, R. Shader, 1989 .

Intrinsic Efficacy of Antipsychotics at Human D2, D3, and D4 Dopamine Receptors: Identification of the Clozapine Metabolite N-Desmethylclozapine as a D2/D3 Partial Agonist

U. Hacksell, E. Pham, D. Weiner, 2005, Journal of Pharmacology and Experimental Therapeutics.

AC-260584, an orally bioavailable M1 muscarinic receptor allosteric agonist, improves cognitive performance in an animal model

K. Mcfarland, D. Bonhaus, J. Lameh, 2010, Neuropharmacology.

Pharmacological and Behavioral Profile of N-(4-Fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl) Carbamide (2R,3R)-Dihydroxybutanedioate (2:1) (ACP-103), a Novel 5-Hydroxytryptamine2A Receptor Inverse Agonist

Ethan S. Burstein, Fabrice Piu, Mark R. Brann, 2006, Journal of Pharmacology and Experimental Therapeutics.

Discovery of non-peptidergic MrgX1 and MrgX2 receptor agonists and exploration of an initial SAR using solid-phase synthesis.

E. Currier, R. Olsson, E. Burstein, 2009, Bioorganic & medicinal chemistry letters.

Integrative functional assays, chemical genomics and high throughput screening: harnessing signal transduction pathways to a common HTS readout.

D. Weiner, M. Brann, F. Piu, 2006, Current pharmaceutical design.

Interactions of the ras-like protein p25rab3A with Mg2+ and guanine nucleotides.

I. Macara, E. Burstein, 1992, The Biochemical journal.

Quantitation of flurazepam and three metabolites by electron capture gas liquid chromatography.

D. Greenblatt, H. Ochs, A. Locniskar, 1988, Journal of analytical toxicology.

Clearance of the antihistamine doxylamine. Reduced in elderly men but not in elderly women.

D. Greenblatt, J. Harmatz, R. Shader, 1989, Clinical pharmacokinetics.

An angiotensin II type 1 receptor activation switch patch revealed through evolutionary trace analysis.

O. Lichtarge, Srinivasan Madabushi, J. L. Hansen, 2010, Biochemical pharmacology.

Constitutively active muscarinic receptors.

T. Spalding, E. Burstein, 2001, Life sciences.

M. Brann, J. Gutkind, E. Currier, 1998, Oncogene.

Identification of novel selective V2 receptor non-peptide agonists.

M. Brann, F. Piu, J. Lameh, 2008, Biochemical pharmacology.

Functional importance of the Ala(116)-Pro(136) region in the calcium-sensing receptor. Constitutive activity and inverse agonism in a family C G-protein-coupled receptor.

M. Brann, P. Krogsgaard‐Larsen, H. Bräuner‐Osborne, 2000, The Journal of biological chemistry.

Relevance of 5-HT2A Receptor Modulation of Pyramidal Cell Excitability for Dementia-Related Psychosis: Implications for Pharmacotherapy

E. Burstein, 2021, CNS Drugs.

Molecular cloning and pharmacology of functionally distinct isoforms of the human histamine H(3) receptor.

D. Weiner, M. Brann, N. Nash, 2002, Neuropharmacology.

Lack of influence of cigarette smoking on triazolam pharmacokinetics.

D. Greenblatt, H. Ochs, E. Burstein, 1987, British journal of clinical pharmacology.

Pimavanserin augments the efficacy of atypical antipsychotic drugs in a mouse model of treatment-refractory negative symptoms of schizophrenia

H. Meltzer, E. Burstein, L. Rajagopal, 2021, Behavioural Brain Research.

II. In vitro evidence that (−)-OSU6162 and (+)-OSU6162 produce their behavioral effects through 5-HT2A serotonin and D2 dopamine receptors

U. Hacksell, A. Carlsson, E. Burstein, 2011, Journal of Neural Transmission.

Pimavanserin reverses multiple measures of anxiety in a rodent model of post-traumatic stress disorder.

E. Burstein, G. Moreno, D. Malin, 2022, European journal of pharmacology.

G-protein-coupled receptor-mediated activation of rap GTPases: characterization of a novel Galphai regulated pathway.

E. Burstein, Anthony Essex, J. Weissman, 2004, Oncogene.

Estrogen Receptor Beta Selective Agonists as Agents to Treat Chemotherapeutic-Induced Neuropathic Pain.

K. Mcfarland, R. Olsson, E. Burstein, 2016, ACS chemical neuroscience.

Lackofinfluence ofcigarette smoking ontriazolam pharmacokinetics

D. Greenblatt, H. Ochs, E. Burstein, 1987 .

Pimavanserin Promotes Trophic Factor Release and Protects Cultured Primary Dopaminergic Neurons Exposed to MPP+ in a GDNF-Dependent Manner.

E. Burstein, Dorothée Buttigieg, R. Steinschneider, 2021, ACS Chemical Neuroscience.

Chemical genomics: massively parallel technologies for rapid lead identification and target validation

Uli Hacksell, Norman Nash, Ethan S. Burstein, 2004, Cytotechnology.

The A-CD analogue of 16 beta,17 alpha-estriol is a potent and highly selective estrogen receptor beta agonist

A. Gustavsson, R. Olsson, E. Burstein, 2013 .

AC-260584, an orally bioavailable M1 muscarinic receptor allosteric agonist, improves cognitive performance in an animal model

K. Mcfarland, D. Bonhaus, J. Lameh, 2010, Neuropharmacology.