JOHN L. NEUMEYER, PHD
- McLean title(s): Director and Professor (Emeritus), Harvard Medical School, McLean Hospital
- Email: jneumeyer@mclean.harvard.edu
- Telephone: (617) 855-3388
- Fax: (617) 855-3887
- Office Address: Alcohol and Drug Abuse Research Center, Medicinal Chemistry Laboratory
- Bio: Dr. Neumeyer received a B.S. degree from Columbia University and Ph.D. in Medicinal Chemistry from University of Wisconsin, Madison, WI in 1961. He began his career as a Research Scientist at Ethicon, Inc., a division of Johnson and Johnson, FMC Corp and Arthur D. Little, Inc. and joined the faculty at Northeastern University in 1969 as Professor of Medicinal Chemistry and Chemistry. He was appointed Matthews Distinguished Professor in 1980, when he co-founded Research Biochemicals International, a chemical company which provided ligands for neuroscience research. Dr. Neumeyer has had a long and creative career in Medicinal Chemistry that is summarized in more than 400 refereed scientific publications. At present, he continues his research activities at Harvard Medical School, the Alcohol and Drug Abuse Research Center at McLean Hospital where he is the Director of the Medicinal Chemistry Program. Dr. Neumeyer was inducted into the American Chemical Society Division of Medicinal Chemistry Hall of Fame in 2008. Dr. Neumeyer's current research interests include the synthesis and evaluation of novel aporphines and benzazepines as D2 and D1 agonists for the treatment of Parkinson's Disease; the development of morphinans with mixed kappa/mu activities as potential medications for the treatment of drug abuse, and the development of brain imaging agents using PET, SPECT and MRI.
- Publications:
- Zhang A, Neumeyer JL: Microwave-Promoted Pd-Catalyzed Cyanation of Aryl Triflates: A Fast and Versatile Access to 3-Cyano-3-desoxy-10-ketomorphinans. Organic Lett. 2003, 5,201-203.
- Zhang A, Vliet AV, Neumeyer JL: Synthesis of Aminothiazole Derived Morphinans. Tetrahedron Lett. 2003, 44: 6459-6462.
- Neumeyer JL, Kula NS, Bergman J, Baldessarini R: Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines. Eur. J.Pharmacol. 2003, 474, 137-140.
- Neumeyer JL, Zhang A, Xiong W, Gu X, Hilbert JE, Knapp BI, Negus SS, Mello NK,Bidlack JM: Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors. J. Med. Chem.2003, 46, 5162-5170.
- Csutoras C, Zhang A, Zhang K, Kula NS, Baldessarini RJ, Neumeyer JL:Synthesis and neuropharmacological evaluations of substituted R-(-)-11-hydroxyaporphines. Bioorganic and Med. Chem. 2004,3553-3559.
- Zhang A, Xiong X, Bidlack JM, Hilbert JE, Knapp BI, Wentland MP and Neumeyer JL,10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kand m opioid ligands: Synthesis and biological evaluation of their binding affinity at opioid receptors. J Med Chem 2004, 47,165-174.
- Peng X, Zhang A, Kula NS, Baldessarini J and Neumeyer JL,Synthesis and amine transporter affinities of novel phenyltropane derivatives as positron emission tomography (PET) imaging agents. Bioorganic and Med Chem Lett. 2004, 14, 5635-5639.
- Zhang, A., Kula, N.S.,Zhang, K, Baldessarini, R.J., Kaufman, M.J., Renshaw, P.F., and Neumeyer,J.L.: Development of polyfluorophenyltropanes: Potential probes for 19F magnetic resonance imaging (MRI) and spectroscopy(MRS) assessments of the dopamine transporter. Letters in Drug Design & Discovery, 2005, 2, 302-306. DOI: 10.2174/1570180054038332
- Zhang, A., Csutoras, C., Zong, R. and Neumeyer, J.L.:Synthesis of 2-fluoro-11-hydroxy-N-propylnoraporphine: A potentialdopamine D2 agonist. Organic Letters, 2005, 7,3239-3242.
- Peng, X., Knapp, B.I.,Bidlack, J.M. and Neumeyer, J.L.: Synthesis and preliminary in vitro investigation of bivalent ligands containing homo-and heterodimeric pharmacophores at µ, δ, and κ opioid receptors. J.Med. Chem. 2006, 49, 256-262. DOI: 10.1021/jm050577x
- Neumeyer, J.L., Peng, X., Knapp, B.I., Bidlack, J.M., Lazurus, L.H., Salvadori, S.,Trapella, C. and Balboni, G.: New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores. J. Med.Chem. 2006, 49, 5640-5643.
- Zhang, A., Neumeyer, J.L. and Baldessarini, R.J.:Recent progress in development of dopamine receptor subtype-selective agents: Potential therapeutic agents for neurological and psychiatricdisorders. Chem. Revs., 2007, 107, 274-302.
- Zhang, A., Zhang, Y., Branfman, A.R., Baldessarini, R.J. and Neumyer, J.L.:Advances in development of dopaminergic aporphinoids. A J. Med.Chem. 2007, 50, 171-181.
- Peng, X. and Neumeyer, J.L.: Kappa receptor bivalent ligands. CurrentTopics in Medicinal Chemistry, 2007, 7, 363-373.
- Peng, X., Knapp, B.I., Bidlack, J.M. and Neumeyer, J.L.:High-affinity carbamate analogues of morphinan at opioid receptors. Bioorganic& Medicinal Chemistry Letters, 2007, 17, 1508-1511.
- Wuest, F., Berndt, M.,Strobel, K., van den Hoff, J., Peng, X., Neumeyer, J.L. and Bergmann, R.: Synthesis and radiopharmacological characterization of 2β-carbo-2'-[18F]fluoroethoxy-3β-(4-bromo-phenyl)tropane ([18F]MCL-322) asa novel PET radiotracer for imaging the dopamine transporter (DAT). Bioorganic & Medicinal Chemistry, 2007,15, 4511-4519.
- Peng, X., Knapp, B.I., Bidlack, J.M. and Neumeyer, J.L.: Pharmacologicalproperties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone and naloxone at σ, δ, and κ opioid receptors. J. Med. Chem. 2007, 50, 2254-2258.
- Peng, X., Knapp, B.I., Bidlack, J.M. and Neumeyer, J.L.: In-vitro investigation of oxazol and urea analogues of morphinan at opioidreceptors. Bioorganic Medicinal Chemistry 2007, 15, 4106-4112.
- Si, Y.-G., Gardner, M.P., Tarazi, F.I., Baldessarini, R.J. and Neumeyer, J.L.:R-(—)-N-alkyl-11-hydroxy-10-hydroxymethy1- and 10-methyl-aporphinesas 5-HT1A receptor ligands. Bioorganic & Medicinal ChemistryLetters 2007, 17, 4128-4130.
- Si,Y-G. and Neumeyer, J.L.:Facile synthesis of 2-methoxy-11-hydroxyaporphine: A potential dopamine D1.receptor ligand.Synthesis, 2007,24,3787-3790.
- Si, Y-G., Gardner,M.P.,Tarazi,F.I.,Baldessarini,R.J.: Synthesis and dopamine receptor affinities of N-alkyl 11-hydroxy-2-methoxynoraporphine: N-Alkyl substituents determine D1 versus D2 Receptor selectivity. J.Med Chem. 2008, 51(4),983-7.
- Fulton B.S., Knapp,B.I., Bidlack J.M.,Neumeyer J.L.: Synthesis and pharmacological evaluation of hydrophobic esters and ethers of butorphanol at opioid receptors. Bioorg. Med. Chem. Lett. 2008, 18, 4474-4476.
- Mathews, J.L., Fulton, B.S., Negus, S.S., Neumeyer, J.L. and Bidlack, J.M.: In vivo characterization of (-)(-)MCL-144 and (+)(-)MCL-193: Isomeric, bivalent ligands with mu/kappa agonist properties. Neurochem. Res. 2008, 33, 2142-2150.
- Si, Y.-G., Gardner, M.P., Tarazi, F.I., Baldessarini, R.J. and Neumeyer, J.L.: Synthesis and binding studies of 2-O-and 11-O-substituted N-alkylnoraporphines. Bioorganic & Medicinal Chemistry Letters, 2008, 18, 3971-3973.
- Decker, M., Fulton, B.S., Zhang B., Knapp, B.I., Bidlack, J.M. and Neumeyer, J.L.: Univalent and bivalent ligands of butorphan: Characteristics of the linking chain determine the affinity and potency of such opioid ligands. J. Med Chem., 2009, 52, 7389-7396.
- Decker, M., Si, Y.-G., Knapp, B.I., Bidlack, J.M. and Neumeyer, J.L.: Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: Ligands for mu, kappa and delta opioid receptors. J. Med Chem., 2009, 52, (DOI: 10.1021/jm9013482).
- Balboni, G.; Salvadori, S.; Trapella, C.; Knapp, B. I.; Bidlack, J. M.; Lazarus, L. H.; Peng, X.; Neumeyer, J. L. Evolution of the Bifunctional Lead µ Agonist/δ Antagonist Containing the 20,60-Dimethyl-L-tyrosine-1,2,3,4-Tetrahydroisoquinoline-3-carboxylic Acid (Dmt-Tic) Opioid Pharmacophore. ACS Chem. Neurosci. 2009, (DOI: 10.1021/cn900025j).
