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) 855-2519
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. In 1980 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 300 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's current research interests include the development 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:
1. 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,.
2. Zhang A, Vliet AV, Neumeyer JL: Synthesis of Aminothiazole Derived Morphinans. Tetrahedron Lett. 2003, 44: 6459-6462.
3. Neumeyer JL, Kula NS, Bergman J, Baldessarini R: Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines. Eur. J. Pharmacol. 2003, 474, 137-140.
4. Neumeyer JL, Zhang A, Xiong W, Gu X, Hilbert JE, Knapp BI, Negus SS, Mello NK, Bidlack JM: Design and Synthesis of Novel Bivalent Morphinan Ligands for Opioid Receptors. J. Med. Chem. 2003, 46, 5162-5170,.
5. 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,.
6. Zhang A, Xiong X, Hilbert JE, DeVita EK, Bidlack JM, and Neumeyer JL, 2-Aminothiazole-Derived Opioids –Bioisosteric Replacement of Phenols, J. Med. Chem. 2004, 47, 1886-1888,.
7. Zhang A, Xiong X, Bidlack JM, Hilbert JE, Knapp BI, Wentland MP and Neumeyer JL, 100-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed ? and ? opioid ligands: Aynthesis and biological evaluation of their binding affinity at opioid receptoes. J Med Chem 2004, 47, 165-174,
8. 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,.
9. 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.
10. Zhang, A., Csutoras, C., Zong, R. and Neumeyer, J.L.: Synthesis of 2-fluoro-11-hydroxy-N-propylnoraporphine: A potential dopamine D2 agonist. Organic Letters, 2005, 7, 3239-3242.
11. 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, ?, and ? opioid receptors. J. Med. Chem. 2006, 49, 256-262.
12. 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.
13. 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 psychiatric disorders. Chem. Revs., 2007, 107, 274-302.
14. 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.
15. Peng, X. and Neumeyer, J.L.: Kappa receptor bivalent ligands. Current Topics in Medicinal Chemistry, 2007, 7, 363-373.
16. Desai, R.I., Neumeyer, J.L., Paronis, C.A., Ngyuyen, P. and Bergman, J.: Behavioral effects of the R-(+)- and S-(-) enantiomers of the D1-like partial receptor agonist SKF 83959 in monkeys. European Journal of Pharmacology, 2007, 558, 98-106.
17. 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.
18. Wuest, F., Berndt, M., Strobel, K., van den Hoff, J., Peng, X., Neumeyer, J.L. and Bergmann, R.: Synthesis and radiopharmacological characterization of 2?-carbo-2’-[18F]fluoroethoxy-3?-(4-bromo-phenyl)tropane ([18F]MCL-322) as a novel PET radiotracer for imaging the dopamine transporter (DAT). Bioorganic & Medicinal Chemistry, 2007,15, 4511-4519.
19. Peng, X., Knapp, B.I., Bidlack, J.M. and Neumeyer, J.L.: Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone and naloxone at ?, ?, and ? opioid receptors. J. Med. Chem. 2007, 50, 2254-2258.
20. Peng, X., Knapp, B.I., Bidlack, J.M. and Neumeyer, J.L.: In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors. Bioorganic Medicinal Chemistry 2007, 15, 4106-4112.
21. 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-aporphines as 5-HT1A receptor ligands. Bioorganic & Medicinal Chemistry Letters 2007, 17, 4128-4130.
22. 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
23. 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.(in press)