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Richard A. Glennon, Ph.D.


Professor
Chairman

Department of Medicinal Chemistry

Location:  Virginia Biotechnology Research Park, Suite 205
Phone: (804) 828-8487
Email: glennon@vcu.edu

Mailing Address

School of Pharmacy - Dept of Medicinal Chemistry
BioTech One, Suite 205
800 E. Leigh St.
P.O. Box 980540
Richmond, VA 23298-0540
Fax: (804) 828-7404


Education

  • M.S., Medicinal Chemistry (Northeastern University, 1969)
  • Ph.D., Medicinal Chemistry (State University of New York at Buffalo, 1973)

Post-Graduate Training

  • NIH Fellowship Post doctoral Fellowship (State University of New York, School of Medicine, 1975)

Academic Appointments/Professional Experience

  • 1983 - Present. Professor of Medicinal Chemistry and Affiliate Professor of Pharmacology, Virginia Commonwealth University
  • (1981 - 1983) Associate Professor of Medicinal Chemistry,
  • (1975 - 1981) Assistant Professor of Medicinal Chemistry,

Research Interests

  • Application of classical and contemporary (e.g. receptor graphics modeling) medicinal chemistry drug design techniques to develop 1) therapeutic agents for the potential treatment of central and neurological disorders (e.g. anxiety, depression, schizophrenia, Alzheimer’s disease), and 2) pharmacological tools (e.g. radioligands, selective agonists and antagonists, or autoradiographic and radioimaging agents) to interrogate drug-receptor interactions at G-protein coupled and ion channel receptors. More specifically, we utilize drug design, chemical synthesis, and preclinical evaluations using various functional assays (i.e., in vitro and in vivo techniques, such as radioligand binding and behavioral drug discrimination) to develop receptor selective- and receptor subtype-selective agents as agonists and/or antagonists (or partial agonists, inverse agonists) at selected receptor populations [e.g. serotonin 5-HT1 – 5-HT7 receptors, nicotinic (e.g. alpha4beta2 and other) cholinergic receptors, sigma receptors, imidazoline receptors]. Specific interests include modulation of DARPP by serotonergic ligands, classification and mechanism of action studies of drugs of abuse (e.g. classical hallucinogens, central stimulants, and certain designer drugs), and agonist-directed receptor trafficking. Other interests involve allosteric modulation of receptors by synthesis and evaluation of novel agents that act at receptor sites not utilized by standard orthosteric neuromodulators/neurotransmitters, receptor dimerization (homo- and hereto-dimerization), and application of classical SAR and QSAR techniques to determine what/how various structural features of drugs influence their receptor binding properties and pharmacological action.

Publications

PubMed Search
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  • Books/Book Chapters
    • Book chapters from the past five years:
    • 46. Glennon, R. A. Medicinal chemistry of alpha4beta2 nicotinic cholinergic receptor ligands, In: Progress in Medicinal Chemistry, Volume 42, Elsevier Science B. V., Amsterdam, 2004, 55-123.
    • 47. Glennon, R. A. Neurobiology of hallucinogens. In: Textbook of Substance Abuse Treatment, M. Galanter and H. D. Kleber, eds., American Psychiatric Publishing, Washington DC, 2004, pp 41-46.
    • 48. Ablordeppey, S. Y.; Glennon, R. A. Pharmacophore models for sigma1 receptor binding, In: Sigma Receptors, Chemistry, Cell Biology and Clinical Implications, Matsumoto, Rae, R.; Bowen, Wayne, D.; Su, Tsung-Ping (Eds.). 2007.
    • 49. Glennon, R. A. Strategies for the development of selective serotonergic agents. In: The Serotonin Receptors: From Molecular Pharmacology to Human Therapeutics, B. L. Roth, ed., Humana Press, NJ., 2008.
    • 50. Glennon, R. A. Hallucinogens, stimulants, and related drugs of abuse, In: Foye’s Textbook of Medicinal Chemistry, D. A. Williams and T. Lemke, eds., Williams and Wilkins, Baltimore, 2008. pp 631-651.
    • 51. Glennon, R. A.; Dukat, M. Serotonin receptors and drugs affecting serotonergic neurotransmission, In: Foye’s Textbook of Medicinal Chemistry, D. A. Williams and T. Lemke, eds., Williams and Wilkins, Baltimore, 2008. pp 417-443.
    • 52. Glennon, R. A. Neurobiology of hallucinogens. In: Textbook of Sub stance Abuse Treatment, M. Galanter and H. D. Kleber, eds., American Psychiatric Publishing, Washington DC, 2008, pp 181-189.
    • 53. Glennon, R. A. The pharmacology of classical hallucinogens and designer drugs. In: Principles of Addiction Medicine, A. W. Graham, T. K. Schultz, M. Mayo-Smith, R. K. Ries and B. B. Wilford, eds., American Society of Addiction Medicine, Chevy Chase, MD., in press.
    • 54. Glennon, R. A.[ Iverson, L. Antidepressants, In: Burger's Medicinal Chemistry and Drug Discovery, Nervous System Agents, D. J. Abraham, ed., Wiley: New York. 2003. In press.
  • Recent Publications
    • Representative publications from the past five years:
    • 308. Glennon, R. A.; Dukat, M.; alpha4beta2 nACh Receptor Pharmacophore Models. Bioorg. Med. Chem. Lett. 2004,14, 1841-1844.
    • 309. Glennon, R. A.; Dukat, M. Musings on alpha4beta2 nicotinic acetylcholine (nACh) receptor pharmacophore models. Curr. Topics Med. Chem. 2004, 4, 631-644.
    • 310. Glennon, R. A.; Grella, B.; Tyacke, R J.; Lau, A.; Westaway, J.; Hudson, A. L. Binding of ?-carbolines at imidazoline I2 receptors: Structure-affinity investigation. Bioorg. Med. Chem. Lett. 2004, 14, 999-1002.
    • 311. Chang-Fong, J.; Tyacke, R. J.; Lau, A.; Westaway, J.; Hudson, A. L.; Glennon, R. A. Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I2 receptor ligands. Bioorg. Med. Chem. Lett. 2004, 14, 1003-1005.
    • 312. Tyacke, R. J.; Lau, A.; Grella, B.; Glennon, R. A.; Nutt, D. J.; Hudson, A. L. Investigation of the affinities of two new ?-carbolines for rat brain imidazoline2 receptors. Ann. N. Y. Acad. Sci. 2004,1009, 361-363.
    • 313. Chang-Fong, J.; Rangisetty, J. B.; Dukat, M.; Setola, V.; Raffay, T.; Roth, B.; Glennon, R. A. 1,2,3,4-Tetrahydrocarbazoles as 5-HT6 serotonin receptor ligands. Bioorg. Med. Chem. Lett. 2004, 14, 1961-1964.
    • 314. Glennon, R. A.; Ismaiel, A. M.; Ablordeppey, S.; El-Ashmawy, M.; Fisher, J. B. Thioxanthene-derived analogs as sigma-1 receptor ligands. Bioorg. Med. Chem. Lett. 2004,14, 2217-2220.
    • 315. Dukat, M.; Smith, C.; Herrick-Davis, K.; Teitler, M.; Glennon, R. A. Binding of tryptamine analogs at h5-HT1E receptors: A structure-affinity investigation. Bioorg. Med. Chem. 2004, 12, 2545-2552.
    • 316. Khorana, N.; Pullagurla, M. R.; Young, R.; Glennon, R. A. Comparison of the discriminative stimulus effects of 3,4-methylenedioxymeth amphet- amine (MDMA) and cocaine: Asymmetric generalization. Drug Alcohol Depend. 2004, 74, 281-287.
    • 317. Dukat, M.; Taroua, M.; Dahdouh, A.; Siripurapu, U.; Damaj, M.; Martin, B. R.; Glennon, R. A. (?)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents. Bioorg. Med. Chem. Lett. 2004, 14, 3651-3654.
    • 318. Pullagurla, M. R.; Bondareva, T.; Young, R.; Glennon, R. A. Modulation of the stimulus effects of (+)amphetamine by the 5-HT6 antagonist MS-245. Pharmacol. Biochem. Behav. 2004, 78, 263-268.
    • 319. Pullagurla, M. R.; Westkaemper, R. B.; Glennon, R. A. Possible differences in modes of binding of agonist and antagonist binding at human 5-HT6 receptors. Bioorg. Med. Chem. Lett. 2004, 14, 4569-4573.
    • 320. Prisinzano, T.; Dukat, M.; Law, H.; Slassi, A.; MacLean, N. A.; DeLannoy, I.; Glennon, R. A. 2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands. Bioorg. Med. Chem. Lett. 2004, 14, 4697-4699.
    • 321. Khorana, N.; Pulagurla, M. R.; Dukat, M.; Young, R.; Glennon, R. A. Stimulus effects of three sulfur-containing psychoactive agents. Pharmacol. Biochem. Behav. 2004, 78, 821-826.
    • 322. Glennon, R. A. Nicotine and pain. Med. Chem. Res. 2004, 13, 74-77.
    • 323. Glennon, R. A.; Bondarev, M. L.; Khorana, N.; Young, R.; May, J. A.; Hellberg, R. R.; McLaughlin, M. A.; Sharif, N. A. ?-Oxygenated analogs of the 5-HT2A serotonin agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane (DOB). J. Med. Chem. 2004, 47, 6034-6041.
    • 324. Lee, M.; Rangisetty, J. B.; Pullagurla, M. R.; Dukat, M.; Setola, V.; Roth, B. L.; Glennon, R. A. 1-(1-Naphthyl)piperazines as a novel template for 5-HT6 serotonin receptor ligands. Bioorg. Med. Chem. Lett. 2005, 15, 1707-1711.
    • 325. Kolanos, R.; Siripurapu, U.; Pullagurla, M. R.; Riaz, M.; Setola, V.; Roth, B. L.; Glennon, R. A. Binding of iso-tryptamines and indenes at h5-HT6 serotonin receptors. Bioorg. Med. Chem. Lett. 2005, 15, 1987-1991.
    • 326. Setola, V.; Dukat, M.; Glennon, R. A.; Roth, B. L. Molecular determinants for the interaction of the vavulopathic anorexigen norfenfluramine with the 5-HT2B receptor. Mol. Pharmacol. 2005, 68, 20-33.
    • 327. Ramunno, A.; Dukat, M.; Lee, M.; Young, R.; El-Zahabi, M.; Damaj, M. I.; Martin, B.; Glennon, R. A. 6-(2-Phenylethyl)nicotine: A novel nicotinic cholinergic receptor ligand. Bioorg. Med. Chem. Lett. 2005, 15, 3237-3240.
    • 328. Abate, C.; Kolanos, R.; Dukat, M.; Setola, V.; Roth, B. L.; Glennon, R. A. Interaction of chiral MS-245 analogs at 5-HT6 receptors. Bioorg. Med. Chem. Lett. 2005, 15, 3510-3513.
    • 329. Dukat, M.; Ramunno, A.: Banzi, R.; Damaj, I. M.; Martin, B.; Glennon, R. A. 3-(2-Aminoethyl)pyridine analogs as ?4?2 nicotinic cholinergic receptor ligands. Bioorg. Med. Chem. Lett. 2005, 15, 4308-4312.
    • 330. Glennon, R. A. Pharmacophore identification for sigma1 receptor binding. Mini-Rev. Med. Chem. 2005, 5, 927-940.
    • 331. Pullagurla, M.; Dukat, M.; Roth, B. L.; Setola, V.; Glennon, R. A. 5-Azatryptamine analogs as h5-HT6 receptor ligands. Med. Chem. Res. 2005, 14, 1-18.
    • 332. Pullagurla, M.; Siripurapu, U.; Kolanos, R.; Bondarev, M. L.; Dukat, M.; Setola, V.; Roth, B. L.; Glennon, R. A. Binding of amine-substituted N1-benzenesulfonylindoles at human 5-HT6 serotonin receptors. Bioorg. Med. Chem. Lett. 2005, 15, 5298-5302.
    • 333. Young, R.; Khorana, N.; Bondareva, T.; Glennon, R. A. Pizotyline effectively attenuates the stimulus effects of N- methyl-3,4-methylenedioxyamphetamine (MDMA). Pharmacol. Biochem. Behav. 2005
    • 334. Glennon, R. A. Binding characteristics of sigma2 receptor ligands. Brazil. J. Pharm. Sci. 2005, 41,1-12.
    • 335. Bondareva, T.; Wesolowska, A.; Dukat, M.; Lee, M.; Young, R.; Glennon, R. A. S(+)- and R(-)N-methyl-1-(3,4-methylenedioxyphenyl)-2-aminopropane (MDMA) as discriminative stimuli: Effect of cocaine. Pharmacol Biochem Behav. 2005, 82, 531-538.
    • 336. Young, R.; Bondareva, T.; Wesolowska, A.; Glennon, R. A. Modulation of a (+)amphetamine discriminative stimulus in rats by 8-hydroxy-2-(N,N-di-n-propylamino)tetralin (8-OH DPAT). Pharmacol. Biochem. Behav. 2006, 83, 612-617.
    • 337. Siripurapu, U.; Kolanos, R.; Dukat, M.; Roth, B. L.; Glennon, R. A. Binding of methoxy-substituted N1-benzenesulfonylindole analogs at human 5-HT6 serotonin receptors. Bioorg. Med. Chem. Lett. 2006, 16, 3793-6.
    • 338. Young, R.; Rothman, R. B.; Rangisetty, J. B.; Partilla, J. S.; Dukat, M.; Glennon, R. A. TDIQ (5,6,7,8-tetrahydro-1,3-dioxolo[4,5-g]isoquinoline) inhibits the consumption of "snacks" in mice. Pharmacol. Biochem. Behav. 2006, 84, 74-83.
    • 339. Young, R.; Batkai,,S.; Dukat, M.; Glennon, R. A. TDIQ (5,6,7,8-tetrahydro-1,3-dioxolo[4,5-g]isoquinoline) exhibits anxiolytic-like activity in a marble-burying assay in mice. Pharmacol. Biochem. Behav. 2006, 84, 62-73.
    • 340. Ragab, H. M.; Kim, J. S.; Dukat, M.; Navarro, H.; Glennon, R. A. Aryloxyethylamines: binding at alpha7 nicotinic acetylcholine receptors. Bioorg. Med. Chem. Lett. 2006, 16, 4283-4276.
    • 341. Sikazwe, D.; Bondarev, M. L.; Dukat, M.; Rangisetty, J. B.; Roth, B. L.; Glennon, R. A. Binding of sulfonyl-containing arylalkylamines at human 5-HT6 serotonin receptors. J. Med. Chem. 2006, 49, 5217-5225.
    • 342. Kolanos, R.; Dukat, M.; Roth, B. L.; Glennon, R. A. Interaction of N1-unsubstituted and N1-benzenesulfonyltryptamines at h5-HT6 receptors. Bioorg. Med. Chem. Lett. 2006 16, 5832-5835.
    • 343. Young, R.; Bondareva, T.; Wesolowska, A.; Young, S.; Glennon, R. A. Effect of the 5-HT6 serotonin antagonist MS-245 on the actions of (-) nicotine. Pharmacol. Biochem. Behav. 2006 83, 612-617.
    • 344. Glennon, R. A.; Bondareva, T,; Young, R. ?-Ethyltryptamine (alpha-ET) as a discriminative stimulus in rats. Pharmacol. Biochem. Behav. 2006, 85, 448-453.
    • 345. Glennon, R. A. 3-(4-Tetrahydropyridin-1-yl)butyl)oxindoles as 5-HT7 receptor ligands. Expert Opin. Ther. Patents 2006, 16, 1171-1174.
    • 346. Nyandege, A.; Kolanos, R.; Roth, B. L.; Glennon, R. A. Further studies on the binding of N1-substituted tryptamines at h5-HT6 serotonin receptors. Bioorg. Med. Chem. Lett. 2007, 17. 1691-1694.
    • 347. Glennon, R. A.; Young, R.; Dukat, M.; Chang-Fong, J.; El-Zahabi, M. N-Methyl-1-(4-methoxyphenyl)-2-aminopropane (PMMA) and N-Methyl-1-(3,4-methylenedioxyphenyl)-2-aminopropane (MDMA) produce non-identical discriminative stimuli in rats. Pharmacol. Biochem. Behav. 2007 86, 477-484.
    • 348. Dukat, M.; Glennon, R. A.; Young, S. MD-354: what is it good for? CNS Drug Rev. 2007, 13, 1-20.
    • 349. Dukat, M.; Wesolowska, A.; Young, R.; Glennon, R. A. The 5-HT3 receptor partial agonist MD-354 (meta-chlorophenylguanidine) enhances the discriminative stimulus actions of (+)amphetamine in rats. Pharmacol. Biochem. Behav. 2007, 87, 203-207.
    • 350. Kim, J. S.; Padnya, A.; Weltzin, M.; Edmonds, B. W.; Schulte, M. K.; Glennon, R. A. Synthesis of desformylflustrabromine and its evaluation as an alpha4beta2 and alpha7 nACh receptor modulator. Bioorg. Med. Chem. Lett. 2007, 17, 4855-4860.
    • 351. De Oliviera, E.; Brandt, C. A.; Da Silviera, M. A.; Glennon, R. A. Synthesis of pyrrolidine-substituted benzamides via iodocyclization of beta-enaminoesters. Tetrahedron Lett. 2008, 48, 6393-6396.
    • 352. Young, R. A.; Glennon, R. A. MDMA (N-methyl-3,4-methylene- dioxyamphetamine) and its stereoisomers: Similarities and differences in behavioral effects in an automated activity apparatus in mice. Pharmacol. Biochem. Behav. 2008, 88, 318-331.
    • 353. Dukat, M.; Mosier, P. D.; Kolanos, R.; Roth, B. L.; Glennon, R. A. Binding of Serotonin and N1-Benzenesulfonyltryptamine-Related Analogs at Human 5-HT6 Serotonin Receptors: Receptor Modeling Studies. J. Med. Chem. 2008, 51, 603-611.
    • 354. Runyon, S. P.; Mosier, P. D.; Roth, B. L.; Glennon, R. A.; Westkaemper, R. B. Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation. J. Med. Chem. 2008, 51, 6808-6828.
    • 355. May, J. A.; Sharif, N. A.; Chen, H. H.; Liao, J. C.; Kelly, C. R.; Glennon, R. A.; Young, R.; Li, J. X.; Rice, K. C.; France, C. P. Pharmacological properties and discriminative stimulus effects of a novel and selective 5-HT2 receptor agonist AL-38022A [(S)-2-(8,9-dihydro-7H-pyrano[2,3-g]indazol-1-yl)-1-methylethylamine]. Pharmacol. Biochem. Behav. 2009, 91, 307-314.
    • 356. Khorana, N.; Young, R.; Glennon, R. A. Effect of 8-hydroxy-2-(N,N-di-n-propylamino)tetralin and MDMA on the discriminative stimulus effects of the classical hallucinogen DOM in rats. Pharmacol. Biochem. Behav. 2009, 91, 385-392.
    • 357. Young, R.; Glennon, R. A. S(-)Propranolol as a discriminative stimulus and its comparison to the stimulus effects of cocaine in rats. Psychopharmacology (Berl) 2009, 203, 369-382.
    • 358. Abate, C.; Mosier, P. D.; Berardi, F.; Glennon, R. A. A structure-affinity and comparative molecular field analysis of sigma-2 receptor ligands. Central Nerv. System Agents in Med. Chem. In press.
    • 359. Glennon, R. A.: Siripurapu, U.; Dukat, M.; Roth, B. L.; Kolanos, R.; Bond- arev, M. L.; Sikazwe, D.; Lee, M. The medicinal chemistry of 5-HT6 receptor ligands with a focus on arylsulfonyltryptamines. Curr. Topics Med. Chem. In press.