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Recent Publications

Last updated: June 20, 2020


  1. Behavorial Effects of the Benzodiazepine-Positive Modulator SH-053-2′F-S-CH3 in an Immune-Mediated Neurodevelopmental Disruption Model,” Richetto, J.; Labouesse, M.; Poe, M.M.; Cook, J.M.; Grace, A.; Riva, M.; Meyer, U., J. of Neuropsychopharmacology, 1-11 (2015).
  2. “Triple Monoamine Uptake Inhibitors Demonstrate a Pharmacologic Association Between Excessive Drinking and Impulsivity In High Alcohol-Preferring (HAP) Mice,” O’Tousa, S.; Warnock, K. T.; Matson, L. M.; Namjoshi, O. A.; Van Linn, M. L.; Tiruveedhula, V.V.; Halcomb, M.E.; Cook, J. M.; Nicholas J. Grahame, N. J.; June, H. L., Addiction Biology, 20, 236-247 (2015). DOI: 10.1111/adb.12100.
  3. “A Review: Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model”, Clayton, T.; Poe, M.; Rallapalli, S.; Biawat, P.;Savic, M.; Rowlett, J.; Gallos, G.; Emala, C.; Kaczorowski, C.; Stafford, D.; Arnold, L.; Cook, J. M., Int J.Med.Chem., Volume 2015, Article ID 430248, http//
  4. “Regulating Anxiety with Extrasynaptic Inhibition,” Botta, P.; Demmou, L.; Xu, C.; Lu, T.; Poe, M.M.; Xu, L.; Cook, J.M.; Rudolph, U.; Sah, P.; Luthi, A., doi: 10.1038/nn.4102. Nature Neuroscience, 18, 1493-1499 (2015).
  5. “First Stereospecific Total Synthesis of (-)-Affinisine Oxindole as well as Facile Entry Into the C (7) – Diastereomeric Chitosenine Stereochemistry, “Fonseca, G.; Wang, Z.; Namjoshi, O.; Deschamps, J.’ Cook, J.; Tetrahedron Lett, 56,3052-3056 (2015).
  6. “Anti-tumor Activity of 3-Indolylmethanamines 31B and PS121912”, Guthrie, M.; Preetpal, S; Hill, E.; Horan, T.; Premchendar, N.; Teske, K.; Yuan, N.; Gutherie, L.; Sidorko, M.; Kodali, R.; Cook, J.; Han, L.; Silvaggi, N.; Bikle, D.; Moore, R.; Singh, R.; Arnold, A.; Anticancer Res 35(11), 6001-6007 (2015.)
  7. “Pharmacokinetic/Toxicity Properties of the New Anti-Staphylococcal Lead Compound SK-03-92,” Schwan, W.; Kolesar, J.; Kabir, M.S.; Elder Jr, E.; Williams, J.; Minerath, R.; Cook, J.M.; Witzigmann, C.; Monte, A.; Flaherty, T.; Antibiotics, 4, 617-626 (2015).
  8. “Targeting the γ-Aminobutyric Acid A Receptor α4 Subunit in Airway Smooth Muscle to Alleviate Bronchoconstriction”, Yocum, G.T., Gallos, G., Zhang, Y., Jahan, R., Stephen, M.R., Varagic, Z., Puthenkalam, R., Ernst, M., Cook, J.M. and Emala, C.W., American Journal of Respiratory Cell and Molecular Biology, 54(4), pp.546-553 (2016), doi: 10.1165/rcmb.2015-0176OC.
  9. “Effects of Hz-166, A Novel α2 and α3 Subunit-containing GABA(A) Receptor Agonist, On Inflammatory Pain and Operant Behavior in Mice, “Fischer, B.; Kroll, C.; Poe, M.; Cook, J.; Abstracts Drug and Alcohol Dependence, 146, e278 (2015).
  10. “Genetic and Pharmacological Manipulation of Glyoxalase 1 Regulates Voluntary Ethanol Consumption in Mice,” McMurray, K.; Sidhu, P.; Arnold, A.; Cook, J.; Palmer, A., Addiction Biology, org/10.1111/adb.12333, Dec 2015.
  11. “Indentification of a Repressor of Staphylococcal Sortase Sensor(RssS) / Regulator (RssR) Rwo-Component Regulatory System tied to Drug Persistence and Represiion of The Staphylococcal aureus Sortase Gene,” Chwan, W.; Medina-Beilski, S.; Baker, A.; Lane, M.; Cook, J.; Kabir.; Shahjahan, M. Microbiology, submitted.
  12. “Sex-dependent Rapid Mild Antidepressant Activity of an α5 Subunit Containing GABA(A) Receptor Positive Allosteric Modulator in The Mouse Unpredictable Chronic Mild Stress Mode,” Piantadosi, S.; French, B.; Poe, M.; Timic, T.; Markovic, B.; Pabba, M.; Seney, M.; Savic, M.; Cook, J.; Sibille, E.; Frontiers in Pharmacology, 7 (Article 446), doi: 10.3389/fphar.2016.00446 (2016).
  13. “Synthesis of Aza and Carbocyclic β-Carbolines for The Treatment of Alcohol Abuse. Regiospecific Solution to the Problem of 3, 6-Disubstitued β-and Aza- β-Carboline Specificity,” Tiruveedhula, V.V.N, Methuku, K,; Deschamps, J.; Cook, J.; and Bimol. Chem, 13, 10705-10715 (2015).
  14. “Influence of Nigerian Honey on CYP3A4 Biotransformation of Quinine in Health Volunteers.” Igbinoba, S.; Akanmu, M.; Onyeji, C.; Soyinka, J.; Owolabi, A.; Nathaniel, Ti.; Pullela, S.; Cook, J.; J of Clin Pharmacy and Therapeutics, 40, 545-549 (2015), doi:10.0000/jcpt.12303.
  15. “Ester to Amide Substitution Improves Selectivity, Efficacy and Kinetic Behavior of a Benzodiazepine Positive Modulator of GABA(A) Receptors Containing the α5 Subunit,” Stamenić, T.; Poe, M.; Rehman, S.; Santrać, A.; Divović, B.; Scholze, P.; Ernst, M.; Cook, J.; Savic, M.; J. Pharmacol.,791, 433-433 (2016).
  16. “Metabolic Studies of Drug Candidates for Neurological Disorders and Asthma Based on GABAA Receptor Subtype Selective Ligands Using Mass Spectrometry”, Kodali, R.; Guthrie, M.; Poe, M.; Stephen, M.; Jahan, R.; Emala, C.; Cook, J.M.; Stafford, D.; Arnold, L., Shimadzu Journal, Vol.3, Issue3-Dec 2015.
  17. “Effect of Dehusked Garcinia Kola Seed on the Overall Pharmokinetics of Quinine in Healthy Human Volunteers,” Igbinoba, S.; Onyeji, C.; Akanmu, M.; Soyinka, J.; Owolabi, J.; Puellea, S.; Savina, V.V.; Cook, J.M., Clin.Pharmacol.,55, 348-354 (2015).
  18. “Antagonism of Triazolam Self-Administration in Rhesus Monkeys Responding Under a Progressive-ratio Schedule: In vivo Apparent pA2 Analysis,” Fischer, B; Platt, D.; Rallapalli, S.; Namjoshi, O.; Cook, J.; Rowlett, J.; Drug and Alcohol Dependence, 158, 22-29 (2016).
  19. “eEF2 Pathway Controls Dentrate Gyrus Dependent Behaviour and Excitation-inhibition Balance,” Heise, C.; Taha, E.; Murru, L.; Ponzoni, L.; Cattaneo, A.; Guarnieri, F.C.; Montani, C.; Mossa, A.; Vezzoli, E.; Ippoliot, G.; Zapata, J.; Berrera, I.; Ryazanov, A.G.; Benfante, R.; Braida, D.; Francolinin, M.; Proud, Poe, M.M.; Stephen, M.; Cook, J.M.; C.; Valtorta, F.; Passafaro, M.; Sala, M.; Bachi, A.; Verpelli, C.; Rosenblum, K.; Sala, C.; Cerebral Cortex, doi: 10.1093/cercor/bhw075, 27, 2226-2248 (2017).
  20. “First in Vivo Testing of Novel Compounds Targeting Group 3 Medulloblastomas Using an Implantable Microdevice as a New Paradigm for Drug Development,” Jonas, O.; Calligaris, D.; Methuku, K.; Poe, M.M,; Tranghese, F.; Changelian, A.; Francois, J.; Sieghart, W.; Ernst, M.; Krummel, D.; Cook, J.M.; Pomeroy, S.; Cima, M.; Agar, N.; Langer, R.; Sengupta, S.; J. of Biomedical Nanotechnology, 12, 1297-1302 (2016).
  21. “Effects of the Benzodiazepine GABAA α1-Preferring Antagonist 3-Isopropoxy-β-Carboline Hydrochloride (3-ISOPBC) on Alcohol Seeking and Self-Administration in Baboons,” Holtyn, A., Tiruveedhula V.V.N., Stephen MR, Cook J.M., Weerts EM.; Drug and Alcohol Dependence, 170, 25-31 (2017).
  22. “Sarpagine and Related Alkaloids,” O. Namjoshi; J.M. Cook, in “The Alkaloids,” Volume 76, Hans-Joachim Knölker, Editor, Elsevier, N.Y. pp. 64-171 (2016).
  23. “Synthesis and Evaluation of Vitamin D Receptors-mediated Activities of Cholesterol and Vitamin D Metabolites,” Teske, K.; Bogart, J.; Sanchez, L.; Yu, O.; Preston, J.; Cook, J.; Silvaggi, N.; Bikle, D.; Arnold, L.; J. Med. Chem, 109, 238-246 (2016).
  24. “Development of GABAA Receptor Subtype-Selective Imidazobenzodiazepines as Novel Asthma Treatments”, Forkuo, G.S.; Guthrie, M.; Yuan, N; Nieman, A.; Kodali, R; Jahan, R; Yocum, G.; Treven, M.; Stephen, M.; Poe, M.; Li, G.; Yu, O.; Hartzler, B.; Zahn, N.; Ernst, M.; Emala,C.; Stafford, D.; Cook, J.M.; Arnold, L.A., Molecular Pharmaceutics, (ACS), DOI: 10.1021/acs.molpharmaceut.6600159; 13, 2026-2038 (2016).
  25. “Neonatal Bladder Inflammation Induces Long-term Visceral Pain and Altered Responses of Spinal Neurons in Adult Rats”, Kannampalli, P.; Babygirija,R.’ Zhang,J.; Poe,M.; Li,G.; Cook, J.M.; Shaker,R.; Banerjee, B.; Sengupta, J.; Neuroscience, (2017); 346, 349-364, PMID: 28126369 PMCID: PMC5337157 (2017).
  26. “Modern Methods for Total Synthesis of Important Oxindole Alkaloids”, Fonseca, G.; Cook, J.M.; Organic Chemistry Insights 2016: 6 1-55 DOI: 10.4137/OCI.S17958.
  27. “Early Life Stress is a Risk Factor for Excessive Alcohol Drinking and Impulsivity in Adults and is Mediated via a CRF/GABAA Mechanism”, Gondré-Lewis, M.C., Warnock, K.T., Wang, H., June Jr, H.L., Bell, K.A., Rabe, H., Tiruveedhula, V.V.N.P.B., Cook, J., Lüddens, H., Aurelian, L. and June Sr, H.L., 2016. Stress, 19(2), pp.235-247, DOI: 10.3109/10253890.2016.1160280 (2016).
  28. “Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABAA) Receptor Ligand that Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy”, Poe, M.; Methuku, K.; Li, Guanguan; Verma, A.; Teske, K.; Stafford, D.; Arnold, L.A.; Cramer, J.; Jones, T.; Cerne, R.; Krambis, M.; Witkin, J.; Jambrina, E.;  Rehman, S.;  Ernst, M.; Cook, J.M.; and Schkeryantz, J.; Med. Chem, 59, 10800-10806 (2016).
  29. “Total Synthesis of Macrocarpine D and E via an Enolate-Driven Copper-Mediated Cross-Coupling Process: Replacement of Catalytic Palladium with Copper Iodide”, Rahman, Md. T.; Deschamps, J.; Schwabacher, A.; Cook, J.M.; Org Lett., 18, 4174-4177 (2016).
  30. “Brain Vaculation Resulting from Administration of Low Impact (Type II) AmpaKines are an Artifact Related to AMP aKine Molecular Structure”, Purcell, R.; Lynch, G.; Gill, C.; Johnson, S.; Sheng, Z.; Stephen, M.R.; Garman, R.; Jorther, B.; Bolon, B.; Lippa, A., Toxicol Sci., 162(2):383-395. doi: 10.1093/toxsci/kfx277, 04/01/2018, PMID: 29253237.
  31. “Pharmacological and Antihyperalgesic Properties of the Novel α2/α3 Prefering GABA(A) Receptor Ligand MP-III-024”, Fischer B.; Schlitt, R.; Hamade, B. Z.; Rehman, S.; Ernst, M.; Poe, M.; Li, G.; Kodali, R.; Arnold, L.A.; Cook, J.M., Brain Res., Bull., doi: 10.1016/j. brainresbull.2017.03.001 (2017).
  32. “Antinociceptive Effects of a Novel α2/α3-Subtype Selective GABAA Receptor Positive Allosteric Modulator”, Lewter L.; Fisher J.; Siemian J.; Methuku K.; Poe M.; Cook J.M.; Li J., ACS Chem Neurosci, 2017 Jun 21;8(6):13-05-1312 PMID: 28150939 PMCID: PMC5686453 02/06/2017.
  33. “Characterization of GABAA Receptor Ligands with Automated Patch-Clamp Using Human Neurons Derived from Pluripotent Stem Cells”, Yuan, N.Y.; Poe, M.M.;  Witzigmann, C.; Cook, J.M.; Stafford, D.C.; Arnold,  A., J Pharmacol Toxicol Methods, doi. Org/ 10.1016/j. vascn.2016.08.006 (2016); 82: 109-114 (2016).
  34. “Optimization of Substituted Imidazobenzodiazepines as Novel Asthma Treatments”, Jahan, R.; Stephen, M.R.; Forkuo, G.S.; Kodali, R.; Guthrie, M.L.; Nieman, A.N.; Yuan, N.Y.; Zahn, N.M.; Poe, M.M.; Li, G.; Yu, O.B.; Yocum, G.T.; Emala, C.W.; Stafford, D.C.; Cook,  M.; Arnold,  L.A., Eur J. Med. Chem., doi: 10.1016/j.ejmech.2016.11.045, 126, 550-560 (2017).
  35. “Synthesis of Bisindole Alkaloids from The Apocynaceae Which Contain a Macroline or Sarpagine Unit: A Review”, Rahman, M.T.; Tiruveedhula, V.V.N.; Cook, J.M., Molecules, 2016, 21, 1525; doi: 10.3390/molecules21111525 (2016).
  36. “Benzodiazepine Ligands with Improved α5 Selectivity and Their Airway Smooth Muscle Relaxant Effect”, Puthenkalam, R.; Treven, M.; Ramerstorfer, J.; Steudle, F.; Scholze, P.; Gallos, G.; Poe, M.M.; Methuku, K.R.; Li, Guanguan; Arnold, L.A.; Seighert, W.; Santrac, Anja.; Savic, M.; Emala, C.; Cook, J.M.; Ernst, M., Pharmacology, 00,0000-0000 (2017).
  37. “Alleviation of Multiple Asthmatic Pathologic Features with Orally Available and Subtype Selective GABAA Receptor Modulators”, Forkuo GS, Nieman AN, Yuan NY, Kodali R, Yu OB, Zahn NM, Jahan R, Li G, Stephen MR, Guthrie ML, Poe MM, Hartzler BD, Harris TW, Yocum GT, Emala CW, Steeber DA, Stafford DC, Cook JM, Arnold LA, Mol Pharm, doi: 10.1021/acs.molpharmaceut.7b00183, 14(6):2088-2098, PMID: 28440659, PMCID: PMC5497587, 2017.
  38. “Trigeminal neuropathic pain development and maintenance in rats are suppressed by a positive modulator of α6 GABAA receptors”, Vasović, D.; Divović, B.; Treven, M.; Knutson, D.; Steudle, F.; Scholze, P.; Obradović, A.; Fabjan, J.; Brković, B.; Seighart, W.; Ernst, M.; Cook, J.M.; Savić, M., J. Pain.,, 23:973-984, Jan 2019.
  39. “Cerebellar α6 subunit‐containing GABAA receptors: A novel therapeutic target for disrupted prepulse inhibition in neuropsychiatric disorders”, Lee, H.-J.; Ernst, M.; Huang, W.-J.; Chiou, J.-F.; Chen, H.-L.; Mouri, A.; Chen, L.-C.; Mamiya, T.; Fan, P.-C.; Knutson, D.; Witzigmann, C.; Cook, J.; Seighart, W.; Nabeshima, T.; Chiou, L.-C.; J. Pharmacol,, March 2018.
  40. “Abuse-related effects of subtype-selective GABAA receptor positive allosteric modulators in an assay of intracranial self-stimulation in rats”, meyer KL, Li G, Poe MM, Cook JM, Banks ML, Stevens Negus S, Psychopharmacology (Berl), 2017 July ; 234(14): 2091–2101. doi:10.1007/s00213-017-4615-8.
  41. “Further evaluation of the potential anxiolytic activity of imidazo[1,5-a][1,4]diazepin agents selective for α2/3-containing GABAA receptors”, Witkin JM, Cerne R, Wakulchik M, S J, Gleason SD, Jones TM, Li G, Arnold LA, Li JX, Schkeryantz JM, Methuku KR, Cook JM, Poe MM, Pharmacol Biochem Behav 2017 Jun;157:35-40 PMID: 28442369 PMCID: PMC5519285 04/27/2017.
  42. “Negative allosteric modulation of alpha 5-containing GABAA receptors engenders antidepressant-like effects and selectively prevents age-associated hyperactivity in tau-depositing mice”, Xu, N.; Ernst, M.; Cerne, R.; Wakalchik, M.; Li, X.; Jones, T.; Gleason, S.; Morrow, D.; Schkeryantz, J.; Rahman, Md.T.; Li, G.; Poe, M.; Cook, J.M.; Witkin, J., Psychopharmacology, DOI: org/10.1007/s00213-018-4832-9, 235 (4), 1151–1161, 2018.
  43. “Positive modulation of α5 GABAA receptors in preadolescence prevents reduced locomotor response to amphetamine in adult female but not male rats prenatally exposed to lipopolysaccharide”, Batinić B, Santrač A, Jančić I, Li G, Vidojević A, Marković B, Cook JM, Savić MM, Int J Dev Neurosci 2017 Oct;61:31-39 PMID: 28610974 PMCID: PMC5563212 06/15/2017.
  44. “Evidence that Sedative Effecst of Benzodiazepines Involve Unexpected GABAA Receptor Subtypes: Quantitative Observation Studies in Rhesus Monkeys”, Meng, Z.; Duke, A.; Platt, D.; Li, Guanguan; Stephen M.R.; Tiruveedhula, V.V.N.; Cook, J.; Rowlett, J., Neuropharmacology, submitted.
  45. “Concise Total Synthesis of (-)-Affinisine Oxindole, (+)-Isoalstonisine, (+)-Alstofoline, (-)-Macrogentine, (+)-Na -Demethylalstonisine, (-)-Alstonoxine A, and (+)-Alstonisine”, Stephen MR; Rahman MT; Tiruveedhula VVNPB; Fonseca GO; Deschamps JR; Cook JM, Eur. J., DOI: 10.1002/chem.201703572, 2017 Nov 07, 23(62):15805-15819, PMID: 28875520 09/07/2017.
  46. “Identification of Staphylococcus aureus Cellular Pathways Affected by the Stilbenoid Lead Drug SK-03-92 Using a Microarray”, Schwan WR, Polanowski R, Dunman PM, Medina-Bielski S, Lane M, Rott M, Lipker L, Wescott A, Monte A, Cook JM, Baumann DD, Tiruveedhula VVNPB, Witzigmann CM, Mikel C, Rahman MT, Antibiotics 2017 Sep 11;6(3) PMID: 28892020 PMCID: PMC5617981 09/12/2017.
  47. “Neurobiological correlates of state-dependent context fear”, Meyer MAA, Corcoran KA, Chen HJ, Gallego S, Li G, Tiruveedhula VV, Cook JM, Radulovic J, Learn Mem, DOI: 10.1101/lm.045542.117, 2017 Sep; 24(9):385-391, PMID: 2881-4463,  PMCID: PMC5580530 08/18/2017.
  48. “Identification of a novel, fast-acting GABAergic antidepressant”, McMurray, K.M.; Ramaker, M.J.; Barkley-Levenson, A.M.; Sidhu, P.S.; Elkin, P.K.; Reddy, M.K.; Guthrie, M.L.; Cook, J.M.; Rawal, V.H.; Arnold, L.A.; Dulawa, S.C.; Palmer, A.A., Mol Psychiatry., doi:10.1038/mp.2017.14, PMID: 28322281, PMCID: PMC5608625, March 2017.
  49. “Total Synthesis of Sarpagine Related Bioactive Indole alkaloids”, Rahman, M. T.; Deschamps, J. R.; Imler, G. H.; Cook, J. M., Eur. J., doi: 10.1002/chem.201705575, 24 (10), 2354-2359, 02/06/2018.
  50. “The α6 subunit-containing GABAA receptor: A novel drug target for inhibition of trigeminal activation”, Fan, P.C.; Lai, T.H.; Hor, C.C.; Lee, M.T.; Huang, P.; Sieghart, W.; Ernst, M.; Knutson, D.E.; Cook, J.; Chiou, L.C., Neuropharmacology, doi: 10.1016/j.neuropharm.2018.07.017, 2018, September; 140: 1-13.
  51. “A novel orally available asthma drug candidate that reduces smooth muscle constriction and inflammation by targeting GABA(A) receptors in the lung”, Forkuo G.; Nieman, A.; Zahn, N.; Kodali, R.; Li, G.; Roni, S.; Stephen, M.; Harris, T.; Jahan, R.; Guthrie, M.; Yu, O.; Fisher, J.; Yocum, G.; Emala, C.; Steeber, D.; Stafford, D.; Cook, J.; Arnold, L., Molecular Pharmaceutics (2018), 15 (5), 1766-1777; DOI: 10.1021/acs.molpharmaceut.7b01013.
  1. “Design and Synthesis of Novel Deuterated Ligands Functionally Selective for the γ-Aminobutyric Acid Type A Receptor (GABAAR) α6 Subtype with Improved Metabolic Stability and Enhanced Bioavailability”, Knutson, D.; Kodali, R.; Divović, B.; Treven, M.; Stephen, M.; Zahn, N.; Dobričić, V.; Huber, A.; Meirelles, M.; Verma, R.; Wimmer, L.; Witzigmann, C.; Arnold, A.; Chiou, L.; Ernst, M.; Mihovilovic, M.; Savić, M.M.; Sieghart, W.; Cook, J., J. Med. Chem., 2018, 61 (6), 2422–2446, DOI: 10.1021/acs.jmedchem.7b01664.
  2. “Attaining in vivo selectivity of positive modulation of α3βγ2 GABAA receptors in rats: a hard task!”, Batinić, B.;  Stanković, T.; Stephen, M.; Kodali, R.; Tiruveedhula, V.V.N.; Li, G.; Scholze, P.; Marković, B.; Obradović, A.L.; Ernst, M.;  Cook, J.; Savić, , Eur Neuropsychopharmacol, doi: 10.1016/j.euroneuro.2018.05.014, PMID: 29891214, Jun 2018.
  3. “Novel Benzodiazepine-Like Ligands with Various Anxiolytic, Antidepressant, or Pro-Cognitive Profiles”, Prevot, T.; Li, G.; Vidojevic, A.; Misquitta, K.; Santrac, A.; Knutson, D.; Stephen, M.; Kodali, R.; Zahn, N.; Arnold, L.; Scholze, P.; Fisher, J.; Marković, B.; Banasr, M.; Cook, J.; Savić, M.; Sibille, E., Mol Neuropsychiatry, DOI 10.1159/000496086, Jan 23, 2019.
  4. “Synthesis of chiral GABAA receptor subtype selective ligands as potential agents to treat schizophrenia as well as depression”, Li, G.; Stephen, M.; Kodali, R.; Zahn, N.; Poe, M.; Tiruveedhula, V.V.N.;  Huber, A,; Schussman, M.; Qualmann, K.; Panhans, C.; Raddatz, N.; Baker, D.; Prevot, T.; Banasr, M.; Sibille, E.; Arnold, A.; Cook, J., Arkivoc, 2018, part iv, 158-183.
  5. “Bioisosteres of ethyl 8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo [1,5-a][1,4]diazepine-3-carboxylate (HZ-166) as novel alpha 2,3 selective potentiators of GABAA receptors: improved bioavailability enhances anticonvulsant efficacy”, J. M. Witkin, J. L. Smith, X. Ping, S. D. Gleason, M. M. Poe, G. Li, X. Jin, J. Hobbs, J. M. Schkeryantz, J. S. McDermott, A. I. Alatorre, J. N. Siemian, J.W. Cramer, D. C. Airey, K. R. Methuku, T. M. Jones, M. J. Krambis, J. L. Fisher, J. M. Cook, R. Cerne, Neuropharmacology, DOI: 10.1016/j.neuropharm.2018.05.006.
  6. “Evidence that Sedative Effects of Benzodiazepines Involve Unexpected GABAA Receptor Subtypes: Quantitative Observation Studies in Rhesus Monkeys”, Duke, A.; Meng, Z.; Platt, D.; Atack, J.; Dawson, G.; Reynolds, D.; Tiruveedhula, V.V.N.; Li, G.; Stephen, M.; Sieghart, W.; Cook J.; Rowlett, J. K., Pharmacol. Exp. Ther., DOI: 10.1124/jp-et.118.249250, May 2018.
  7. “Inverse agonists selective for GABAA receptors containing the α5 subunit attenuate alcohol cue-induced reinstatement and active alcohol self-administration in rats”, Cassie M. Chandler, Jaren Reeves-Darby, Sherman A. Jones, Guanguan Li, Md T. Rahman, James M. Cook, Donna M. Platt, Psychopharmacology, Submitted 2018.
  8. “Improved Synthesis of Anxiolytic, Anticonvulsant and Antinociceptive α2/α3-GABA(A)ergic Receptor Subtype Selective Ligands as Promising Agents to Treat Anxiety, Epilepsy, as well as Neuropathic Pain”, Li, G.; Golani, L. K.; Jahan, R.; Rashid, F.; Cook, J. M, Synthesis, 2018, 50(20): 4124-4132, DOI: 10.1055/s-0037-1610211.
  9. “An Antidepressant-Related Pharmacological Signature for Positive Allosteric Modulators of alpha 2/3-Containing GABAA Receptors”, Methuku, K.R.; Li, X.; Cerne, R.; Gleason, S.; Schkeryantz, J.M.; Tiruveedhula, V.V.N.; Golani, L. K.; Li, G.; Poe, M.; Rahman, M.T.; Cook, J.; Fisher, J.; Witkin, J.; Biochem. Behav., DOI: 10.1016/j.pbb.20-18.04.009, April 2018.
  10. “Modulation of relapse-like drinking in rats by ligands targeting the a5GABAA receptor”, Chandler, C.; Reeves-Darby, J.; Jones, S.; Li, G.; Rahman, M.T.; Cook, J.; Platt, D., Alcohol Clin Exp Res, Submitted, May 2018.
  11. “Unprecedented stereocontrol in the synthesis of 1,2,3‐ trisubstituted tetrahydro‐β‐carbolines via a new asymmetric Pictet—Spengler reaction towards sarpagine‐type indole alkaloids”, Rahman, M.T.; Cook, J., J. Org. Chem, DOI: 10.10-02/ejoc.201800600, April 2018.
  12. “Different Benzodiazepines Bind with Distinct Binding Modes to GABAA Receptors”, Elgarf, A.; Siebert, D.; Steudle, F.; Draxler, A.; Li, G.; Huang, S.; Cook, J.; Ernst, M.; Scholze, P., ACS Chem Biol., DOI: 10.1021/acschembio.8b00144, May 16 2018.
  13. “α5GABAA subunit-containing receptors and sweetened alcohol cue-induced reinstatement and active sweetened alcohol self-administration in male rats”, Chandler CM.; Reeves-Darby J.; Jones SA.; McDonald JA.; Li G.; Rahman M.T.; Cook J.M.; Platt D.M., Psychopharmacology (Berl), doi: 10.1007/s00213-018-5163-6, Jan 12, 2019.
  14. “Zolpidem activation of alpha 1-containing GABAA receptors selectively inhibits high frequency action potential firing of cortical neurons”, Neumann, E.; Rudolph, W.; Knutson, D.; Li, G.; Cook, J.M.; Antkowiak, B.; Drexler, B., ,, Jan 09, 2019.
  15. “Trigeminal neuropathic pain development and maintenance in rats are suppressed by a positive modulator of α6GABAA receptors”, Vasović D.; Divović B.; Treven M.; Knutson D.; Steudle F.; Scholze P.; Obradović A.; Fabjan J.; Brković B.; Sieghart W.; Ernst M.; Cook J.M.; Savić M.M., Eur J Pain., doi: 10.1002/ejp.1365, Jan 11, 2019.
  16. “Effects of the α2/α3-subtype-selective GABAA receptor positive allosteric modulator KRM-II-81 on pain-depressed behavior in rats: comparison with ketorolac and diazepam”, Moerkea, M.J.; Li, G; Golani, L.K.; Cook, J.M.; Negus, S.S., Behav Pharmacol.,  doi: 10.1097/FBP.0000000000000464, Jan 10, 2019.
  17. “A Novel GABAA Receptor Ligand MIDD0301 with Limited Blood-Brain Barrier Penetration Relaxes Airway Smooth Muscle Ex Vivo and In Vivo”, Yocum, G.T.; Perez-Zoghbi, J.F.; Danielsson, J.; Kuforiji, A.S.; Zhang, Y.; Li, G.; Rashid Roni M.S.; Kodali, R.; Stafford, D.; Arnold, L.A.; Cook, J.M.; Emala, C.W., Am J Physiol Lung Cell Mol Physiol. ,, Nov 29, 2018.
  18. “GABAA Receptor Subtypes Revisited: Evaluation of Anxiolytic-Like, Reinforcing, and Sed-ative Effects of the Functionally Selective α3 Subunit-Containing GABAA Receptor Ligand YT-III-31 in Rhesus Monkeys”, Meng, Z.; Berro, L.F.; Sawyer, E.K.; Rüedi-Bettschen, D.; Cook, J.E.; Li, G.; Platt, D.M.; Cook, J.M.; Rowlett, J.K., Psychopharmacology, Submitted, Feb 2019.
  19. “Modulating native GABAA receptors in medulloblastoma with positive allosteric benzodiazepine-derivatives induces cell death”, Kallay, L.; Keskin, H.; Ross, A.; Rupji, M.; Moody, O.A.; Wang, X.; Li, G.; Ahmed, T.; Rashid, F.; Stephen, M.R.; Cottrill, K.A.; Nuckols, T.A.; Xu, M.; Martinson, D.E.; Tranghese, F.; Pei, Y.; Cook, J.M.; Kowalski, J.; Taylor, M.D.; Jenkins, A.; Pomeranz Krummel, D.A.; Sengupta, S., J Neurooncol. (2019), 142, 411-422, doi: 10.1007/s11060-019-03115-0.
  20. “The C-19 Methyl Substituted Sarpagine-Macroline-Ajmaline Alkaloids: Diversity, Occurrence, Bioactivity, and Synthesis”, Rahman, M. T.; Cook, J. M., Studies in Natural Products Chemistry, Vol. 64, Atta-ur-Rahman, Ed.; Elsevier: Amsterdam, 2020, doi: 10.1016/B978-0-12-817903-1.00001-2.
  21. “The α2,3-selective potentiator of GABAA receptors, KRM-II-81, reduces nociceptive-associated behaviors induced by formalin and spinal nerve ligation in rats”, Witkin, J.M.; Cerne, R; Davis P.G.; Freeman, K.b.; Carmo, J.M.; Rowlett, J.; Methuku, K.R.; Okun, A.; Gleason, S.D.; Li, X.; Poe, R.M.; Li, G.; Schkeryantz, J.M.; Jahan, R.; Yang, L.; Guo1, W.; Anderson, W.H.; Catlow, J.T.; Jones, T/M.; Porreca, F.; Smith, J.l.; Knopp, K.L.; Cook, J.M., Biochem. Behav. (2019), 180: 22-31,
  22. “The value of human epileptic tissue in the characterization and development of novel antiepileptic drugs: The example of CERC-611 and KRM-II-81”, Witkin, J.M.; Ping, X.; Cerne, R.; Mouser, C.; Jin, X.; Hobbs, J.; Tiruveedhula, VVNPB; Li, G.; Jahan, R.; Rashid, F.; Golani, L.; Cook, J.M.;, Smith, J.L., Res.  (2019),
  23. “MIDD0301 – A first‐in‐class anti‐inflammatory asthma drug targets GABAA receptors without causing systemic immune suppression”, Zahn, N.M.; Huber, A.T.; Mikulsky, B.N.; Stepanski, M.E.; Kehoe, A.S,; Li, G.; Schussman, M.; Rashid Roni, M.S.; Kodali, R.; Cook, J.M.; Stafford, D.C.; Steeber, D.A.; Arnold, L.A., Basic Clin Pharmacol Toxicol., doi: 10.1111/bcpt.13206, Jan 2019.
  24. “The Ambidextrous Pictet–Spengler Reaction: Access to the (+)- or (–)-Enantiomers of the Bioactive C-19 Methyl-Substituted Sarpagine/Macroline/Ajmaline Alkaloids from Either d- or l-Tryptophan”, Rahman, M.T.; Cook, J.M., Synthesis, DOI: 10.1055/s-0037-1610687, Feb, 2019.
  25. “GABAA α2/α3 receptor subtypes and the abuse-related effects of ethanol in rhesus monkeys: Experiments with selective positive allosteric modulators”, Berro, L.F.; Rüedi-Bettschen, D.; Cook, J.E.; Golani, L.K.; Li, G.; Jahan, R.;  Rashid, F.; Cook, J.M.; Rowlett, J.K.; Platt, D.M., Clin. Exp. Res. (2019), 43 (5),
  26. “The positive allosteric modulator of α2/3-containing GABAA receptors, KRM-II-81, is active in pharmaco-resistant models of epilepsy and reduces hyperexcitability after traumatic brain injury”, Witkin J.M.; Li, G.; Golani, L.; Xiong, W.; Smith, J.L.; Ping, X.; Rashid, F.; Jahan, R.; Cerne, R.; Cook, J.M.; Jin X., Pharmacol. Exp. Ther. (2019), doi: 10.1124/jpet.119.260968 .
  27. “Insight into Novel Treatment for Cognitive Dysfunctions across Disorders”, Prevot, T.D.; Li, G.; Cook, J.M.; Sibille, E., ACS Chem. Neurosci., DOI: 10.1021/acschemneuro.9b00148, March 2019.
  28. “Non-sedating benzodiazepines cause paralysis and tissue damage in the parasitic blood fluke Schistosoma mansoni”, McCusker, P.; Mian, M. Y.; Li, G.; Olp, M. D.; Phani Babu, V. V. N.; Rashid, F.; Golani, L. K.; Verma, R. S.; Smith, B. C.;  Cook, J.M.; Chan, J.D., PLoS NTD, 2019, doi: 10.1371/journal.pntd.0007826, PMCID: PMC6881066.
  29. “Facilitation of Social Support through Negative Allosteric Modulation of α5-Associated GABAA Receptors: A Novel Mechanism for the Treatment of Depression, Agitation, and Aggression in the Elderly”, Witkin, J.M.; Golani, L.K.; Cerne, R,; Rahman, M.T.; Li, G.; Poe, M.M.;  Cook, J.M. ; Smith, J.L., OBM Geriatrics (2019), doi: 10.21926/obm.geriatr.1903073.
  30. “The effects of pH on the structure and bio-availability of Imidazobenzodiazepine-3-Carboxylate MIDD0301”, Roni, M. R.; Li, G.;  Mikulsky,N.; Knutson, D. E.; Mian, Y.; Zahn, N. M.; Cook, J.M.; Stafford, D. C.; Arnold, L. A., Mol. Pharmaceutics (2020), doi: 10.1021/acs.molpharmaceut.9b01210.
  31. “Improvements in the pharmacological profile of diazepam by KRM-II-81, an imidazodiazepine positive allosteric modulator of a2/3-containing GABAA receptors: Preclinical data predict enhanced efficacy for epilepsy, chronic pain, anxiety, and depression”, Cerne, R.; Fisher, J.L.; Siemian, J. N.; Smith, J.L.; Knutson, D.E.; Cook, J.M.; Witkin, J.M., J Pharmaceut Biomed, 2 (1):117, Dec 2019.
  32. “Depressive-like behaviors induced by somatostatin-positive GABA neuron silencing are rescued by alpha 5 GABA-A receptor potentiation”, Neuropsychopharmacology, submitted, June 2020.
  33. “Reversal of age-related neuronal atrophy by α5-GABAA receptor positive allosteric modulation”, Prevot, T.;  Sumitomo, A.; Tomoda, T.; Knutson, D.E.; Li, G.; Mondal, P.; Banasr, M.; Cook, J.M.; Sibille, E., CEREB CORTEX, submitted, June 2020.
  34. “Targeting nitric oxide production in microglia with novel imidazodiazepines for nonsedative pain treatment”, Nieman, A.; Li, G.; Zahn, N.M.; Mian, Y.; Mikulsky, B.N.; Hoffman, D.A.; Wilcox, T.M.; Kehoe, A.S.; Luecke, I.W.; Poe, M.M.; Alvarez-Carbonell, D.A.; Cook, J.M.; Stafford, D.C.; Arnold, L.A., ACS Chemical Neuroscience (2020), doi: 1021/acschemneuro.0c00324.
  35. “The Imidazodiazepine Anticonvulsant, KRM-II-81, Produces Novel, Non-diazepam-like Antiepileptogentic Effects”, Knutson, D.; Smith, J.; Ping, X.; Jin, X.; Golani, L.; Li, G. ; Tiruveedhula, V. V. N.; Rashid, F.; Mian, Y.; Jahan, R.; Sharmin, D.; Cerne, R.; Cook, J.; Witken, J., ACS Chem. Neurosci., submitted, May 2020.
  36. “α6GABAA receptor positive modulators alleviate migraine-like grimaces in mice via compensating GABAergic deficit in trigeminal ganglia (135/135)”, Tzeng, H.; Lee, M.T.; Knutson, D.E.; Fan, P.; Ernst, M.; Seighert, W.; Cook, J.M.; Chiou, L., PLoS Biol., submitted, 2020.
  37. “Nanocrystal dispersion of DK-I-56-1, a poorly soluble pyrazoloquinolinone positive modulator of α6 GABAA receptors: formulation approach toward improved in vivo performance”, Vasović, D.; Divović, B.; Treven, M.; Knutson, D.E.; Steudle , F.; Scholze, P.; Obradović, A.; Fabjan, J.; Brković, B.; Sieghart, W.; Ernst, M.; Cook, J.M.; Savić, M.M., Eur J Pain, 2019, 23(5): 973-984, doi: 10.1002/ejp.1365.

Group Pictures

GROUP PHOTO ARCHIVE (hover cursor over photo for caption) Faculty of the year (2016-2017) award goes to Dr. Cook Dr. Cook receiving the award from Mark. 05-23-2017 Professor Kishi, Professor Cook and Professor Sosnovsky (98 years old) at Lunch March… Read More