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mGlu2/3 receptor antagonism: A mechanism to induce rapid antidepressant effects without ketamine-associated side-effects.

Witkin JM.

Pharmacol Biochem Behav. 2020 Jan 16;190:172854. doi: 10.1016/j.pbb.2020.172854. [Epub ahead of print] Review.


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 JM, Li G, Golani LK, Xiong W, Smith JL, Ping X, Rashid F, Jahan R, Cerne R, Cook JM, Jin X.

J Pharmacol Exp Ther. 2020 Jan;372(1):83-94. doi: 10.1124/jpet.119.260968. Epub 2019 Nov 6.



Witkin JM.

Adv Pharmacol. 2019;86:xi-xiii. doi: 10.1016/S1054-3589(19)30059-6. No abstract available.


Rapid-acting antidepressants.

Witkin JM, Martin AE, Golani LK, Xu NZ, Smith JL.

Adv Pharmacol. 2019;86:47-96. doi: 10.1016/bs.apha.2019.03.002. Epub 2019 Apr 24.


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 JM, Ping X, Cerne R, Mouser C, Jin X, Hobbs J, Tiruveedhula VVNPB, Li G, Jahan R, Rashid F, Kumar Golani L, Cook JM, Smith JL.

Brain Res. 2019 Nov 1;1722:146356. doi: 10.1016/j.brainres.2019.146356. Epub 2019 Jul 29. Review.


A medium throughput rodent model of relapse from addiction with behavioral and pharmacological specificity.

Eiler WJA 2nd, Gleason SD, Smith JL, Witkin JM.

Pharmacol Biochem Behav. 2019 Aug;183:72-79. doi: 10.1016/j.pbb.2019.06.005. Epub 2019 Jun 14.


Modulation of TARP γ8-Containing AMPA Receptors as a Novel Therapeutic Approach for Chronic Pain.

Knopp KL, Simmons RMA, Guo W, Adams BL, Gardinier KM, Gernert DL, Ornstein PL, Porter W, Reel J, Ding C, Wang H, Qian Y, Burris KD, Need A, Barth V, Swanson S, Catlow J, Witkin JM, Zwart R, Sher E, Choong KC, Wall TM, Schober D, Felder CC, Kato AS, Bredt DS, Nisenbaum ES.

J Pharmacol Exp Ther. 2019 Jun;369(3):345-363. doi: 10.1124/jpet.118.250126. Epub 2019 Mar 25.


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 JM, Cerne R, Davis PG, Freeman KB, do Carmo JM, Rowlett JK, Methuku KR, Okun A, Gleason SD, Li X, Krambis MJ, Poe M, Li G, Schkeryantz JM, Jahan R, Yang L, Guo W, Golani LK, Anderson WH, Catlow JT, Jones TM, Porreca F, Smith JL, Knopp KL, Cook JM.

Pharmacol Biochem Behav. 2019 May;180:22-31. doi: 10.1016/j.pbb.2019.02.013. Epub 2019 Feb 27.


Evaluation of 5-HT7 receptor antagonism for the treatment of anxiety, depression, and schizophrenia through the use of receptor-deficient mice.

Balcer OM, Seager MA, Gleason SD, Li X, Rasmussen K, Maxwell JK, Nomikos G, Degroot A, Witkin JM.

Behav Brain Res. 2019 Mar 15;360:270-278. doi: 10.1016/j.bbr.2018.12.019. Epub 2018 Dec 10.


Animal models of fatigue in major depressive disorder.

Stutz PV, Golani LK, Witkin JM.

Physiol Behav. 2019 Feb 1;199:300-305. doi: 10.1016/j.physbeh.2018.11.042. Epub 2018 Dec 1. Review.


Effects of 5-HT7 receptor antagonists on behaviors of mice that detect drugs used in the treatment of anxiety, depression, or schizophrenia.

Maxwell J, Gleason SD, Falcone J, Svensson K, Balcer OM, Li X, Witkin JM.

Behav Brain Res. 2019 Feb 1;359:467-473. doi: 10.1016/j.bbr.2018.11.019. Epub 2018 Nov 22.


Rapid-Acting Antidepressants.

Witkin JM, Knutson DE, Rodriguez GJ, Shi S.

Curr Pharm Des. 2018;24(22):2556-2563. doi: 10.2174/1381612824666180730104707. Review.


Pharmacological characterization of the neurotrophic sesquiterpene jiadifenolide reveals a non-convulsant signature and potential for progression in neurodegenerative disease studies.

Witkin JM, Shenvi RA, Li X, Gleason SD, Weiss J, Morrow D, Catow JT, Wakulchik M, Ohtawa M, Lu HH, Martinez MD, Schkeryantz JM, Carpenter TS, Lightstone FC, Cerne R.

Biochem Pharmacol. 2018 Sep;155:61-70. doi: 10.1016/j.bcp.2018.06.022. Epub 2018 Jun 22.


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.

Witkin JM, Smith JL, Ping X, Gleason SD, Poe MM, Li G, Jin X, Hobbs J, Schkeryantz JM, McDermott JS, Alatorre AI, Siemian JN, Cramer JW, Airey DC, Methuku KR, Tiruveedhula VVNPB, Jones TM, Crawford J, Krambis MJ, Fisher JL, Cook JM, Cerne R.

Neuropharmacology. 2018 Jul 15;137:332-343. doi: 10.1016/j.neuropharm.2018.05.006. Epub 2018 May 3.


An antidepressant-related pharmacological signature for positive allosteric modulators of α2/3-containing GABAA receptors.

Methuku KR, Li X, Cerne R, Gleason SD, Schkeryantz JM, Tiruveedhula VVNPB, Golani LK, Li G, Poe MM, Rahman MT, Cook JM, Fisher JL, Witkin JM.

Pharmacol Biochem Behav. 2018 Jul;170:9-13. doi: 10.1016/j.pbb.2018.04.009. Epub 2018 Apr 30.


Chronic pain impairs cognitive flexibility and engages novel learning strategies in rats.

Cowen SL, Phelps CE, Navratilova E, McKinzie DL, Okun A, Husain O, Gleason SD, Witkin JM, Porreca F.

Pain. 2018 Jul;159(7):1403-1412. doi: 10.1097/j.pain.0000000000001226.


Negative allosteric modulation of alpha 5-containing GABAA receptors engenders antidepressant-like effects and selectively prevents age-associated hyperactivity in tau-depositing mice.

Xu NZ, Ernst M, Treven M, Cerne R, Wakulchik M, Li X, Jones TM, Gleason SD, Morrow D, Schkeryantz JM, Rahman MT, Li G, Poe MM, Cook JM, Witkin JM.

Psychopharmacology (Berl). 2018 Apr;235(4):1151-1161. doi: 10.1007/s00213-018-4832-9. Epub 2018 Jan 26.


Protein complexes as psychiatric and neurological drug targets.

Kato AS, Witkin JM.

Biochem Pharmacol. 2018 May;151:263-281. doi: 10.1016/j.bcp.2018.01.018. Epub 2018 Jan 9. Review.


Preclinical profile of a dopamine D1 potentiator suggests therapeutic utility in neurological and psychiatric disorders.

Bruns RF, Mitchell SN, Wafford KA, Harper AJ, Shanks EA, Carter G, O'Neill MJ, Murray TK, Eastwood BJ, Schaus JM, Beck JP, Hao J, Witkin JM, Li X, Chernet E, Katner JS, Wang H, Ryder JW, Masquelin ME, Thompson LK, Love PL, Maren DL, Falcone JF, Menezes MM, Zhang L, Yang CR, Svensson KA.

Neuropharmacology. 2018 Jan;128:351-365. doi: 10.1016/j.neuropharm.2017.10.032. Epub 2017 Oct 26.


Targeted Blockade of TARP-γ8-Associated AMPA Receptors: Anticonvulsant Activity with the Selective Antagonist LY3130481 (CERC-611).

Witkin JM, Schober DA, Gleason SD, Catlow JT, Porter WJ, Reel J, Jin X, Hobbs J, Gehlert D, Gernert DL, Gardinier KM, Kato AS, Ping X, Smith JL.

CNS Neurol Disord Drug Targets. 2017;16(10):1099-1110. doi: 10.2174/1871527316666171101132047.


Auxiliary subunits of AMPA receptors: The discovery of a forebrain-selective antagonist, LY3130481/CERC-611.

Kato AS, Witkin JM.

Biochem Pharmacol. 2018 Jan;147:191-200. doi: 10.1016/j.bcp.2017.09.015. Epub 2017 Oct 5. Review.


Prediction of human efficacious antidepressant doses using the mouse forced swim test.

Yuen E, Swanson S, Witkin JM.

Pharmacol Biochem Behav. 2017 Oct;161:22-29. doi: 10.1016/j.pbb.2017.09.002. Epub 2017 Sep 6.


Structural Determinants of the γ-8 TARP Dependent AMPA Receptor Antagonist.

Lee MR, Gardinier KM, Gernert DL, Schober DA, Wright RA, Wang H, Qian Y, Witkin JM, Nisenbaum ES, Kato AS.

ACS Chem Neurosci. 2017 Dec 20;8(12):2631-2647. doi: 10.1021/acschemneuro.7b00186. Epub 2017 Sep 5.


Electroencephalographic, cognitive, and neurochemical effects of LY3130481 (CERC-611), a selective antagonist of TARP-γ8-associated AMPA receptors.

Witkin JM, Li J, Gilmour G, Mitchell SN, Carter G, Gleason SD, Seidel WF, Eastwood BJ, McCarthy A, Porter WJ, Reel J, Gardinier KM, Kato AS, Wafford KA.

Neuropharmacology. 2017 Nov;126:257-270. doi: 10.1016/j.neuropharm.2017.07.028. Epub 2017 Jul 28.


Synthesis of (-)-11-O-Debenzoyltashironin: Neurotrophic Sesquiterpenes Cause Hyperexcitation.

Ohtawa M, Krambis MJ, Cerne R, Schkeryantz JM, Witkin JM, Shenvi RA.

J Am Chem Soc. 2017 Jul 19;139(28):9637-9644. doi: 10.1021/jacs.7b04206. Epub 2017 Jul 6.


Behavioral Effects of a Novel Benzofuranyl-Piperazine Serotonin-2C Receptor Agonist Suggest a Potential Therapeutic Application in the Treatment of Obsessive-Compulsive Disorder.

Rodriguez MM, Overshiner C, Leander JD, Li X, Morrow D, Conway RG, Nelson DL, Briner K, Witkin JM.

Front Psychiatry. 2017 May 22;8:89. doi: 10.3389/fpsyt.2017.00089. eCollection 2017.


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. doi: 10.1016/j.pbb.2017.04.009. Epub 2017 Apr 22.


Further Evaluation of Mechanisms Associated with the Antidepressantlike Signature of Scopolamine in Mice.

Martin AE, Schober DA, Nikolayev A, Tolstikov VV, Anderson WH, Higgs RE, Kuo MS, Laksmanan A, Catlow JT, Li X, Felder CC, Witkin JM.

CNS Neurol Disord Drug Targets. 2017;16(4):492-500. doi: 10.2174/1871527316666170309142646.


Preclinical predictors that the orthosteric mGlu2/3 receptor antagonist LY3020371 will not engender ketamine-associated neurotoxic, motor, cognitive, subjective, or abuse-liability-related effects.

Witkin JM, Monn JA, Li J, Johnson B, McKinzie DL, Wang XS, Heinz BA, Li R, Ornstein PL, Smith SC, Mitch CH, Calligaro DO, Swanson S, Allen D, Phillips K, Gilmour G.

Pharmacol Biochem Behav. 2017 Apr;155:43-55. doi: 10.1016/j.pbb.2017.03.001. Epub 2017 Mar 8.


Comparative Effects of LY3020371, a Potent and Selective Metabotropic Glutamate (mGlu) 2/3 Receptor Antagonist, and Ketamine, a Noncompetitive N-Methyl-d-Aspartate Receptor Antagonist in Rodents: Evidence Supporting the Use of mGlu2/3 Antagonists, for the Treatment of Depression.

Witkin JM, Mitchell SN, Wafford KA, Carter G, Gilmour G, Li J, Eastwood BJ, Overshiner C, Li X, Rorick-Kehn L, Rasmussen K, Anderson WH, Nikolayev A, Tolstikov VV, Kuo MS, Catlow JT, Li R, Smith SC, Mitch CH, Ornstein PL, Swanson S, Monn JA.

J Pharmacol Exp Ther. 2017 Apr;361(1):68-86. doi: 10.1124/jpet.116.238121. Epub 2017 Jan 30.


Preclinical findings predicting efficacy and side-effect profile of LY2940094, an antagonist of nociceptin receptors.

Witkin JM, Rorick-Kehn LM, Benvenga MJ, Adams BL, Gleason SD, Knitowski KM, Li X, Chaney S, Falcone JF, Smith JW, Foss J, Lloyd K, Catlow JT, McKinzie DL, Svensson KA, Barth VN, Toledo MA, Diaz N, Lafuente C, Jiménez A, Benito A, Pedregal C, Martínez-Grau MA, Post A, Ansonoff MA, Pintar JE, Statnick MA.

Pharmacol Res Perspect. 2016 Nov 7;4(6):e00275. doi: 10.1002/prp2.275. eCollection 2016 Dec.


Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity.

Chappell MD, Li R, Smith SC, Dressman BA, Tromiczak EG, Tripp AE, Blanco MJ, Vetman T, Quimby SJ, Matt J, Britton TC, Fivush AM, Schkeryantz JM, Mayhugh D, Erickson JA, Bures MG, Jaramillo C, Carpintero M, Diego JE, Barberis M, Garcia-Cerrada S, Soriano JF, Antonysamy S, Atwell S, MacEwan I, Condon B, Sougias C, Wang J, Zhang A, Conners K, Groshong C, Wasserman SR, Koss JW, Witkin JM, Li X, Overshiner C, Wafford KA, Seidel W, Wang XS, Heinz BA, Swanson S, Catlow JT, Bedwell DW, Monn JA, Mitch CH, Ornstein PL.

J Med Chem. 2016 Dec 22;59(24):10974-10993. Epub 2016 Dec 6.


Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABAA) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy.

Poe MM, Methuku KR, Li G, Verma AR, Teske KA, Stafford DC, Arnold LA, Cramer JW, Jones TM, Cerne R, Krambis MJ, Witkin JM, Jambrina E, Rehman S, Ernst M, Cook JM, Schkeryantz JM.

J Med Chem. 2016 Dec 8;59(23):10800-10806. Epub 2016 Nov 28.


Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression.

Dressman BA, Tromiczak EG, Chappell MD, Tripp AE, Quimby SJ, Vetman T, Fivush AM, Matt J, Jaramillo C, Li R, Khilevich A, Blanco MJ, Smith SC, Carpintero M, de Diego JE, Barberis M, García-Cerrada S, Soriano JF, Schkeryantz JM, Witkin JM, Wafford KA, Seidel W, Britton T, Overshiner CD, Li X, Wang XS, Heinz BA, Catlow JT, Swanson S, Bedwell D, Ornstein PL, Mitch CH.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5663-5668. doi: 10.1016/j.bmcl.2016.10.067. Epub 2016 Oct 25.


Forebrain-selective AMPA-receptor antagonism guided by TARP γ-8 as an antiepileptic mechanism.

Kato AS, Burris KD, Gardinier KM, Gernert DL, Porter WJ, Reel J, Ding C, Tu Y, Schober DA, Lee MR, Heinz BA, Fitch TE, Gleason SD, Catlow JT, Yu H, Fitzjohn SM, Pasqui F, Wang H, Qian Y, Sher E, Zwart R, Wafford KA, Rasmussen K, Ornstein PL, Isaac JT, Nisenbaum ES, Bredt DS, Witkin JM.

Nat Med. 2016 Dec;22(12):1496-1501. doi: 10.1038/nm.4221. Epub 2016 Nov 7.


Consequences of constitutive deletion of melanin-concentrating hormone-1 receptors for feeding and foraging behaviors of mice.

Eiler WJ 2nd, Chen Y, Slieker LJ, Ardayfio PA, Statnick MA, Witkin JM.

Behav Brain Res. 2017 Jan 1;316:271-278. doi: 10.1016/j.bbr.2016.09.028. Epub 2016 Sep 12.


Erratum: A Selective Nociceptin Receptor Antagonist to Treat Depression: Evidence from Preclinical and Clinical Studies.

Post A, Smart TS, Krikke-Workel J, Dawson GR, Harmer CJ, Browning M, Jackson K, Kakar R, Mohs R, Statnick M, Wafford K, McCarthy A, Barth V, Witkin JM.

Neuropsychopharmacology. 2016 Sep;41(10):2624. doi: 10.1038/npp.2016.78. Epub 2016 Aug 11.


Hedonic and motivational responses to food reward are unchanged in rats with neuropathic pain.

Okun A, McKinzie DL, Witkin JM, Remeniuk B, Husein O, Gleason SD, Oyarzo J, Navratilova E, McElroy B, Cowen S, Kennedy JD, Porreca F.

Pain. 2016 Dec;157(12):2731-2738.


A Comment on "Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-γ8".

Witkin JM, Gardinier KM.

J Pharmacol Exp Ther. 2016 Sep;358(3):502-3. doi: 10.1124/jpet.116.234419. No abstract available.


The Rapidly Acting Antidepressant Ketamine and the mGlu2/3 Receptor Antagonist LY341495 Rapidly Engage Dopaminergic Mood Circuits.

Witkin JM, Monn JA, Schoepp DD, Li X, Overshiner C, Mitchell SN, Carter G, Johnson B, Rasmussen K, Rorick-Kehn LM.

J Pharmacol Exp Ther. 2016 Jul;358(1):71-82. doi: 10.1124/jpet.116.233627. Epub 2016 May 12.


A Novel, Orally Bioavailable Nociceptin Receptor Antagonist, LY2940094, Reduces Ethanol Self-Administration and Ethanol Seeking in Animal Models.

Rorick-Kehn LM, Ciccocioppo R, Wong CJ, Witkin JM, Martinez-Grau MA, Stopponi S, Adams BL, Katner JS, Perry KW, Toledo MA, Diaz N, Lafuente C, Jiménez A, Benito A, Pedregal C, Weiss F, Statnick MA.

Alcohol Clin Exp Res. 2016 May;40(5):945-54. doi: 10.1111/acer.13052. Epub 2016 Apr 16.


Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8.

Gardinier KM, Gernert DL, Porter WJ, Reel JK, Ornstein PL, Spinazze P, Stevens FC, Hahn P, Hollinshead SP, Mayhugh D, Schkeryantz J, Khilevich A, De Frutos O, Gleason SD, Kato AS, Luffer-Atlas D, Desai PV, Swanson S, Burris KD, Ding C, Heinz BA, Need AB, Barth VN, Stephenson GA, Diseroad BA, Woods TA, Yu H, Bredt D, Witkin JM.

J Med Chem. 2016 May 26;59(10):4753-68. doi: 10.1021/acs.jmedchem.6b00125. Epub 2016 Apr 29.


In vitro pharmacological and rat pharmacokinetic characterization of LY3020371, a potent and selective mGlu2/3 receptor antagonist.

Witkin JM, Ornstein PL, Mitch CH, Li R, Smith SC, Heinz BA, Wang XS, Xiang C, Carter JH, Anderson WH, Li X, Broad LM, Pasqui F, Fitzjohn SM, Sanger HE, Smith JL, Catlow J, Swanson S, Monn JA.

Neuropharmacology. 2017 Mar 15;115:100-114. doi: 10.1016/j.neuropharm.2015.12.021. Epub 2015 Dec 31.


A Novel Nociceptin Receptor Antagonist LY2940094 Inhibits Excessive Feeding Behavior in Rodents: A Possible Mechanism for the Treatment of Binge Eating Disorder.

Statnick MA, Chen Y, Ansonoff M, Witkin JM, Rorick-Kehn L, Suter TM, Song M, Hu C, Lafuente C, Jiménez A, Benito A, Diaz N, Martínez-Grau MA, Toledo MA, Pintar JE.

J Pharmacol Exp Ther. 2016 Feb;356(2):493-502. doi: 10.1124/jpet.115.228221. Epub 2015 Dec 9.


A Selective Nociceptin Receptor Antagonist to Treat Depression: Evidence from Preclinical and Clinical Studies.

Post A, Smart TS, Krikke-Workel J, Dawson GR, Harmer CJ, Browning M, Jackson K, Kakar R, Mohs R, Statnick M, Wafford K, McCarthy A, Barth V, Witkin JM.

Neuropsychopharmacology. 2016 Jun;41(7):1803-12. doi: 10.1038/npp.2015.348. Epub 2015 Nov 20. Erratum in: Neuropsychopharmacology. 2016 Sep;41(10):2624.


Inquiries into the Biological Significance of Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8 Through Investigations of TARP γ-8 Null Mice§.

Gleason SD, Kato A, Bui HH, Thompson LK, Valli SN, Stutz PV, Kuo MS, Falcone JF, Anderson WH, Li X, Witkin JM.

CNS Neurol Disord Drug Targets. 2015;14(5):612-26.


Obituary: J. David LEander, Ph.D. : (April 8, 1944-November 14, 2014).

Witkin JM, Gleason SD, Carter RB, Dykstra LA.

Psychopharmacology (Berl). 2015 Apr;232(7):1175-6. doi: 10.1007/s00213-015-3885-2. Epub 2015 Feb 21. No abstract available.


Commentary: obstacles to the discovery of medicines for psychiatric disorders in modern times.

Witkin JM.

CNS Neurol Disord Drug Targets. 2015;14(1):4-6. No abstract available.


M1 and m2 muscarinic receptor subtypes regulate antidepressant-like effects of the rapidly acting antidepressant scopolamine.

Witkin JM, Overshiner C, Li X, Catlow JT, Wishart GN, Schober DA, Heinz BA, Nikolayev A, Tolstikov VV, Anderson WH, Higgs RE, Kuo MS, Felder CC.

J Pharmacol Exp Ther. 2014 Nov;351(2):448-56. doi: 10.1124/jpet.114.216804. Epub 2014 Sep 3.


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