PUBLICATIONS

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2023

Rouzbeh N, Rau AR, Benton AJ, Yi F, Anderson CM, Johns MR, Jensen L, Lotti JS, Holley DC, Hansen KB. Allosteric modulation of GluN1/GluN3 NMDA receptors by GluN1-selective competitive antagonists. J Gen Physiol (2023) 155(6):e202313340. PMID: 37078900

See MEDIA for molecular dynamics simulations from this study.

2022

Bechthold E, Grey L, Diamant E, Schmidt J, Steigerwald R, Zhao F, Hansen KB, Bunch L, Clausen RP, Wünsch B. In vitro ADME characterization of a very potent 3-acylamino-2-aminopropionic acid-derived GluN2C-NMDA receptor agonist and its ester prodrugs. Biol Chem (2022) 404(4):255-265. PMID: 36427206

Zhao F, Mazis G, Yi F, Lotti JS, Layeux MS, Schultz EP, Bunch L, Hansen KB, Clausen RP. Discovery of (R)-2-amino-3-triazolpropanoic acid derivatives as NMDA receptor glycine site agonists with GluN2 subunit-specific activity. Front Chem (2022) 10:1008233. PMID: 36465862

Elmasri M, Lotti JS, Aziz W, Steele OG, Karachaliou E, Sakimura K, Hansen KB, Penn AC. Synaptic Dysfunction by Mutations in GRIN2B: Influence of Triheteromeric NMDA Receptors on Gain-of-Function and Loss-of-Function Mutant Classification. Brain Sci (2022) 12(6):789. PMID: 35741674

Zhao F, Atxabal U, Mariottini S, Yi F, Lotti JS, Rouzbeh N, Liu N, Bunch L, Hansen KB, Clausen RP. Derivatives of (R)-3-(5-Furanyl)carboxamido-2-aminopropanoic Acid as Potent NMDA Receptor Glycine Site Agonists with GluN2 Subunit-Specific Activity. J Med Chem (2022) 65(1):734-746. PMID: 34918931.

2021

Hansen KB, Wollmuth LP, Bowie D, Furukawa H, Menniti FS, Sobolevsky AI, Swanson GT, Swanger SA, Greger IH, Nakagawa T, McBain CJ, Jayaraman V, Low CM, Dell’Acqua ML, Diamond JS, Camp CR, Perszyk RE, Yuan H, Traynelis SF. Structure, Function, and Pharmacology of Glutamate Receptor Ion Channels. Pharmacol Rev (2021) 73(4):298-487. PMID: 34753794.

Maolanon A, Papangelis A, Kawiecki D, Mou TC, Syrenne JT, Yi F, Hansen KB, Clausen RP. Stereoselective synthesis of novel 2′-(S)-CCG-IV analogues as potent NMDA receptor agonists. Eur J Med Chem (2021) 212:113099. PMID: 33383257.

Strong KL, Epplin MP, Ogden KK, Burger PB, Kaiser TM, Wilding TJ, Kusumoto H, Camp CR, Shaulsky G, Bhattacharya S, Perszyk RE, Menaldino DS, McDaniel MJ, Zhang J, Le P, Banke TG, Hansen KB, Huettner JE, Liotta DC, Traynelis SF. Distinct GluN1 and GluN2 Structural Determinants for Subunit-Selective Positive Allosteric Modulation of N-Methyl-d-aspartate Receptors. ACS Chem Neurosci (2021) 12(1):79-98. PMID: 33326224.

2020

Zhu Z, Yi F, Epplin MP, Liu D, Summer SL, Mizu R, Shaulsky G, XiangWei W, Tang W, Burger PB, Menaldino DS, Myers SJ, Liotta DC, Hansen KB, Yuan H, Traynelis SF. Negative allosteric modulation of GluN1/GluN3 NMDA receptors. Neuropharmacology (2020) 176:108117. PMID: 32389749.

Yi F, Rouzbeh N, Hansen KB, Xu Y, Fanger CM, Gordon E, Paschetto K, Menniti FS, Volkmann RA. PTC-174, a positive allosteric modulator of NMDA receptors containing GluN2C or GluN2D subunits. Neuropharmacology (2020) 173:107971. PMID: 31987864.

Kayser S, Hansen JC, Staudt M, Moroz A, Larsen Y, Temperini P, Yi F, Syrenne JT, Krogsgaard-Larsen N, Iliadis S, Nielsen B, Hansen KB, Pickering DS, Bunch L. Stereoselective Synthesis of New (2S,3R)-3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid Analogues Utilizing a C(sp3)-H Activation Strategy and Structure-Activity Relationship Studies at the Ionotropic Glutamate Receptors. ACS Chem Neurosci (2020) 11(5):674-701. PMID: 32065744.

Zhao F, Rouzbeh N, Hansen KB, Clausen RP. Improved synthetic route for the GluN2-specific NMDA receptor glycine site agonist AICP. Tetrahedron Lett (2020) 61(12):151653.

2019

Yi F, Bhattacharya S, Thompson CM, Traynelis SF, Hansen KB. Functional and pharmacological properties of triheteromeric GluN1/2B/2D NMDA receptors. J Physiol (2019) 597(22):5495-5514. PMID: 31541561.

Poulie CBM, Alcaide A, Krell-Jørgensen M, Larsen Y, Astier E, Bjørn-Yoshimoto WE, Yi F, Syrenne JT, Storgaard M, Nielsen B, Frydenvang KA, Jensen AA, Hansen KB, Pickering DS, Bunch L. Design and Synthesis of 2,3- trans-Proline Analogues as Ligands for Ionotropic Glutamate Receptors and Excitatory Amino Acid Transporters. ACS Chem Neurosci (2019) 10(6):2989-3007. PMID: 31124660.

Sainas S, Temperini P, Farnsworth JC, Yi F, Møllerud S, Jensen AA, Nielsen B, Passoni A, Kastrup JS, Hansen KB, Boschi D, Pickering DS, Clausen RP, Lolli ML. Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands. J Med Chem (2019) 62(9):4467-4482. PMID: 30943028.

Marwick KFM, Hansen KB, Skehel PA, Hardingham GE, Wyllie DJA. Functional assessment of triheteromeric NMDA receptors containing a human variant associated with epilepsy. J Physiol (2019) 597(6):1691-1704. PMID: 30604514.

2018

Hansen KB, Yi F, Perszyk RE, Furukawa H, Wollmuth LP, Gibb AJ, Traynelis SF. Structure, function, and allosteric modulation of NMDA receptors. J Gen Physiol (2018) 150(8):1081-1105. PMID: 30037851.

Bhattacharya S, Khatri A, Swanger SA, DiRaddo JO, Yi F, Hansen KB, Yuan H, Traynelis SF. Triheteromeric GluN1/GluN2A/GluN2C NMDARs with Unique Single-Channel Properties Are the Dominant Receptor Population in Cerebellar Granule Cells. Neuron (2018) 99(2):315-328.e5. PMID: 30056832.

Yi F, Zachariassen LG, Dorsett KN, Hansen KB. Properties of Triheteromeric N-Methyl-d-Aspartate Receptors Containing Two Distinct GluN1 Isoforms. Mol Pharmacol (2018) 93(5):453-467. PMID: 29483146.

2017

Gynther M, Proietti Silvestri I, Hansen JC, Hansen KB, Malm T, Ishchenko Y, Larsen Y, Han L, Kayser S, Auriola S, Petsalo A, Nielsen B, Pickering DS, Bunch L. Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist. J Med Chem (2017) 60(23):9885-9904. PMID: 29205034.

Maolanon AR, Risgaard R, Wang SY, Snoep Y, Papangelis A, Yi F, Holley D, Barslund AF, Svenstrup N, Hansen KB, Clausen RP. Subtype-Specific Agonists for NMDA Receptor Glycine Binding Sites. ACS Chem Neurosci (2017) 8(8):1681-1687. PMID: 28514141.

Lind GE, Mou TC, Tamborini L, Pomper MG, De Micheli C, Conti P, Pinto A, Hansen KB. Structural basis of subunit selectivity for competitive NMDA receptor antagonists with preference for GluN2A over GluN2B subunits. Proc Natl Acad Sci U S A (2017) 114(33):E6942-E6951. PMID: 28760974.

Jessen M, Frederiksen K, Yi F, Clausen RP, Hansen KB, Bräuner-Osborne H, Kilburn P, Damholt A. Identification of AICP as a GluN2C-Selective N-Methyl-D-Aspartate Receptor Superagonist at the GluN1 Glycine Site. Mol Pharmacol (2017) 92(2):151-161. PMID: 28588066.

Hansen KB, Yi F, Perszyk RE, Menniti FS, Traynelis SF. NMDA Receptors in the Central Nervous System. Methods Mol Biol (2017) 1677:1-80. PMID: 28986865.

Yi F, Traynelis SF, Hansen KB. Selective Cell-Surface Expression of Triheteromeric NMDA Receptors. Methods Mol Biol (2017) 1677:145-162. PMID: 28986871.

2016

Tamborini L, Chen Y, Foss CA, Pinto A, Horti AG, Traynelis SF, De Micheli C, Mease RC, Hansen KB, Conti P, Pomper MG. Development of Radiolabeled Ligands Targeting the Glutamate Binding Site of the N-Methyl-d-aspartate Receptor as Potential Imaging Agents for Brain. J Med Chem (2016) 59(24):11110-11119. PMID: 28002957.

Yi F, Mou TC, Dorsett KN, Volkmann RA, Menniti FS, Sprang SR, Hansen KB. Structural Basis for Negative Allosteric Modulation of GluN2A-Containing NMDA Receptors. Neuron (2016) 91(6):1316-1329. PMID: 27618671.

Cheriyan J, Balsara RD, Hansen KB, Castellino FJ. Pharmacology of triheteromeric N-Methyl-D-Aspartate Receptors. Neurosci Lett (2016) 617:240-6. PMID: 26917100.

Kristensen AS, Hansen KB, Naur P, Olsen L, Kurtkaya NL, Dravid SM, Kvist T, Yi F, Pøhlsgaard J, Clausen RP, Gajhede M, Kastrup JS, Traynelis SF. Pharmacology and Structural Analysis of Ligand Binding to the Orthosteric Site of Glutamate-Like GluD2 Receptors. Mol Pharmacol (2016) 89(2):253-62. PMID: 26661043.

2015

Zimmerman SS, Khatri A, Garnier-Amblard EC, Mullasseril P, Kurtkaya NL, Gyoneva S, Hansen KB, Traynelis SF, Liotta DC. Correction to “Design, synthesis, and structure-activity relationship of a novel series of GluN2C-selective potentiators”. J Med Chem (2015) 58(6):2862. PMID: 25738634.

2014

Poulsen MH, Andersen J, Christensen R, Hansen KB, Traynelis SF, Strømgaard K, Kristensen AS. Binding of ArgTX-636 in the NMDA receptor ion channel. J Mol Biol (2015) 427(1):176-89. PMID: 24862283.

Khatri A, Burger PB, Swanger SA, Hansen KB, Zimmerman S, Karakas E, Liotta DC, Furukawa H, Snyder JP, Traynelis SF. Structural determinants and mechanism of action of a GluN2C-selective NMDA receptor positive allosteric modulator. Mol Pharmacol (2014) 86(5):548-60. PMID: 25205677.

Hansen KB, Traynelis SF. Glutamate receptors: mechanistic twists and turns. Nat Chem Biol (2014) 10(9):698-9. PMID: 25271345.

Zimmerman SS, Khatri A, Garnier-Amblard EC, Mullasseril P, Kurtkaya NL, Gyoneva S, Hansen KB, Traynelis SF, Liotta DC. Design, synthesis, and structure-activity relationship of a novel series of GluN2C-selective potentiators. J Med Chem (2014) 57(6):2334-56. PMID: 24512267.

Hansen KB, Ogden KK, Yuan H, Traynelis SF. Distinct functional and pharmacological properties of Triheteromeric GluN1/GluN2A/GluN2B NMDA receptors. Neuron (2014) 81(5):1084-1096. PMID: 24607230.

Yuan H, Hansen KB, Zhang J, Pierson TM, Markello TC, Fajardo KV, Holloman CM, Golas G, Adams DR, Boerkoel CF, Gahl WA, Traynelis SF. Functional analysis of a de novo GRIN2A missense mutation associated with early-onset epileptic encephalopathy. Nat Commun (2014) 5:3251. PMID: 24504326.

2013

Kvist T, Greenwood JR, Hansen KB, Traynelis SF, Bräuner-Osborne H. Structure-based discovery of antagonists for GluN3-containing N-methyl-D-aspartate receptors. Neuropharmacology (2013) 75:324-36. PMID: 23973313.

Kvist T, Steffensen TB, Greenwood JR, Mehrzad Tabrizi F, Hansen KB, Gajhede M, Pickering DS, Traynelis SF, Kastrup JS, Bräuner-Osborne H. Crystal structure and pharmacological characterization of a novel N-methyl-D-aspartate (NMDA) receptor antagonist at the GluN1 glycine binding site. J Biol Chem (2013) 288(46):33124-35. PMID: 24072709.

Vance KM, Hansen KB, Traynelis SF. Modal gating of GluN1/GluN2D NMDA receptors. Neuropharmacology (2013) 71:184-90. PMID: 23578394.

Hansen KB, Tajima N, Risgaard R, Perszyk RE, Jørgensen L, Vance KM, Ogden KK, Clausen RP, Furukawa H, Traynelis SF. Structural determinants of agonist efficacy at the glutamate binding site of N-methyl-D-aspartate receptors. Mol Pharmacol (2013) 84(1):114-27. PMID: 23625947.

Risgaard R, Nielsen SD, Hansen KB, Jensen CM, Nielsen B, Traynelis SF, Clausen RP. Development of 2′-substituted (2S,1’R,2’S)-2-(carboxycyclopropyl)glycine analogues as potent N-methyl-d-aspartic acid receptor agonists. J Med Chem (2013) 56(10):4071-81. PMID: 23614571.

2012

Hedegaard M, Hansen KB, Andersen KT, Bräuner-Osborne H, Traynelis SF. Molecular pharmacology of human NMDA receptors. Neurochem Int (2012) 61(4):601-9. PMID: 22197913.

Vance KM, Hansen KB, Traynelis SF. GluN1 splice variant control of GluN1/GluN2D NMDA receptors. J Physiol (2012) 590(16):3857-75. PMID: 22641781.

Hansen KB, Ogden KK, Traynelis SF. Subunit-selective allosteric inhibition of glycine binding to NMDA receptors. J Neurosci (2012) 32(18):6197-208. PMID: 22553026.

2011

Acker TM, Yuan H, Hansen KB, Vance KM, Ogden KK, Jensen HS, Burger PB, Mullasseril P, Snyder JP, Liotta DC, Traynelis SF. Mechanism for noncompetitive inhibition by novel GluN2C/D N-methyl-D-aspartate receptor subunit-selective modulators. Mol Pharmacol (2011) 80(5):782-95. PMID: 21807990.

Hansen KB, Traynelis SF. How glutamate receptor subunits mix and match: details uncovered. Neuron (2011) 71(2):198-200. PMID: 21791278.

Kvist T, Hansen KB, Bräuner-Osborne H. The use of Xenopus oocytes in drug screening. Expert Opin Drug Discov  (2011) 6(2):141-53. PMID: 22647133.

2010

Risgaard R, Hansen KB, Clausen RP. Partial agonists and subunit selectivity at NMDA receptors. Chemistry (2010) 16(47):13910-8. PMID: 20945316.

Mullasseril P, Hansen KB, Vance KM, Ogden KK, Yuan H, Kurtkaya NL, Santangelo R, Orr AG, Le P, Vellano KM, Liotta DC, Traynelis SF. A subunit-selective potentiator of NR2C- and NR2D-containing NMDA receptors. Nat Commun (2010) 1:90. PMID: 20981015.

Hansen KB, Furukawa H, Traynelis SF. Control of assembly and function of glutamate receptors by the amino-terminal domain. Mol Pharmacol (2010) 78(4):535-49. PMID: 20660085.

Conti P, Pinto A, Tamborini L, Madsen U, Nielsen B, Bräuner-Osborne H, Hansen KB, Landucci E, Pellegrini-Giampietro DE, De Sarro G, Donato Di Paola E, De Micheli C. Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists: design, synthesis, and pharmacological characterization. ChemMedChem (2010) 5(9):1465-75. PMID: 20665761.

Traynelis SF, Wollmuth LP, McBain CJ, Menniti FS, Vance KM, Ogden KK, Hansen KB, Yuan H, Myers SJ, Dingledine R. Glutamate receptor ion channels: structure, regulation, and function. Pharmacol Rev (2010) 62(3):405-96. PMID: 20716669.

Mosley CA, Acker TM, Hansen KB, Mullasseril P, Andersen KT, Le P, Vellano KM, Bräuner-Osborne H, Liotta DC, Traynelis SF. Quinazolin-4-one derivatives: A novel class of noncompetitive NR2C/D subunit-selective N-methyl-D-aspartate receptor antagonists. J Med Chem (2010) 53(15):5476-90. PMID: 20684595.

Hansen KB, Mullasseril P, Dawit S, Kurtkaya NL, Yuan H, Vance KM, Orr AG, Kvist T, Ogden KK, Le P, Vellano KM, Lewis I, Kurtkaya S, Du Y, Qui M, Murphy TJ, Snyder JP, Bräuner-Osborne H, Traynelis SF. Implementation of a fluorescence-based screening assay identifies histamine H3 receptor antagonists clobenpropit and iodophenpropit as subunit-selective N-methyl-D-aspartate receptor antagonists. J Pharmacol Exp Ther (2010) 333(3):650-62. PMID: 20197375.

Lolli ML, Giordano C, Pickering DS, Rolando B, Hansen KB, Foti A, Contreras-Sanz A, Amir A, Fruttero R, Gasco A, Nielsen B, Johansen TN. 4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues. J Med Chem (2010) 53(10):4110-8. PMID: 20408529.

Andersen J, Olsen L, Hansen KB, Taboureau O, Jørgensen FS, Jørgensen AM, Bang-Andersen B, Egebjerg J, Strømgaard K, Kristensen AS. Mutational mapping and modeling of the binding site for (S)-citalopram in the human serotonin transporter. J Biol Chem (2010) 285(3):2051-63. PMID: 19892699.

2009

Zhong H, Hansen KB, Boyle NJ, Han K, Muske G, Huang X, Egebjerg J, Sánchez C. An allosteric binding site at the human serotonin transporter mediates the inhibition of escitalopram by R-citalopram: kinetic binding studies with the ALI/VFL-SI/TT mutant. Neurosci Lett (2009) 462(3):207-12. PMID: 19616061.

Yuan H, Hansen KB, Vance KM, Ogden KK, Traynelis SF. Control of NMDA receptor function by the NR2 subunit amino-terminal domain. J Neurosci (2009) 29(39):12045-58. PMID: 19793963.

Andersen J, Taboureau O, Hansen KB, Olsen L, Egebjerg J, Strømgaard K, Kristensen AS. Location of the antidepressant binding site in the serotonin transporter: importance of Ser-438 in recognition of citalopram and tricyclic antidepressants. J Biol Chem (2009) 284(15):10276-84. PMID: 19213730.

Hansen KB, Naur P, Kurtkaya NL, Kristensen AS, Gajhede M, Kastrup JS, Traynelis SF. Modulation of the dimer interface at ionotropic glutamate-like receptor delta2 by D-serine and extracellular calcium. J Neurosci (2009) 29(4):907-17. PMID: 19176800.

Sivaprakasam M, Hansen KB, David O, Nielsen B, Traynelis SF, Clausen RP, Couty F, Bunch L. Stereocontrolled synthesis and pharmacological evaluation of azetidine-2,3-dicarboxylic acids at NMDA receptors. ChemMedChem (2009) 4(1):110-7. PMID: 19009584.

Hansen KB, Bräuner-Osborne H. FLIPR assays of intracellular calcium in GPCR drug discovery. Methods Mol Biol (2009) 552:269-78. PMID: 19513656.

Hansen KB, Bräuner-Osborne H. Xenopus oocyte electrophysiology in GPCR drug discovery. Methods Mol Biol (2009) 552:343-57. PMID: 19513662.

2008

Clausen RP, Christensen C, Hansen KB, Greenwood JR, Jørgensen L, Micale N, Madsen JC, Nielsen B, Egebjerg J, Bräuner-Osborne H, Traynelis SF, Kristensen JL. N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands. J Med Chem (2008) 51(14):4179-87. PMID: 18578474.

Hansen KB, Bräuner-Osborne H, Egebjerg J. Pharmacological characterization of ligands at recombinant NMDA receptor subtypes by electrophysiological recordings and intracellular calcium measurements. Comb Chem High Throughput Screen (2008) 11(4):304-15. PMID: 18473740.

2007

Erreger K, Geballe MT, Kristensen A, Chen PE, Hansen KB, Lee CJ, Yuan H, Le P, Lyuboslavsky PN, Micale N, Jørgensen L, Clausen RP, Wyllie DJ, Snyder JP, Traynelis SF. Subunit-specific agonist activity at NR2A-, NR2B-, NR2C-, and NR2D-containing N-methyl-D-aspartate glutamate receptors. Mol Pharmacol (2007) 72(4):907-20. PMID: 17622578.

Naur P, Hansen KB, Kristensen AS, Dravid SM, Pickering DS, Olsen L, Vestergaard B, Egebjerg J, Gajhede M, Traynelis SF, Kastrup JS. Ionotropic glutamate-like receptor delta2 binds D-serine and glycine. Proc Natl Acad Sci U S A (2007) 104(35):14116-21. PMID: 17715062.

Hansen KB, Yuan H, Traynelis SF. Structural aspects of AMPA receptor activation, desensitization and deactivation. Curr Opin Neurobiol (2007) 17(3):281-8. PMID: 17419047.

Christiansen B, Hansen KB, Wellendorph P, Bräuner-Osborne H. Pharmacological characterization of mouse GPRC6A, an L-alpha-amino-acid receptor modulated by divalent cations. Br J Pharmacol (2007) 150(6):798-807. PMID: 17245368.

Jørgensen CG, Clausen RP, Hansen KB, Bräuner-Osborne H, Nielsen B, Metzler B, Kehler J, Krogsgaard-Larsen P, Madsen U. Synthesis and pharmacology of glutamate receptor ligands: new isothiazole analogues of ibotenic acid. Org Biomol Chem (2007) 5(3):463-71. PMID: 17340770.

2005

Hansen KB, Clausen RP, Bjerrum EJ, Bechmann C, Greenwood JR, Christensen C, Kristensen JL, Egebjerg J, Bräuner-Osborne H. Tweaking agonist efficacy at N-methyl-D-aspartate receptors by site-directed mutagenesis. Mol Pharmacol (2005) 68(6):1510-23. PMID: 16131614.

Conti P, De Amici M, Grazioso G, Roda G, Pinto A, Hansen KB, Nielsen B, Madsen U, Bräuner-Osborne H, Egebjerg J, Vestri V, Pellegrini-Giampietro DE, Sibille P, Acher FC, De Micheli C. Synthesis, binding affinity at glutamic acid receptors, neuroprotective effects, and molecular modeling investigation of novel dihydroisoxazole amino acids. J Med Chem (2005) 48(20):6315-25. PMID: 16190758.

Wellendorph P, Hansen KB, Balsgaard A, Greenwood JR, Egebjerg J, Bräuner-Osborne H. Deorphanization of GPRC6A: a promiscuous L-alpha-amino acid receptor with preference for basic amino acids. Mol Pharmacol (2005) 67(3):589-97. PMID: 15576628.

2004

Clausen RP, Hansen KB, Calí P, Nielsen B, Greenwood JR, Begtrup M, Egebjerg J, Bräuner-Osborne H. The respective N-hydroxypyrazole analogues of the classical glutamate receptor ligands ibotenic acid and (RS)-2-amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic acid. Eur J Pharmacol (2004) 499(1-2):35-44. PMID: 15363949.

2003

Brehm L, Greenwood JR, Hansen KB, Nielsen B, Egebjerg J, Stensbøl TB, Bräuner-Osborne H, Sløk FA, Kronborg TT, Krogsgaard-Larsen P. (S)-2-Amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid, a potent and selective agonist at the GluR5 subtype of ionotropic glutamate receptors. Synthesis, modeling, and molecular pharmacology. J Med Chem (2003) 46(8):1350-8. PMID: 12672235.