Ralvenius WT, Acuna MA, Benke D, Matthey A, Daali Y, Rudolph U, Desmeules J, Zeilhofer HU, Besson M, The clobazam metabolite N-desmethyl clobazam is an α2 preferring benzodiazepine with an improved therapeutic window for antihyperalgesia

Neuropharmacology Jul5;109:366-375 (2016)

Behlke LM, Foster RA, Liu J, Benke D, Benham RS, Nathanson AJ, Yee BK, Zeilhofer HU, Engin E, Rudolph U, A Pharmacogenetic „Restriction-of-Function“ Approach Reveals Evidence for Anxiolytic-Like Actions Mediated by α5-Containing GABAA Receptors in Mice

Neuropsychopharmacology May11 (2016)

Acuna MA, Yevenes GE, Ralvenius WT, Benke D, Di Lio A, Lara CO, Munoz B, Burgos CF, Moraga-Cid G, Corringer PJ, Zeilhofer HU, Phosphorylation state-dependent modulation of spinal glycine receptors alleviates inflammatory pain J Clin Invest.Jul1;126(7):2547-60 (2016)


Bessons M, Matthey A, Daali Y, Poncet A, Vuillemier P, Curatolo M, Zeilhofer HU, GABAergic modulation in central sensitization in humans: a randomized placebo-controlled pharmacokinetic-pharmacodynamic study comparing clobazam with clonazepam in healthy volunteers. Pain Mar;156(3):397-404 (2015)


Giber K, Diana MA, Plattner VM, Dugué GP, Bokor H, Rousseau CV, Magloczky Z, Havas L, Hangya B, Wildner H, Zeilhofer HU, Dieudonné S, Acsady L, A subcortical inhibitory signal for behavioral arrest in the thalamus. Nat Neurosci. Apr;18(4):562-568 (2015)


Foster E, Wildner H, Tudeau L, Haueter S, Ralvenius WT, Jegen M, Johannssen H, Hösli L, Haenraets K, Ghanem A, Conzelmann KK, Bösl M, Zeilhofer HU, Targeted ablation, silencing, and activation establish glycinergic dorsal horn neurons as key components of a spinal gate for pain and itch. Neuron Mar;18;85(6):1289-304 (2015)

Husson Z, Rousseau CV, Broll I, Zeilhofer HU, Dieudonné S, Differential GABAergic and glycinergic inputs of inhibitory interneurons and purkinje cells to principal cells of the cerebellar nuclei J Neurosci. Jul 9;34(28):9418-31 (2014)  
Maier PJ, Zemoura K, Acuna MA, Yévenes GE, Zeilhofer HU, Benke D, Ischemia-like oxygen and glucose deprivation mediates down-regulation of cell surface γ-aminobutyric acidB receptors via the endoplasmic reticulum (ER) stress-induced transcription factor CCAAT/enhancer-binding protein (C/EBP)-homologous protein (CHOP) J Biol Chem. May 2;289(18):12896-907 (2014)  
Hermann M, Stillhard, P, Wildner H, Seruggia D, Kapp V, Sanchez-Iranzo H, Mercader N, Montoliu L, Zeilhofer HU, Pelczar P, Binary recombinase systems for high-resolution conditional mutagenesis Nucleic Acids Res. April;42(6):3894-907 (2014)  
Punnakkal P, von Schoultz C, Haenraets K, Wildner H, Zeilhofer HU, Morphological, biophysical and synaptic properties of glutamatergic neurons of the mouse spinal dorsal horn J Physiol. Feb 15;592(PT 4):759-76 (2014)  

Paul J, Yévenes GE, Benke D, Di Lio AD, Ralvenius WT, Witschi R, Scheurer L, Cook JM, Rudolph U, Fritschy JM, Zeilhofer HU, Anthihyperalgesia by a2-GABAA Receptors Occurs Via a Genuine Spinal Action and Does Not Involve Supraspinal Sites. Neurophsychopharmacology Jan;39(2):477-87 (2014)

Zemoura K, Schenkel M, Acuna MA, Yévenes GE, Zeilhofer HU, Benke D, Endoplasmic reticulum-associated degradation controls cell surface expression of y-aminobutyric acis, type B receptors J. Biol Chem. Nov 29;288(48);34897-905 (2013)  

Tyagarajan SK, Ghosh H, Yévenes GE, Imanishi SY, Zeilhofer HU, Gerrits B, Fritschy JM, Extracellular signal-regulated kinase and glycogen synthase kinase 3β regulate gephyrin postsynaptic aggregatin and GABAergic synaptic function in a calpain-dependent mechanism. J Biol Chem. Apr 5;288(14)9634-47 (2013)


Wildner H, Das Gupta R, Bröhl D, Heppenstall PA, Zeilhofer HU, Birchmeier C, Genome-wide expression analysis of pft1a- and ascl1-deficient mice reveals new markers for distinct dorsal horn interneuron populations contributing to nociceptive reflex plasticity. J Neurosci. Apr 24;33(17):7299-307 (2013)


Besson M, Daali Y, Lio AD, Dayer P, Zeilhofer HU, Desmeules J, Antihyperalgesic Effect oft he GABAA Ligand Clobazam in a Neuropathic Pain Model in Mice: A Pharmacokinetic-Pharmacodynamic Study. Basic Clin Pharmacol Toxicol. Mar;112(3):192-7(2013)


Paul J, Zeilhofer HU, Fritschy JM, Selective distribution of GABAA receptor subtypes in mouse spinal dorsal horn neurons and primary afferents. J Comp Neurol. Dec 1:520(17):3895-911 (2012)


Kato A, Punnakkal P, Pernia-Andrade AJ, von Schoultz C, Sharapov S, Nyilas R, Katona I, Zeilhofer HU, Endocannabinoid-dependent plasticity at spinal nociceptor synapses. J. Physiol. Oct; 590(Pt 19):4717-33 (2012)


Bosshard SC, Granjean J, Schroeter A, Baltes C, Zeilhofer HU, Rudin M, Hyperalgesia by low doses of the local anesthetic lidocaine involves annabinoid signaling: an fMRI study in mice. Pain Jul;153(7):1450-8 (2012)


Yévenes GE, Zeilhofer HU, Molecular sites fort the positive allosteric modulation of glycine receptors by endocannabinoids. PLoS One. Aug; 6(8):e23886 (2011)


Witschi R, Punnakkal P, Paul J, Walczak JS, Cervero F, Fritschy JM, Kuner R, Keist R, Rudolph U, Zeilhofer HU, Presynaptic α2-GABAA Receptors in Primary Afferent Depolarization and Spinal Pain Control. J. Neurosci. June 1; 31(22):8134-8142. (2011)


Johansson T, Narumiya S, Zeilhofer HU, Contribution of peripheral versus central EP1 prostaglandin receptors to inflammatory pain. Neurosci Lett. May 16; 495(2):98-101. (2011)


Di Lio A, Benke D, Besson M, Desmeules J, Daali Y, Wang Zj, Edwankar R, Cook JM, Zeilhofer HU, HZ166, a novel GABAA receptor subtype-selective benzodiazepine site ligand, is antihyperalgesic in mouse models of inflammatory and neuropathic pain. Neuropharmacology. Mar;60(4):626-32 (2011)


Röhn TA, Ralvenius WT, Paul J, Borter P, Hernandez M, Witschi R, Grest P, Zeilhofer HU, Bachmann MF, Jennings GT, A virus-like particle-based anti-nerve growth factor vaccine reduces inflammatory hyperalgesia: potential long-term therapy for chronic pain. J Immunol. Feb 1;186(3):1769-80 (2011)


Tyagarajan SK, Ghosh H, Yévenes GE, Nikonenko I, Ebeling C, Schwerdel C, Sidler C, Zeilhofer HU, Gerrits B, Muller D, Fritschy JM, Regulation of GABAergic synapse formation and plasticity by GSK3β-dependent phosphorylation of gephyrin. Proc Natl Acad Sci USA Jan 4;108(1):379-84 (2011)

Witschi R, Johansson T, Morscher G, Scheurer L, Deschamps J, Zeilhofer HU, Hoxb8-CreMice: A tool for brain-sparing conditional gene deletion. Genesis Oct 1;48(10):596-602. (2010)  
Johansson T, Broll I, Frenz T, Hemmers S, Becher B, Zeilhofer HU, Buch T. Building a zoo of mice for genetic analyses: A comprehensive protocol for the rapid generation of BAC transgenic mice. Genesis Apr; 48(4):264-280. (2010)  
Andratsch M, Mair N, Constantin CE, Scherbakov N, Benetti C, Quarta S, Vogl C, Sailer CA, Uceyler N, Brockhaus J, Martini R, Sommer C, Zeilhofer HU, Müller W, Kuner R, Davis JB, Rose-John S, Kress M. A key role for gp130 expressed on peripheral sensory nerves in pathological pain. J Neurosci. Oct 28; 29(43):13473-83. (2009)  
Restrepo CE, Lundfald L, Szabó G, Erdélyi F, Zeilhofer HU, Glover JC, Kiehn O. Transmitter-phenotypes of commissural interneurons in the lumbar spinal cord of newborn mice. J Comp Neurol. Jul 16; 517(2):177-192. (2009)  
Bagnall MW, Zingg B, Sakatos A, Moghadam SH, Zeilhofer HU, Lac S. Glycinergic projection neurons of the cerebellum. J Neurosci. Aug 12; 29(32):10104-10. (2009)  
Knabl J, Zeilhofer UB, Crestani F, Rudolph U, Zeilhofer HU. Genuine antihyperalgesia by systemic diazepam revealed by experiments in GABAA receptor point-mutated mice. Pain Feb;141(3):233-8. (2009)  
Knabl J, Witschi R, Hösl K, Reinold H, Zeilhofer UB, Ahmadi S, Brockhaus J, Sergejeva M, Hess A, Brune K, Fritschy JM, Rudolph U, Möhler H, Zeilhofer HU. Reversal of pathological pain through specific spinal GABAA receptor subtypes. Nature Jan 17;451(7176):330-4. (2008)  
Lundfald L, Restrepo CE, Butt SJ, Peng CY, Droho S, Endo T, Zeilhofer HU, Sharma K, Kiehn O. Phenotype of V2-derived interneurons and their relationship to the axon guidance molecule EphA4 in the developing mouse spinal cord. Eur J Neurosci. Dec;26(11):2989-3002. (2007)  
Nazzaro C, Rizzi A, Salvadori S, Guerrini R, Regoli D, Zeilhofer HU, Calo G. UFP-101 antagonizes the spinal antinociceptive effects of nociceptin/orphanin FQ: Behavioral and electrophysiological studies in mice. Peptides  28(3):663-9. (2007)  
Hess A, Sergejeva M, Budinsky L, Zeilhofer HU, Brune K. Imaging of hyperalgesia in rats by functional MRI. Eur J Pain 11:109-119. (2007)  
Hösl K, Reinold H, Müller U, Narumiya S, Zeilhofer HU. Spinal prostaglandin E receptors of the EP2 subtype and the glycine receptor α3 subunit, which mediate central Inflammatory hyperalgesia, do not contribute to pain after peripheral nerve injury or formalin injection. Pain 126:46-53. (2006)  
Rizzi A, Nazzaro C, Marzola G, Zucchini S, Trapella C, Guerrini R, Zeilhofer HU, Regoli D, Calò G. Endogenous nociceptin/orphanin FQ signalling produces opposite spinal antinociceptive and supraspinal pronociceptive effects in the mouse formalin test: pharmacological and genetic evidences. Pain 124:100-108. (2006)  
Dumitrescu O, Protti DA, Majumdar S, Zeilhofer HU, Wässle H. Ionotropic glutamate receptors in the mouse retina. Visual Neurosci. 23:79-90. (2006)  
Reinold H, Ahmadi S, Depner UB, Layh B, Heindl C, Hamza M, Pahl A, Brune K, Narumiya S, Müller U, Zeilhofer HU. Spinal Inflammatory Hyperalgesia Is Mediated by Spinal Prostaglandin E Receptors of the EP2 Subtype. J Clin Invest 115:673–679. (2005)  
Zeilhofer HU, Studler B, Arabadzisz D, Schweizer C, Ahmadi S, Layh B, Bösl MR, Fritschy J-M. Glycinergic neurons expressing EGFP in BAC transgenic mice. J Comp Neurol 482:123-141. (2005)  
Hartmann B, Ahmadi S, Heppenstall PA, Lewin G, Schott C, Borchardt T, Seeburg PH, Zeilhofer HU, Sprengel R, Kuner R. The AMPA receptor subunits, GluR-A and GluR-B reciprocally modulate spinal synaptic plasticity and inflammatory pain. Neuron 44:637-650. (2004)  
Muth-Selbach, U, Dybek E, Kollosche K, Stegmann J-U, Holthusen, H, Lipfert P, Zeilhofer HU. The spinal antinociceptive effect of nocistatin in neuropathic rats is blocked by D-serine. Anesthesiology 101:753-758. (2004)  
Haverkamp S, Müller U, Zeilhofer HU, Harvey RJ, Wässle H. Diversity of glycine receptors in the mouse retina: localization of the α2 subunit. J Comp Neurol 477:399-411. (2004)  
Harvey RJ, Depner UB, Wässle H, Ahmadi S, Heindl C, Reinold H, Smart TG, Harvey K, Schütz B, Abo-Salem OM, Zimmer A, Poisbeau P, Welzl H, Wolfer DP, Betz H, Zeilhofer HU, Müller U. GlyR α3: An essential target for spinal inflammatory pain sensitization. Science 304:884-887 (2004)  
Harvey RJ, Depner UB, Wässle H, Ahmadi S, Heindl C, Reinold H, Smart TG, Harvey K, Schütz B, Abo-Salem OM, Zimmer A, Poisbeau P, Welzl H, Wolfer DP, Betz H, Zeilhofer HU, Müller U. GlyR α3: An essential target for spinal inflammatory pain sensitization. Science 304:884-887 (2004) (Suppl.)  
Bayer K, Ahmadi S, Zeilhofer HU. Gabapentin may inhibit synaptic transmission in the mouse spinal cord dorsal horn through a preferential block of P/Q-type Ca2+ channels. Neuropharmacol 46:743-749. (2004)  
Ahmadi S, Muth-Selbach U, Lauterbach A, Lipfert P, Neuhuber WL, Zeilhofer HU. Facilitation of spinal NMDA receptor-currents by synaptically released glycine. Science 300:2094-209. (2003)1.13 Ahmadi S, Muth-Selbach U, Lauterbach A, Lipfert P, Neuhuber WL, Zeilhofer HU. Facilitation of spinal NMDA receptor-currents by synaptically released glycine. Science 300:2094-209. (2003)  
Depner UB, Reinscheid RK, Takeshima H, Brune K, Zeilhofer HU. Normal sensitivity of acute pain, but increased inflammatory hyperalgesia in mice lacking the nociceptin precursor polypeptide or the nociceptin receptor. Eur J Neurosci 17:2381-2387. (2003)  
von Wegerer J, Becker K, Glockenhammer D, Becker CM, Zeilhofer HU, Swandulla D. Spinal inhibitory synaptic transmission in the glycine receptor mouse mutant spastic. Neurosci Lett 345:45-48. (2003)  
Becker L, v. Wegerer J, Schenkel J, Zeilhofer HU, Swandulla D, Weiher H. Disease-specific human glycine receptor α1 subunit causes hyperekplexia phenotype and impaired glycine- and GABAA receptor transmission in transgenic mice. J Neurosci 22:2505-2512. (2002)  
Ahmadi S, Lippross S, Neuhuber WL, Zeilhofer HU. PGE2 selectively blocks inhibitory glycinergic neurotransmission onto rat superficial dorsal horn neurons. Nat Neurosci 5:34-40. (2002)  


Zeilhofer HU, Wildner H, Yévenes GE, Fast synaptic inhibition in spinal sensory processing and pain control. Physiol Rev. Jan; 92(1):193-235. (2012)
Zeilhofer HU, Benke D, Yévenes GE, Chronic Pain States: Pharmacological Strategies to Restore Diminished Inhibitory Spinal Pain Control. Annu Rev Pharmacol Toxicol. Feb 10;52:111-33 (2012)
Yévenes GE, Zeilhofer HU, Allosteric Modulation of Glycine Receptors. Br J Pharmacol. Sep; 164(2): 224-36 (2011)
Zeilhofer HU, Moehler H, Di Lio A. GABAergic analgesia: new insights from mutant mice and subtype-selective agonists. Trends Pharmacol Sci. Jul 16. Aug; 30(8):397-402 (2009)
Zeilhofer HU, Witschi R, Hoesl K. Subtype-selective GABAA receptor mimetics-novel antihyperalgesic agents? J Mol Med. (Berl) May;87(5):465-9 (2009)
Zeilhofer HU. Zeilhofer UB. Spinal dis-inhibition in inflammatory pain. Neurosci Lett. Jun 6;437(3):170-4. (2008)
Zeilhofer HU. Loss of glycinergic and GABAergic inhibition in chronic pain--contributions of inflammation and microglia. Int Immunopharmacol. Feb; 8 (2):182-7. (2008) 
Zeilhofer HU. Prostanoids in Nociception and Pain. Biochem Pharmacol 73:165-174. (2007)
Zeilhofer HU, Brune K. Analgesic strategies beyond inhibition of cyclooxygenases. Trends Pharmacol Sci 27:467-74. (2006)
Zeilhofer HU. Synaptic Modulation in Pain Pathways. Reviews Physiol, Biochem Pharmacol 155:73-100. (2005)
Zeilhofer HU. The glycinergic control of nociception. Cell Mol Life Sci 62:2027-2035. (2005)
Zeilhofer HU, Calò G. Nociceptin/orphanin FQ and its receptor – Potential targets for pain therapy? J Pharmacol Exp Ther 306:423-429. (2003)


  1. Zeilhofer HU, Ralvenius WT, Acuna MA, Restoring the spinal pain gate: GABA(A) receptors as targets for novel analgesics. Adv Pharmacol.73:71-96 (2015)
  2. Harkany T, Zeilhofer HU, Cattaneo A, Neurotrophin and endocanabinoid interactions in the neurobiology of pain. Eur J Neurosci. Feb;39(3):331-3 (2014)
  3. Benke D, Zeilhofer HU, Divorce of obligatory partners in pain: disruption of GABAB receptor heterodimers in neuralgia. EMBO J. Aug 1; 31(15)3234-6 (2012)
  4. Zeilhofer HU, Spinal neuroplasticity in chronic pain. e-Neuroforum 2:35-41. (2011)
  5. Zeilhofer HU. Spinal cannabinoids – a double-edged sword? (Commentary on Zhang et al.) European Journal of Neuroscience Jan; 31(2):223-4. (2010)
  6. Zeilhofer HU. Etifoxine (Stresam ®) for chemotherapy-induced pain? Pain. Oct 10. [Epub ahead of print] No abstract available. (2009)
  7. Brune K, Zeilhofer HU. Antipyretic analgesics: basic aspects In: McMahon SB, Koltzenburg M: Wall and Melzack’s Textbook of Pain, 6th edition. pp 459-469. Churchill Livingstone, Edinburgh. (2006)  
  8. Zeilhofer HU, Ahmadi S, Lauterbach A, Lippross S. Glycinergic neurotransmission and the control of spinal hyperalgesia. In: Handwerker HO, Brune K: Hyperalgesia: Molecular Mechanisms and Clinical Implications. 2003 IASP Research symposium. IASP press Seattle, (2004)
  9. Zeilhofer HU, Sittl R. Kapitel 6: Therapie mit Analgetika und Lokalanästhetika. In: Lemmer, Brune: Pharmakotherapie. Springer Verlag, Heidelberg, pages 81-92. (2004)
  10. Zeilhofer HU, Okuda-Ashitaka E, Reinscheid RK. Nociceptin/orphanin FQ, Nocistatin and Pain. Proceedings of the 10th World Congress on Pain, Progress in Pain Research and Management 24, (ed. Dostrovsky JO, Carr DB, Koltzenburg M, IASP Press, Seattle). (2003)
  11. Hinz B, Zeilhofer HU, Brune K. Non-opioid analgesics. In: Bruera ED, Portenoy RK: Cancer Pain. Assessment and Management. Cambridge University Press. New York. (2003)
  12. Zeilhofer HU, Brune K. A role for COX-1 in neuropathic pain? Anesthesiol 99:1043-1044. (2003)
  13. Brune K, Zeilhofer HU. Antipyretic analgesics. In: Melzack R, Wall PD: Handbook of Pain Management. pp 339-351. Churchill Livingstone, Edinburgh. (2003)