Publication Library

Koch ED et al., 2019. Cebranopadol, a Novel First-in-Class Analgesic Drug Candidate: First Experience With Cancer-Related Pain for up to 26 Weeks

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Eerdekens MH et al., 2019. Cancer-related chronic pain: Investigation of the novel analgesic drug candidate cebranopadol in a randomized, double-blind, noninferiority trial

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Christoph T., 2018. Synergistic interaction between the agonism of cebranopadol at nociceptin/orphanin FQ and classical opioid receptors in the rat spinal nerve ligation model

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Schiene K et al., 2018.Inhibition of experimental visceral pain in rodents by cebranopadol

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Schiene, K., 2018. Nociceptin/orphanin FQ opioid peptide (NOP) receptor and µ-opioid peptide (MOP) receptors both contribute to the anti-hypersensitive effect of cebranopadol in a rat model of arthritic pain

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Tzschentke TM & Rutten K.. 2018. Mu-opioid peptide (MOP) and nociceptin/orphanin FQ peptide (NOP) receptor activation both contribute to the discriminative stimulus properties of cebranopadol in the rat.

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Kleideiter E., 2018. Clinical Pharmacokinetic Characteristics of Cebranopadol, a Novel First-in-Class Analgesic

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Tzschentke TM., 2018. Limited potential of cebranopadol to produce opioid-type physical dependence in rodents

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Tzschentke TM., 2017. Antihyperalgesic, Antiallodynic, and Antinociceptive Effects of Cebranopadol, a Novel Potent Nociceptin/Orphanin FQ and Opioid Receptor Agonist, after Peripheral and Central Administration in Rodent Models of Neuropathic Pain

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Linz K et al., 2017. Opioid-type Respiratory Depressant Side Effects of Cebranopadol in Rats Are Limited by Its Nociceptin/Orphanin FQ Peptide Receptor Agonist Activity

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Dahan A., 2017. Respiratory Effects of the Nociceptin/Orphanin FQ Peptide and Opioid Receptor Agonist, Cebranopadol, in Healthy Human Volunteers

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Christoph A et al., 2017. Cebranopadol, a novel first-in-class analgesic drug candidate: first experience in patients with chronic low back pain in a randomized clinical trial

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Linz K et al., 2014. Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist

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Schunk S et al., 2014. Discovery of a Potent Analgesic NOP and Opioid Receptor Agonist: Cebranopadol

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Valdor M et al., 2018. RNA interference-based functional knockdown of the voltage-gated potassium channel Kv7.2 in dorsal root ganglion neurons after in vitro and in vivo gene transfer by adeno-associated virus vectors

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Patel R et al., 2015. Electrophysiological characterization of activation state-dependent Ca(v)2 channel antagonist TROX-1 in spinal nerve injured rats

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Nardi A et al. 2012. Advances in targeting voltage-gated sodium channels with small molecules

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Steinhagen H & Damann N. 2012. Channeling drug discovery

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Pan et al., 2018. Nociceptin/orphanin FQ opioid peptide-receptor expression in pachyonychia congenita

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Rutten et al., 2018. Selectivity profiling of NOP, MOP, DOP and KOP receptor antagonists in the rat spinal nerve ligation model of mononeuropathic pain

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Anand P et al., 2016. Nociceptin/orphanin FQ receptor expression in clinical pain disorders and functional effects in cultured neurons

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Schiene K et al., 2015. Mechanical hyperalgesia in rats with diabetic polyneuropathy is selectively inhibited by local peripheral nociceptin/orphanin FQ receptor and µ-opioid receptor agonism

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Rutten K et al., 2014. Pharmacogenomic study of the role of the nociceptin/orphanin FQ receptor and opioid receptors in diabetic hyperalgesia

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Schunk S. et al., 2014. Discovery of Spiro[cyclohexane-dihydropyrano[3,4-b]indole]-amines as Potent NOP and Opioid Receptor Agonists

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Schröder W et al., 2014. Functional plasticity of the N/OFQ-NOP receptor system determines analgesic properties of NOP receptor agonists

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Rutten K et al., 2010. Pharmacological blockade or genetic knockout of the NOP receptor potentiates the rewarding effect of morphine in rats

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Rutten K et al., 2010. Effects of the NOP receptor agonist Ro65-6570 on the acquisition of opiate- and psychostimulant-induced conditioned place preference in rats

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Bloms-Funke P et al., 2000. Agonistic effects of the opioid buprenorphine on the nociceptin/OFQ receptor

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Christoph T et al., 2006. The antiallodynic effect of NMDA antagonists in neuropathic pain outlasts the duration of the in vivo NMDA antagonism

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Christoph T et al., 2006. Antiallodynic effects of NMDA glycine(B) antagonists in neuropathic pain: possible peripheral mechanisms.

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Gaunitz C et al., 2002. Formalin-induced changes of NMDA receptor subunit expression in the spinal cord of the rat.

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Tzschentke TM, 2002. Glutamatergic mechanisms in different disease states: overview and therapeutical implications -- an introduction.

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Chizh BA, 2002. Novel approaches to targeting glutamate receptors for the treatment of chronic pain: review article.

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Chizh BA et al., 2001. NMDA receptor antagonists as analgesics: focus on the NR2B subtype.

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Chizh BA et al., 2001. Supraspinal vs spinal sites of the antinociceptive action of the subtype-selective NMDA antagonist ifenprodil.

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Tzschentke TM et al., 2000. Blockade of behavioral sensitization by MK-801: fact or artifact? A review of preclinical data.

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Chizh BA et al., 2000. The N-methyl-D-aspartate antagonistic and opioid components of d-methadone antinociception in the rat spinal cord.

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Pippel et al., 2017. Localization of the gate and selectivity filter of the full-length P2X7 receptor

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Hausmann R, Kless A, Schmalzing G. 2015. Key sites for P2X receptor function and multimerization: overview of mutagenesis studies on a structural basis

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Hausmann R et al., 2014. A hydrophobic residue in position 15 of the rP2X3 receptor slows desensitization and reveals properties beneficial for pharmacological analysis and high-throughput screening

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Saul A et al., 2013. Heteromeric assembly of P2X subunits

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Hausmann R et al., 2013.Salt bridge switching from Arg290/Glu167 to Arg290/ATP promotes the closed-to-open transition of the P2X2 receptor

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Wolf C et al., 2011. Molecular determinants of potent P2X2 antagonism identified by functional analysis, mutagenesis, and homology docking

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Gerevich Z et al., 2007. Metabotropic P2Y receptors inhibit P2X3 receptor-channels via G protein-dependent facilitation of their desensitization

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Ramos-Zepeda G et al., 2004. Spinal vs. supraspinal antinociceptive activity of the adenosine A(1) receptor agonist cyclopentyl-adenosine in rats with inflammation

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Gerevich Z et al., 2004. Inhibition of N-type voltage-activated calcium channels in rat dorsal root ganglion neurons by P2Y receptors is a possible mechanism of ADP-induced analgesia

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Chizh BA, Illes P.. 2001. P2Y receptor-mediated inhibition of voltage-dependent Ca2+ channels in rat dorsal root ganglion neurons

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Fischer W et al., 2003. Characterization of P2X3, P2Y1 and P2Y4 receptors in cultured HEK293-hP2X3 cells and their inhibition by ethanol and trichloroethanol

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Borvendeg SJ et al., 2003. Subsensitivity of P2X but not vanilloid 1 receptors in dorsal root ganglia of rats caused by cyclophosphamide cystitis

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Chizh BA, Illes P.. 2001. IP2X receptors and nociception

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Stollenwerk A., 2018. Review of Post-Marketing Safety Data on Tapentadol, a Centrally Acting Analgesic

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Serrie A et al., 2017. Tapentadol prolonged-release for moderate-to-severe chronic osteoarthritis knee pain: a double-blind, randomized, placebo- and oxycodone controlled release-controlled study

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Lange B et al., 2017. Efficacy and safety of tapentadol prolonged release for moderate-to-severe chronic osteoarthritis knee pain: a pooled analysis of two double-blind, randomized, placebo- and oxycodone controlled release-controlled studies

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Baron R et al., 2017. Retrospective analyses versus RCTs: comparing like with like?

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Kress HG et al., 2016. Direct conversion from tramadol to tapentadol prolonged release for moderate to severe, chronic malignant tumour-related pain

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Baron R et al., 2016. Effectiveness of Tapentadol Prolonged Release (PR) Compared with Oxycodone/Naloxone PR for the Management of Severe Chronic Low Back Pain with a Neuropathic Component: A Randomized, Controlled, Open-Label, Phase 3b/4 Study

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Baron R et al., 2016. Effectiveness of Tapentadol Prolonged Release (PR) Compared with Oxycodone/Naloxone PR for the Management of Severe Chronic Low Back Pain with a Neuropathic Component: A Randomized, Controlled, Open-Label, Phase 3b/4 Study

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Sánchez Del Águila MJ et al., 2015. Practical considerations for the use of tapentadol prolonged release for the management of severe chronic pain

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Sadeghi M et al., 2015. μ-Opioid receptor activation and noradrenaline transport inhibition by tapentadol in rat single locus coeruleus neurons

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Hillewaert V et al., 2015. Determination of tapentadol and tapentadol-O-glucuronide in human serum samples by UPLC-MS/MS

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Elling C et al., 2015. Tapentadol prolonged release in the treatment of neuropathic pain related to diabetic polyneuropathy

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Eichenbaum G et al., 2015. Does tapentadol affect sex hormone concentrations differently from morphine and oxycodone? An initial assessment and possible implications for opioid-induced androgen deficiency

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Buynak R et al., 2015. Long-term Safety and Efficacy of Tapentadol Extended Release Following up to 2 Years of Treatment in Patients With Moderate to Severe, Chronic Pain: Results of an Open-label Extension Trial

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Baron R et al., 2015. Effectiveness and Safety of Tapentadol Prolonged Release (PR) Versus a Combination of Tapentadol PR and Pregabalin for the Management of Severe, Chronic Low Back Pain With a Neuropathic Component: A Randomized, Double-blind, Phase 3b Study

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Baron R et al., 2015. Effectiveness and Tolerability of a Moderate Dose of Tapentadol Prolonged Release for Managing Severe, Chronic Low Back Pain with a Neuropathic Component: An Open-label Continuation Arm of a Randomized Phase 3b Study

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Vinik et al., 2014. A randomized withdrawal, placebo-controlled study evaluating the efficacy and tolerability of tapentadol extended release in patients with chronic painful diabetic peripheral neuropathy

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Tzschentke TM et al., 2014. The mu-opioid receptor agonist/noradrenaline reuptake inhibition (MOR-NRI) concept in analgesia: the case of tapentadol

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Schikowski A et al., 2014. Tapentadol prolonged release for severe chronic cancer-related pain: effectiveness, tolerability, and influence on quality of life of the patients

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Sabatowski R et al., 2014. Driving Ability in Patients with Severe Chronic Low Back or Osteoarthritis Knee Pain on Stable Treatment with Tapentadol Prolonged Release: A Multicenter, Open-label, Phase 3b Trial

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Meneghini V et al., 2014. The noradrenergic component in tapentadol action counteracts μ-opioid receptor-mediated adverse effects on adult neurogenesis

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Kress HG et al., 2014. Tapentadol prolonged release for managing moderate to severe, chronic malignant tumor-related pain

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Kögel B et al., 2014. Characterisation of tramadol, morphine and tapentadol in an acute pain model in Beagle dogs

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Galia E., 2014. Evaluation of the tamper-resistant properties of tapentadol extended-release tablets: results of in vitro laboratory analyses

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Etropolski M et al., 2014. Safety and tolerability of tapentadol extended release in moderate to severe chronic osteoarthritis or low back pain management: pooled analysis of randomized controlled trials

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Cowan A et al., 2014. Lack of synergistic interaction between the two mechanisms of action of tapentadol in gastrointestinal transit

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Caputi FF et al., 2014. Opioid receptor gene expression in human neuroblastoma SH-SY5Y cells following tapentadol exposure

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Zannikos PN et al., 2013. Pharmacokinetic evaluation of tapentadol extended-release tablets in healthy subjects

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Steigerwald I et al., 2013. Effectiveness and tolerability of tapentadol prolonged release compared with prior opioid therapy for the management of severe, chronic osteoarthritis pain

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Schwittay A et al., 2013. Tapentadol prolonged release for severe chronic pain: results of a noninterventional study involving general practitioners and internists

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Göhler K et al., 2013. Comparative pharmacokinetics and bioavailability of tapentadol following oral administration of immediate- and prolonged-release formulations

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Gálvez R et al., 2013. Tapentadol prolonged release versus strong opioids for severe, chronic low back pain: results of an open-label, phase 3b study

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Etropolski M et al., 2013. A pooled analysis of patient-specific factors and efficacy and tolerability of tapentadol extended release treatment for moderate to severe chronic pain

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Christoph T et al., 2013. Spinal-supraspinal and intrinsic μ-opioid receptor agonist-norepinephrine reuptake inhibitor (MOR-NRI) synergy of tapentadol in diabetic heat hyperalgesia in mice

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Tzschentke TM et al., 2012. Tapentadol increases levels of noradrenaline in the rat spinal cord as measured by in vivo microdialysis

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Steigerwald I et al., 2012. Effectiveness and safety of tapentadol prolonged release with tapentadol immediate release on-demand for the management of severe, chronic osteoarthritis-related knee pain: results of an open-label, phase 3b study

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Steigerwald I et al., 2012. Effectiveness and safety of tapentadol prolonged release for severe, chronic low back pain with or without a neuropathic pain component: results of an open-label, phase 3b study

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Raffa RB et al., 2012. Mechanistic and functional differentiation of tapentadol and tramadol

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Obradovic M et al., 2012. Cost-effectiveness of tapentadol in severe chronic pain in Spain: a cost analysis of data from RCTs

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Ikenberg R et al., 2012. Cost-effectiveness of tapentadol prolonged release compared with oxycodone controlled release in the UK in patients with severe non-malignant chronic pain who failed 1st line treatment with morphine

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Vorsanger G et al., 2011. Post hoc analyses of data from a 90-day clinical trial evaluating the tolerability and efficacy of tapentadol immediate release and oxycodone immediate release for the relief of moderate to severe pain in elderly and nonelderly patients

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Schwartz S et al., 2011. Safety and efficacy of tapentadol ER in patients with painful diabetic peripheral neuropathy: results of a randomized-withdrawal, placebo-controlled trial

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Schröder W et al., 2011. Synergistic interaction between the two mechanisms of action of tapentadol in analgesia

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Schiene K, De Vry J, Tzschentke TM.. 2011. Antinociceptive and antihyperalgesic effects of tapentadol in animal models of inflammatory pain

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Kögel B et al., 2011. The antinociceptive and antihyperalgesic effect of tapentadol is partially retained in OPRM1 (μ-opioid receptor) knockout mice

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Christoph T et al., 2011. Synergistic antihypersensitive effects of pregabalin and tapentadol in a rat model of neuropathic pain

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Wild JE et al., 2010. Long-term safety and tolerability of tapentadol extended release for the management of chronic low back pain or osteoarthritis pain

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Terlinden R et al., 2010. In vitro and in vivo characterization of tapentadol metabolites

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Schröder W et al., 2010. Differential contribution of opioid and noradrenergic mechanisms of tapentadol in rat models of nociceptive and neuropathic pain

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Oh C et al., 2010. A thorough QT/QTc study of multiple doses of tapentadol immediate release in healthy subjects

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Lange B et al., 2010. Efficacy and safety of tapentadol prolonged release for chronic osteoarthritis pain and low back pain

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Christoph T, De Vry J, Tzschentke TM.. 2010. Tapentadol, but not morphine, selectively inhibits disease-related thermal hyperalgesia in a mouse model of diabetic neuropathic pain

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Afilalo M, Stegmann JU & Upmalis D. 2010 .Tapentadol immediate release: a new treatment option for acute pain management

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Tzschentke TM et al., 2009. Tapentadol hydrochloride: a next-generation, centrally acting analgesic with two mechanisms of action in a single molecule

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Hartrick C et al., 2009. Efficacy and tolerability of tapentadol immediate release and oxycodone HCl immediate release in patients awaiting primary joint replacement surgery for end-stage joint disease: a 10-day, phase III, randomized, double-blind, active- and placebo-controlled study

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Hale M et al., 2009.Tolerability of tapentadol immediate release in patients with lower back pain or osteoarthritis of the hip or knee over 90 days: a randomized, double-blind study

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Daniels SE et al., 2009. A randomized, double-blind, phase III study comparing multiple doses of tapentadol IR, oxycodone IR, and placebo for postoperative (bunionectomy) pain

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Daniels S et al., 2009. A randomized, double-blind, placebo-controlled phase 3 study of the relative efficacy and tolerability of tapentadol IR and oxycodone IR for acute pain

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Stegmann JU et al., 2008. The efficacy and tolerability of multiple-dose tapentadol immediate release for the relief of acute pain following orthopedic (bunionectomy) surgery

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Kneip C et al, 2008. Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes

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Kleinert R et al., 2008. Single dose analgesic efficacy of tapentadol in postsurgical dental pain: the results of a randomized, double-blind, placebo-controlled study

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Tzschentke TM et al., 2007. (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (tapentadol HCl): a novel mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties

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Terlinden R et al., 2007. Absorption, metabolism, and excretion of 14C-labeled tapentadol HCl in healthy male subjects

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Christoph T et al., 2018. Investigation of TRPV1 loss-of-function phenotypes in TRPV1 Leu206Stop mice generated by N-ethyl-N-nitrosourea mutagenesis

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Lee S et al., 2017. Pyrazole C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists

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Lee S et al., 2017. t-Butyl pyridine and phenyl C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists

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Ryu H et al., 2015. Pyridine C-region analogs of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists

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Tran PT et al., 2015. α-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists

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Sun W et al., 2015. 6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists

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Ann J et al., 2015. Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists

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Ryu H et al., 2014. 2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists

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Ryu H et al., 2014. 2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists

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Kim MS et al., 2012. 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent transient receptor potential vanilloid 1 (TRPV1) antagonists: structure-activity relationships of 2-amino derivatives in the N-(6-trifluoromethylpyridin-3-ylmethyl) C-region

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Christoph T et al., 2008. Investigation of TRPV1 loss-of-function phenotypes in transgenic shRNA expressing and knockout mice

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Christoph et al., 2007. Antinociceptive effect of antisense oligonucleotides against the vanilloid receptor VR1/TRPV1

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Christoph T et al., 2006. Silencing of vanilloid receptor TRPV1 by RNAi reduces neuropathic and visceral pain in vivo

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Vulcu SD et al., 2004. Proton conductance of human transient receptor potential-vanilloid type-1 expressed in oocytes of Xenopus laevis and in Chinese hamster ovary cells

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Goswami C et al., 2004. Identification and characterization of a Ca2+ -sensitive interaction of the vanilloid receptor TRPV1 with tubulin

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Behrendt HJ et al., 2004. Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay

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Vulcu SD et al., 2003. The cAMP pathway sensitizes VR1 expressed in oocytes from Xenopus laevis and in CHO cells

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Borvendeg SJ et al., 2003. Subsensitivity of P2X but not vanilloid 1 receptors in dorsal root ganglia of rats caused by cyclophosphamide cystitis

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Jahnel R et al., 2003. Dual expression of mouse and rat VRL-1 in the dorsal root ganglion derived cell line F-11 and biochemical analysis of VRL-1 after heterologous expression

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Himmel HM et al., 2002. The arginine-rich hexapeptide R4W2 is a stereoselective antagonist at the vanilloid receptor 1: a Ca2+ imaging study in adult rat dorsal root ganglion neurons

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Jahnel R et al., 2001. Biochemical characterization of the vanilloid receptor 1 expressed in a dorsal root ganglia derived cell line

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Pletinckx K et al., 2019. Inhibiting the immunoproteasome's β5i catalytic activity affects human peripheral blood-derived immune cell viability

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Alen J et al., 2019. Fragment-Based Discovery of Novel Potent Sepiapterin Reductase Inhibitors

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Rutten K et al., 2018. Standard analgesics reverse burrowing deficits in a rat CCI model of neuropathic pain, but not in models of type 1 and type 2 diabetes-induced neuropathic pain

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Treister R et al., 2018. Accurate pain reporting training diminishes the placebo response: Results from a randomised, double-blind, crossover trial

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Wodarski R et al., 2016. Cross-centre replication of suppressed burrowing behaviour as an ethologically relevant pain outcome measure in the rat: a prospective multicentre study

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Alansary D et al., 2016. Thiol dependent intramolecular locking of Orai1 channels

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Schröder W, Alique M, & Herrero JF, 2016. Effects of the mas-related gene (Mrg) C receptor agonist BAM6-22 on nociceptive reflex activity in naive, monoarthritic and mononeuropathic rats after intraplantar and intrathecal administration

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Quetglas EG et al., 2015. Update on pathogenesis and predictors of response of therapeutic strategies used in inflammatory bowel disease

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Bourgeois C et al., 2014. Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists

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Rutten K et al., 2014. Pharmacological validation of a refined burrowing paradigm for prediction of analgesic efficacy in a rat model of sub-chronic knee joint inflammation

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Rutten K et al., 2014. Burrowing as a non-reflex behavioural readout for analgesic action in a rat model of sub-chronic knee joint inflammation

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Beier H et al., 2008. Semi-mechanistic pharmacokinetic/pharmacodynamic modelling of the antinociceptive response in the presence of competitive antagonism: the interaction between tramadol and its active metabolite on micro-opioid agonism and monoamine reuptake inhibition, in the rat

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Christoph T et al., 2007. Tramadol has a better potency ratio relative to morphine in neuropathic than in nociceptive pain models

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Eitrich T et al., 2007. Classification of highly unbalanced CYP450 data of drugs using cost sensitive machine learning techniques

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Kögel B et al., 2005. Interaction of mu-opioid receptor agonists and antagonists with the analgesic effect of buprenorphine in mice

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Christoph T et al., 2005. Broad analgesic profile of buprenorphine in rodent models of acute and chronic pain

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Streng T et al., 2003. Urodynamic effects of the K+ channel (KCNQ) opener retigabine in freely moving, conscious rats

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Pandita RK et al., 2003. Actions of tramadol on micturition in awake, freely moving rats

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Gillen & Maul, 2002. New pharmacological strategies for pain relief

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