Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Klaus Schiene"'
Autor:
Stefanie Frosch, Frank Porreca, Wolfgang P. Schröder, Klaus Schiene, Jennifer Y. Xie, Thomas Christoph, Klaus Linz, Thomas M. Tzschentke
Publikováno v:
Behavioural Pharmacology. 30:320-326
The aim of this study was to investigate the efficacy of cebranopadol in two rodent models of visceral pain. Cebranopadol is a first-in-class analgesic with agonist activity at the nociceptin/orphanin FQ opioid peptide receptor and classical µ-, δ-
Publikováno v:
Biochemical and biophysical research communications. 500(2)
N-ethyl-N-nitrosourea (ENU) random mutagenesis was used to generate a mouse model for the analysis of the transient receptor potential vanilloid 1 (TRPV1) cation channel. A transversion from T→A in exon 4 led to a Leu206Stop mutation generating a l
Publikováno v:
European Journal of Pharmacology. 754:61-65
Peripheral receptors may contribute to the effects of systemically administered centrally available analgesics. In the present study, we analysed the effect of local peripheral injection of the nociceptin/orphanin FQ peptide (NOP) receptor agonist Ro
Autor:
Sunho Lee, Jin Hee Lee, Jeewoo Lee, Sven Frormann, Suyoung Yoon, Klaus Schiene, Robert Frank-Foltyn, Peter M. Blumberg, Gregor Bahrenberg, Jihyae Ann, Hannelore Stockhausen, Sungeun Kim, Thomas Christoph, Wei Sun, Sun Choi, Aeran Jung, Hyo Shin Kim
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:803-806
A series of N -[{2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)-pyridin-3-yl}methyl] N ′-(6,6-fused heterocyclic) ureas have been investigated as h TRPV1 antagonists. Among them, compound 15 showed highly potent TRPV1 antagonism to capsaicin, with
Publikováno v:
European Journal of Pharmacology. 741:264-271
Targeting functionally independent receptors may provide synergistic analgesic effects in neuropathic pain. To examine the interdependency between different opioid receptors (µ-opioid peptide [MOP], δ-opioid peptide [DOP] and κ-opioid peptide [KOP
Autor:
Thomas M. Tzschentke, Michael Gautrois, Wolfgang P. Schröder, Stefan Schunk, Werner Englberger, Horst Beier, Thomas Christoph, Klaus Schiene, Jean De Vry, Thomas Koch, Babette Kögel, Ulrich Jahnel, Klaus Linz, Stefanie Frosch
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 349:535-548
Cebranopadol (trans-6'-fluoro-4',9'-dihydro-N,N-dimethyl-4-phenyl-spiro[cyclohexane-1,1'(3'H)-pyrano[3,4-b]indol]-4-amine) is a novel analgesic nociceptin/orphanin FQ peptide (NOP) and opioid receptor agonist [Ki (nM)/EC50 (nM)/relative efficacy (%):
Publikováno v:
European Journal of Pain. 18:204-212
Background Innate responses against spontaneous pain are proposed to improve the predictive validity of preclinical analgesia models. Therefore, development and validation of novel readouts is necessary. To investigate whether innate rodent burrowing
Autor:
Tae-Hwan Ha, Sun Choi, HyungChul Ryu, Jeewoo Lee, Klaus Schiene, Dong Wook Kang, Gregor Bahrenberg, Myeong Seop Kim, Thomas Christoph, Shivaji A. Thorat, Ho Shin Kim, Sungeun Kim, Karam Son, Peter M. Blumberg, Robert Frank, Jihyae Ann
Publikováno v:
European Journal of Medicinal Chemistry. 64:589-602
The structure activity relationships of 2-oxy pyridine derivatives in the C-region of N-(6-trifluoromethyl- pyridin-3-ylmethyl) 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as hTRPVl antagonists were investigated. The analysis indicated that
Autor:
Robert B. Raffa, Wolfgang Strasburger, Torsten Hertrampf, Klaus Schiene, Helmut Buschmann, Werner Englberger, Thomas Christoph, Gary Eichenbaum, Rolf Terlinden, Babette Kögel, Christopher M. Flores, Thomas M. Tzschentke
Publikováno v:
Expert Opinion on Pharmacotherapy. 13:1437-1449
Many opioid analgesics share common structural elements; however, minor differences in structure can result in major differences in pharmacological activity, pharmacokinetic profile, and clinical efficacy and tolerability.This review compares and con
Publikováno v:
European Journal of Pharmacology. 666:72-79
Neuropathic pain is a clinical condition which remains poorly treated and combinations of pregabalin, an antagonist of the α2δ-subunit of Ca(2+) channels, with tapentadol, a μ-opioid receptor agonist/noradrenaline reuptake inhibitor, or with class