Research Topics
| T WeiserSummaryAffiliation: Boehringer Ingelheim Publications
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Detail Information
Publications
BIIR 561 CL: a novel combined antagonist of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors and voltage-dependent sodium channels with anticonvulsive and neuroprotective propertiesT Weiser
Boehringer Ingelheim Pharma KG, Department of CNS Research, Ingelheim, Germany
J Pharmacol Exp Ther 289:1343-9. 1999..These data show that BIIR 561 CL is a combined antagonist of AMPA receptors and voltage-gated sodium channels with promising anticonvulsive and neuroprotective properties...- Characterization of the anticonvulsant and neuroprotectant BIIR 561 CL in vitro: effects on native and recombinant alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptorsT Weiser
Boehringer Ingelheim Pharma KG, Germany
Naunyn Schmiedebergs Arch Pharmacol 362:419-26. 2000..8 s; tauoff=1.3 s in hGluR1/2 receptors with 30 microM BIIR 561 CL). Thus, BIIR 561 CL can be anticipated to have a promising profile for the treatment of neurological disorders like brain ischaemia and head trauma... - Inhibition of tetrodotoxin (TTX)-resistant and TTX-sensitive neuronal Na(+) channels by the secretolytic ambroxolThomas Weiser
Department CNS Research, Boehringer Ingelheim Pharma KG, Ingelheim, Germany
Mol Pharmacol 62:433-8. 2002..g., lidocaine or benzocaine), the potency for Na(+) channel block was relatively high. A recent clinical trial has further confirmed that ambroxol relieved pain and was beneficial in patients who suffered from sore throat... - AMPA receptor antagonists with additional mechanisms of action: new opportunities for neuroprotective drugs?Thomas Weiser
Department CNS Research, Boehringer Ingelheim Pharma KG, Binger Strasse, Ingelheim, D 55216, Germany
Curr Pharm Des 8:941-51. 2002.... - In vivo pharmacology of BIIR 561 CL, a novel combined antagonist of AMPA receptors and voltage-dependent Na(+) channelsM Wienrich
Boehringer Ingelheim, Ingelheim, Germany
Br J Pharmacol 133:789-96. 2001..p.) injection. The data show that the combination of blocking AMPA receptor- and voltage-gated Na(+) channels in one molecule induces effective protection in animal models of neuronal over-excitation... - Potent blockade of sodium channels and protection of brain tissue from ischemia by BIII 890 CLA J Carter
Departments of Central Nervous System Research, Boehringer Ingelheim Pharma KG, 55216 Ingelheim am Rhein, Germany
Proc Natl Acad Sci U S A 97:4944-9. 2000..Our results demonstrate that BIII 890 CL is a potent, selective, and highly use-dependent Na(+) channel blocker that protects brain tissue from the deleterious effects of focal cerebral ischemia in rodents... - Interactions of the dye Evans Blue and GYKI 52466, a 2,3-benzodiazepine, with (S)- alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors in cultured rat cortical neurons: electrophysiological evidence for at least two different binding sites T Weiser
Boehringer Ingelheim KG, Department of Biological Research, CNS Pharmacology, Ingelheim, Germany
Neurosci Lett 216:29-32. 1996..We therefore conclude that GYKI 52466 and Evans Blue bind to two different sites at AMPA receptors in primary cultured cortical neurons... - The AMPA receptor/Na(+) channel blocker BIIR 561 CL is protective in a model of global cerebral ischaemiaT Weiser
Department of CNS Research, Boehringer Ingelheim Pharma KG, D-52218 Ingelheim, Germany
Eur J Pharmacol 421:165-70. 2001..A compound with these properties might be an interesting candidate for the treatment of disorders related to global cerebral ischaemia in man... - Comparison of the effects of four Na+ channel analgesics on TTX-resistant Na+ currents in rat sensory neurons and recombinant Nav1.2 channelsThomas Weiser
Department CNS Research, Boehringer Ingelheim Pharma GmbH and Co KG, D 88397 Biberach, Germany
Neurosci Lett 395:179-84. 2006..Based on the drugs' potencies found in this study, and the published information on clinically achievable plasma levels, the amount of Na(+) channel block to induce analgesia after systemic administration was estimated... - Ambroxol, a Nav1.8-preferring Na(+) channel blocker, effectively suppresses pain symptoms in animal models of chronic, neuropathic and inflammatory painWolfram Gaida
Department of CNS Research, Boehringer Ingelheim Pharma GmbH and Co KG, D-88397 Biberach, Germany
Neuropharmacology 49:1220-7. 2005..These data show that a Nav1.8-preferring Na(+) channel blocker can effectively suppress pain symptoms in a variety of models for chronic, neuropathic and inflammatory pain at plasma levels, which can be achieved in the clinic... - AMPA receptor antagonists for the treatment of strokeThomas Weiser
CNS Research, Boehringer Ingelheim Pharma GmbH and Co KG, Birkendorfer Strasse, D 88397 Biberach, Germany
Curr Drug Targets CNS Neurol Disord 4:153-9. 2005..The latter compound is also described as blocker of voltage-gated sodium channels. Targetting more than one mechanism in the excitotoxicity cascade might be a fruitful approach for the development of neuroprotective drugs... - A novel toxicity-based assay for the identification of modulators of voltage-gated Na+ channelsThomas Weiser
Boehringer Ingelheim Pharma GmbH and Co KG, D 88397 Biberach, Germany
J Neurosci Methods 137:79-85. 2004..1 +/- 0.08; correlation coefficient: 0.93). In summary, these data show that this novel toxicity assay is well suited to test Na+ channel blockers... - The effects of IDRA 21, a positive modulator of the AMPA receptor, on delayed matching performance by young and aged rhesus monkeysJerry J Buccafusco
Alzheimer s Research Center, Medical College of Georgia, Augusta, GA 30912, USA
Neuropharmacology 46:10-22. 2004..They also indicate that the drug is associated with long-term effects that could limit dosing regimens to one dose every two or three days. The nature of the protracted mnemonic effects produced by the compound remains to be elucidated... - Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of strokeMatthias Grauert
Department of Medicinal Chemistry, Boehringer Ingelheim Pharma KG, 88397 Biberach an der Riss, and Corporate Development, Boehringer Ingelheim GmbH, 55216 Ingelheim am Rhein, Germany
J Med Chem 45:3755-64. 2002..This compound was chosen as the best candidate for further pharmacological investigations... - Ambroxol: a CNS drug?Thomas Weiser
Department of Medical Sciences, Boehringer Ingelheim Pharma GmbH and Co, KG, Ingelheim, Germany
CNS Neurosci Ther 14:17-24. 2008..The analgesic effects of ambroxol by either systemic administration to animals, or by topical application in humans can be explained by ambroxol-induced blockade of ion channels in peripheral neurons... - [Local anesthetics and pain therapy in pharyngitis]Horst Wunderer
Boehringer Ingelheim Pharma GmbH and Co. KG, 88400 Biberach
Med Monatsschr Pharm 27:342-7. 2004 - Toxicogenomics in the pharmaceutical industry: hollow promises or real benefit?Anke Luhe
F Hoffmann La Roche Ltd, Non Clinical Drug Safety, 4070 Basel, Switzerland
Mutat Res 575:102-15. 2005.... - Assessment of hepatotoxic liabilities by transcript profilingStefan Ruepp
F Hoffmann La Roche Ltd, PRBN S 90 5 18, CH 4070 Basel, Switzerland
Toxicol Appl Pharmacol 207:161-70. 2005..Together, these results support the useful application of toxicogenomics in raising alerts for adverse effects and generating mechanistic hypotheses that can be followed up by confirmatory experiments...