Chris G Parsons
Affiliation: Merz Pharmaceuticals
- Peripherally acting NMDA receptor/glycineB site receptor antagonists inhibit morphine toleranceWojciech Danysz
Merz Pharmaceuticals GmbH, Eckenheimer Landstrasse 100, 60318 Frankfurt Main, Germany
Neuropharmacology 48:360-71. 2005..The present data suggest that blockade of NMDA receptor/glycine(B) sites in the periphery may attenuate tolerance to the antinociceptive effects of morphine...
- Memantine does not show intracellular block of the NMDA receptor channelChris G Parsons
Merz Pharmaceuticals GmbH, Eckenheimer Landstrasse 100, D 60318, Frankfurt, Germany
Eur J Pharmacol 587:99-103. 2008..In conclusion, intracellular block of the NMDA receptor, as reported for Mg2+, is not of significance for the therapeutic effects of memantine...
- MRZ-99030 - A novel modulator of Aβ aggregation: I - Mechanism of action (MoA) underlying the potential neuroprotective treatment of Alzheimer's disease, glaucoma and age-related macular degeneration (AMD)Christopher G Parsons
Merz Pharmaceuticals, Eckenheimer Landstrasse 100, D 60318 Frankfurt, Germany Electronic address
Neuropharmacology 92:158-69. 2015..Moreover, in vivo studies demonstrate the neuroprotective potential of MRZ-99030 after systemic and topical administration in animal models of Alzheimer's disease and glaucoma/AMD respectively...
- Patch clamp combined with voltage/concentration clamp to determine the kinetics and voltage dependency of N-methyl-D-aspartate (NMDA) receptor open channel blockersChris G Parsons
Pharmacology, Non Clinical Science, Merz Pharmaceuticals GmbH, Eckenheimer Landstraße 100, 60318, Frankfurt am Main, Germany
Methods Mol Biol 1183:43-63. 2014....
- Pharmacodynamics of memantine: an updateG Rammes
Clinical Neuropharmacology, Max Planck Institute of Psychiatry, 80804 Munich, Germany
Curr Neuropharmacol 6:55-78. 2008..In addition, there has been further confirmation of the MOA of memantine as an uncompetitive NMDA receptor antagonist and essentially no data contradicting our understanding of the benign side effect profile of memantine...
- Memantine and cholinesterase inhibitors: complementary mechanisms in the treatment of Alzheimer's diseaseChris G Parsons
In Vitro Pharmacology, Merz Pharmaceuticals GmbH, Eckenheimer Landstrasse 100, 60318, Frankfurt, Germany
Neurotox Res 24:358-69. 2013..Preclinical data have shown how these drugs act via two different, but interconnected, pathological pathways, and that their complementary activity may produce greater effects than either drug individually...
- Blocking kinetics of memantine on NR1a/2A receptors recorded in inside-out and outside-out patches from Xenopus oocytesChris G Parsons
In Vitro Pharmacology, Preclinical Research and Development, Merz Pharmaceuticals GmbH, Eckenheimer Landstrasse 100, D 60318, Frankfurt am Main 1, Germany
J Neural Transm 115:1367-73. 2008..These results provide further support for the hypothesis that rapid relief of block via strong synaptic membrane depolarisation underlies the good therapeutic profile of memantine...
- Memantine as an example of a fast, voltage-dependent, open channel N-methyl-D-aspartate receptor blockerChris G Parsons
Head in Vitro Pharmacology, Preclinical Research and Development, Merz Pharmaceuticals GmbH, Germany
Methods Mol Biol 403:15-36. 2007....
- The NMDA receptor antagonist memantine as a symptomatological and neuroprotective treatment for Alzheimer's disease: preclinical evidenceWojciech Danysz
Merz Pharmaceuticals GmbH, Frankfurt am Main, Germany
Int J Geriatr Psychiatry 18:S23-32. 2003..As such, if overactivation of NMDA receptors is present in AD, memantine would be expected to improve both symptoms (cognition) and to slow down disease progression because it takes over the physiological function of magnesium...
- Potency, voltage-dependency, agonist concentration-dependency, blocking kinetics and partial untrapping of the uncompetitive N-methyl-D-aspartate (NMDA) channel blocker memantine at human NMDA (GluN1/GluN2A) receptorsKate E Gilling
In Vitro Pharmacology, Preclinical Research and Development, Merz Pharmaceuticals GmbH, Eckenheimer Landstrasse 100, D 60318 Frankfurt am Main 1, Germany
Neuropharmacology 56:866-75. 2009....
- Alzheimer's disease, β-amyloid, glutamate, NMDA receptors and memantine--searching for the connectionsWojciech Danysz
Merz Pharmaceuticals GmbH, Eckenheimer Landstraße, Frankfurt am Main, Germany
Br J Pharmacol 167:324-52. 2012....
- Memantine: a NMDA receptor antagonist that improves memory by restoration of homeostasis in the glutamatergic system--too little activation is bad, too much is even worseChris G Parsons
Merz Pharmaceuticals, Eckenheimer Landstrasse 100, 60318 Frankfurt am Main, Germany
Neuropharmacology 53:699-723. 2007....
- Assessment of the effects of NS11394 and L-838417, α2/3 subunit-selective GABA(A) [corrected] receptor-positive allosteric modulators, in tests for pain, anxiety, memory and motor functionMartine Hofmann
Departments of In vivo Pharmacology, Merz Pharmaceuticals GmbH, Frankfurt am Main, Germany
Behav Pharmacol 23:790-801. 2012..Therefore, the anxiolytic effect and the lack of side-effects of these compounds, as described in the literature, could not be confirmed in the present study...
- Brain concentrations of mGluR5 negative allosteric modulator MTEP in relation to receptor occupancy - Comparison to MPEPJens Nagel
Merz Pharmaceuticals GmbH, Frankfurt Main, Germany
Pharmacol Rep 67:624-30. 2015..To verify relation between brain free levels, receptor occupancy in vivo and in vitro affinity at the target for mGluR5 negative allosteric modulator (NAM) MTEP...
- Chronic memantine does not block 3-nitropropionic acid-delayed ischaemic tolerance in rat hippocampal slices ex vivoTadeusz Frankiewicz
Department of Preclinical Research and Development, Merz Pharmaceuticals GmbH, Eckenheimer Landstrasse 100, 60318 Frankfurt Main, Germany
Neurotox Res 5:617-22. 2004..3%). We conclude that although NMDA receptors do seem to be involved in chemically-induced ischaemic tolerance, semi-chronic pre-treatment with therapeutically-relevant doses of memantine does not block ischaemic tolerance...
- Potential role of N-methyl-D-aspartate receptors as executors of neurodegeneration resulting from diverse insults: focus on memantineGary L Wenk
Department Psychology and Neuroscience, Ohio State University, Ohio, USA
Behav Pharmacol 17:411-24. 2006....
- Effects of low-affinity NMDA receptor channel blockers in two rat models of chronic painIvan O Medvedev
Institute of Pharmacology, Pavlov Medical University, 6 8 Lev Tolstoy Street, 197089 St Petersburg, Russia
Neuropharmacology 47:175-83. 2004..Thus, studies on the prevention and management of chronic pain should focus on preemptive or long-term administration of NMDA receptor antagonists...
- Neuroprotective activity of selective mGlu1 and mGlu5 antagonists in vitro and in vivoKinga Szydlowska
Laboratory of Transcription Regulation, The Nencki Institute of Experimental Biology, Pasteur 3 Street, 02 093 Warsaw, Poland
Eur J Pharmacol 554:18-29. 2007..EMQMCM was not protective at 5 mg/kg (given 2 h after occlusion) but at 10 mg/kg 50% of neuroprotection was observed. The present data support stronger neuroprotective potential of mGlu5 than mGlu1 antagonists...
- The antiallodynic effect of NMDA antagonists in neuropathic pain outlasts the duration of the in vivo NMDA antagonismThomas Christoph
Department of Pharmacology, Grünenthal GmbH Research Centre, Zieglerstrasse 6, 52078 Aachen, Germany
Neuropharmacology 51:12-7. 2006..Development of short-acting NMDA antagonists could represent a strategy for improving their tolerability...
- mGlu1 and mGlu5 receptor antagonists lack anticonvulsant efficacy in rodent models of difficult-to-treat partial epilepsyWolfgang Loscher
Department of Pharmacology, Toxicology and Pharmacy, University of Veterinary Medicine, Bunteweg 17, D 30559 Hannover, Germany
Neuropharmacology 50:1006-15. 2006..The present results do not support a significant anticonvulsant potential of group I mGlu receptor antagonists in rodent models of difficult-to-treat partial epilepsy...
- N-methyl-D-aspartate receptors mediate endogenous opioid release in enteric neurons after abdominal surgerySimona Patierno
CURE Digestive Diseases Research Center, Digestive Diseases Division, Department of Medicine, David Geffen School of Medicine, University of California Los Angeles, 90073, USA
Gastroenterology 128:2009-19. 2005..We tested the hypothesis that N-methyl-D-aspartate (NMDA) receptors mediate surgery-induced opioid release in enteric neurons...
- Expression of polyglutamine-expanded huntingtin induces tyrosine phosphorylation of N-methyl-D-aspartate receptorsCheng Song
Department of Pharmacology, Boston University School of Medicine, Boston, Massachusetts 02118, USA
J Biol Chem 278:33364-9. 2003....