A5102909121- Pesticide Exposure and Toxicity
- Insect and Pesticide Research
- Cholinesterase and Neurodegenerative Diseases
- Receptor Mechanisms and Signaling
- Neuroscience and Neuropharmacology Research
- Nicotinic Acetylcholine Receptors Study
- Neurotransmitter Receptor Influence on Behavior
- Neuropeptides and Animal Physiology
- Ion channel regulation and function
- Environmental Toxicology and Ecotoxicology
- Social and Demographic Issues in Germany
- Pain Mechanisms and Treatments
- Neuroscience and Neural Engineering
- Phosphodiesterase function and regulation
- Anesthesia and Neurotoxicity Research
- Hearing Loss and Rehabilitation
- Synthesis and Biological Evaluation
- Pesticide and Herbicide Environmental Studies
- Pharmacological Receptor Mechanisms and Effects
- Animal Ecology and Behavior Studies
- Schizophrenia research and treatment
- Anesthesia and Sedative Agents
- Attention Deficit Hyperactivity Disorder
- Neural dynamics and brain function
- Renin-Angiotensin System Studies
Institut für Pharmakologie und Toxikologie der Bundeswehr
2013-2024
Universität der Bundeswehr München
2013-2024
HES-SO University of Applied Sciences and Arts Western Switzerland
2021
Solothurner Spitäler
2021
Kantonsspital Graubünden
2021
Kantonsspital Aarau
2021
University of Bern
2021
Swiss Cancer League
2021
University Hospital of Lausanne
2021
Institute of Pharmacology
2011-2017
Here we describe the properties of CP-154,526, a potent and selective nonpeptide antagonist corticotropin (ACTH) releasing factor (CRF) receptors. CP-154,526 binds with high affinity to CRF receptors (Ki < 10 nM) blocks CRF-stimulated adenylate cyclase activity in membranes prepared from rat cortex pituitary. Systemically administered antagonizes stimulatory effects exogenous on plasma ACTH, locus coeruleus neuronal firing startle response amplitude. Potential anxiolytic was revealed...
Ziprasidone (CP-88,059) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects in preclinical assays predictive of antipsychotic activity. Whereas the compound vitro vivo, its most action antagonism 5-HT2A receptors, where affinity an order magnitude greater than that observed for D2 sites. Laboratory clinical findings have led to hypothesis receptors brain limits undesirable motor side associated with blockade improves efficacy against negative...
CP-96,345, a nonpeptide substance P antagonist, is selective for the tachykinin NK1 receptor. The compound binds to single population of sites in guinea pig brain and potently inhibits P-induced excitation locus ceruleus neurons. CP-96,345 should be useful tool studying action central nervous system.
The selective NK 1 receptor antagonist, CP‐99,994, produced dose‐related (0.1‐1.0 mg kg −1 , s.c.) inhibition of vomiting and retching in ferrets challenged with central (loperamide apomorphine), peripheral (CuSO 4 ) mixed (ipecac, cisplatin) emetic stimuli. Parallel studies the enantiomer, CP‐100,263 (1 mgkg s.c), which is > 000 fold less potent as a indicated that it was without significant effect against CuSO loperamide, cisplatin apomorphine‐induced emesis. Against ipecac, inhibited...
Muscarinic acetylcholine receptors are known to play key roles in facilitating cognitive processes. However, the specific of individual muscarinic receptor subtypes (M 1 -M 5 ) learning and memory not well understood at present. In present study, we used wild-type (M2 +/+ M 2 receptor-deficient -/- mice examine potential role hippocampal synaptic plasticity. M2 showed significant deficits behavioral flexibility working Barnes circular maze T-maze delayed alternation tests, respectively. The...
Local rates of cerebral glucose utilization were measured in rats by the quantitative 2-deoxy-D-[14C]glucose autoradiographic method during electrical stimulation ventral tegmental area. Rats trained intracranial self-stimulation showed a pattern changes forebrain metabolic activity distinctly different from seen stimulated experimenter. These findings provide information about distribution local specific to reinforced instrumental behavior.
A series of substituted phenethyl derivatives 3-benzisothiazolylpiperazine incorporating potent D2 and 5-HT2A antagonist activity was investigated as an approach to a novel atypical antipsychotic agent. The in vitro profile 8e from this is combination receptor affinity comparable the typical agent haloperidol 5-HT2A/D2 ratio clozapine. In vivo possesses consistent with efficacious less tendency induce extrapyramidal side effects man.
1. To determine how acetylcholine (ACh) modulates the somatodendritic processing of EPSPs, we performed whole-cell recordings from CA1 pyramidal cells hippocampal slices and examined effect cholinergic agonist, carbachol (CCh), on alpha-amino-3-hydroxy-5-methyl isoxazole-4-propionate (AMPA) miniature EPSP-like waveforms evoked by brief dendritic glutamate pulses (glutamate-evoked postsynaptic potentials, GPSPs). 2. Although CCh is known to enhance intrinsic excitability neuron in several...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXT1-Naphthylpiperazine derivatives as potential atypical antipsychotic agentsJohn A. Lowe III, Thomas F. Seeger, Arthur Nagel, Harry R. Howard, Patricia Seymour, James H. Heym, Frank E. Ewing, Michael Newman, Anne W. Schmidt, and Cite this: J. Med. Chem. 1991, 34, 6, 1860–1866Publication Date (Print):June 1, 1991Publication History Published online1 May 2002Published inissue 1 June...
A series of 2-aryloxy-4-alkoxy-pyridines ( 1) was identified as novel, selective, and orally active antagonists the corticotropin-releasing factor 1 (CRF receptor. Among these, compound 2 (CP-316311) is a potent selective CRF receptor antagonist with an IC 50 value 6.8 nM in binding demonstrates oral efficacy central nervous system (CNS) vivo models. The regiochemistry compounds this determined by X-ray structural analysis. method to control regioselectivity via pyridine- N-oxides developed....
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTAn initial three-component pharmacophore for specific serotonin-3 receptor ligandsJames P. Rizzi, Arthur A. Nagel, Terry Rosen, Stafford McLean, and Thomas SeegerCite this: J. Med. Chem. 1990, 33, 10, 2721–2725Publication Date (Print):October 1, 1990Publication History Published online1 May 2002Published inissue 1 October 1990https://pubs.acs.org/doi/10.1021/jm00172a007https://doi.org/10.1021/jm00172a007research-articleACS PublicationsRequest reuse...
The quantitative 2-deoxy[14C]glucose method was used to determine local cerebral glucose utilization in unrestrained rats responding (lever-press) for rewarding electrical stimulation area A10 (ventral tegmental area) and similarly implanted inactive controls. Self-stimulation associated with significant increases metabolic activity, highly circumscribed the ventral area, that continued rostrally within a rather compact zone of activity through medial forebrain bundle, extending via diagonal...