A5028454763- Receptor Mechanisms and Signaling
- Neuroscience and Neuropharmacology Research
- Neurotransmitter Receptor Influence on Behavior
- Ion channel regulation and function
- Pharmacological Receptor Mechanisms and Effects
- Synthesis and Biological Evaluation
- Nicotinic Acetylcholine Receptors Study
- Synthesis and bioactivity of alkaloids
- Neuropeptides and Animal Physiology
- Neuroendocrine regulation and behavior
- Chemical Synthesis and Analysis
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Lipid Membrane Structure and Behavior
- Pain Mechanisms and Treatments
- Nitric Oxide and Endothelin Effects
- Synthesis of heterocyclic compounds
- Chemical Reaction Mechanisms
- Phenothiazines and Benzothiazines Synthesis and Activities
- Quinazolinone synthesis and applications
- Stress Responses and Cortisol
- Adenosine and Purinergic Signaling
- Photoreceptor and optogenetics research
- Malaria Research and Control
- Cannabis and Cannabinoid Research
University of Alberta
2009-2023
Health PEI
2020
University of Prince Edward Island
2020
Research Institute of Health Sciences
2019
Universitat de les Illes Balears
2019
University at Buffalo, State University of New York
2019
Université de Strasbourg
2019
Dalhousie University
2017
Walsh University
2015
St George's Hospital
2014
Saturable binding of (±)‐[ 3 H]‐baclofen and [ H]‐γ‐aminobutyric acid ([ H]‐GABA) to rat brain crude synaptic membranes has been examined by means a centrifugation assay. The could be detected in fresh or previously frozen tissue was dependent on the presence physiological concentrations Ca 2+ Mg although lower affinity Na + ‐dependent component also observed. Both components probably reflect receptor recognition sites. saturable portion bound formed 20.3 ± 6.9% total ligand. This displaced...
Saturable binding of (±)‐[ 3 H]‐baclofen and [ H]‐γ‐aminobutyric acid ([ H]‐GABA) to rat brain crude synaptic membranes has been examined by means a centrifugation assay. The could be detected in fresh or previously frozen tissue was dependent on the presence physiological concentrations Ca 2+ Mg although lower affinity Na + ‐dependent component also observed. Both components probably reflect receptor recognition sites. saturable portion bound formed 20.3 ± 6.9% total ligand. This displaced...
Disposable plasticware such as test tubes, pipette tips, and multiwell assay or culture plates are used routinely in most biological research laboratories. Manufacturing of plastics requires the inclusion numerous chemicals to enhance stability, durability, performance. Some lubricating (slip) agents, exemplified by oleamide, also occur endogenously humans biologically active, cationic biocides included prevent bacterial colonization plastic surface. We demonstrate that these manufacturing...
1 An in vitro receptor autoradiography procedure is described for visualizing binding sites the excitatory amino acid antagonist radiolabelled MK-801, rat and gerbil brain sections. 2 Ten micron sections were labelled by incubation at room temperature 20 min 30 nm [3H]-MK-801. This was followed rinses s fresh buffer solution. Specifically bound ligand determined with 100 μm unlabelled MK-801 amounted to 55–60% of total. 3 Phencyclidine, (±)-SKF 10047, ketamine 2-aminophosphonovaleric (APV)...
Peripheral compression neuropathy is a common clinical entity but little human nerve material has been available for study. It difficult to develop an experimental model of chronic which reliable and reproducible, making it assess the various treatment modalities currently in use manage this problem. In recent study using rat model, connective tissue fiber changes associated with were described by authors. The present expands same multifascicular median cynomolgus monkey, test whether or not...
Abstract: GTP and GDP decreased the saturable binding of [ 3 H]baclofen or H]γ‐aminobutyric acid ([ H]GABA) to GABA B but not A receptors whereas GMP displayed negligible activity. This effect was specific guanyl nucleotides mimicked by high concentrations ATP. The inhibition ligand result a diminished receptor affinity with no change in number. use complete physiological saline solution rather than Tris buffer plus Ca 2+ Mg increased potency at receptor. results are discussed relation...
1 In rat whole brain homogenates, saturation analysis revealed that both [3H]-idazoxan and [3H]-RX821002, a selective α2-adrenoceptor ligand, bound with high affinity to an apparent single population of sites. However, the Bmax for was significantly (P < 0.01) greater than [3H]-RX821002. 2 competition studies, (−)-adrenaline displaced 3 nm binding consistent labelling α2-adrenoceptors. this displacement incomplete since 23.68 ± 1.11% specific remained in presence excess concentration (100...
A novel class of antimalarial pyrido[1,2-a]benzimidazoles were synthesized and evaluated for antiplasmodial activity cytotoxicity following hits identified from screening commercially available compound collections. The most active these, TDR86919 (4c), showed improved in vitro vs the drug-resistant K1 strain Plasmodium falciparum relative to chloroquine (IC(50) = 0.047 μM v 0.17 μM); potency was retained against a range drug-sensitive strains, with negligible mammalian (L-6) cell line...
In the pursuit of new antimalarial leads, a phenotypic screening various commercially sourced compound libraries was undertaken by World Health Organisation Programme for Research and Training in Tropical Diseases (WHO-TDR). We report here detailed characterization one hits from this process, TDR32750 (8a), which showed potent activity against Plasmodium falciparum K1 (EC(50) ~ 9 nM), good selectivity (>2000-fold) compared to mammalian cell line (L6), significant rodent model malaria when...
Nonadrenergic imidazoline binding sites (imidazoline I2 sites) have been described to be colocated with monoamine oxidase (MAO) in the mitochondrial fraction of various cell types. In present work, authors considered whether this colocation could associated a functional interplay. rat liver membranes, [3H]-idazoxan receptors was competed for by naphazoline and idazoxan, which also shared high affinity alpha-2 adrenoceptors (alpha-2 ARs). The chemicals 2-n-heptylimidazoline (S 15430),...
The density of the Imidazoline₂ binding site (I₂BS) has been shown to change in psychiatric conditions such as depression and addiction, along with neurodegenerative disorders Alzheimer's disease Huntington's chorea. presence I₂BS on glial cells possibility that they may some way regulate fibrillary acidic protein led increased interest into role ligands characterized by marked gliosis. In addition, it suggested be a marker for human glioblastomas. Therefore, development positron emission...