A5025531394- Chemical Synthesis and Analysis
- Chemical Reactions and Isotopes
- Receptor Mechanisms and Signaling
- Neuroscience and Neuropharmacology Research
- Nicotinic Acetylcholine Receptors Study
- Synthesis and Biological Evaluation
- Radiopharmaceutical Chemistry and Applications
- Cholinesterase and Neurodegenerative Diseases
- Forensic Toxicology and Drug Analysis
- Celiac Disease Research and Management
- Neuropeptides and Animal Physiology
- Neurotransmitter Receptor Influence on Behavior
- Amino Acid Enzymes and Metabolism
- Helicobacter pylori-related gastroenterology studies
- Medical Imaging Techniques and Applications
- Diabetes and associated disorders
- Traumatic Brain Injury and Neurovascular Disturbances
- Neuroendocrine regulation and behavior
- Chemical synthesis and alkaloids
- Mass Spectrometry Techniques and Applications
- Ion channel regulation and function
- Adenosine and Purinergic Signaling
- Galectins and Cancer Biology
- Coordination Chemistry and Organometallics
- Boron Compounds in Chemistry
Technical University of Denmark
2010-2017
Tracer Technologies (United States)
2010
Centre for Sustainable Energy
2010
Background: Pituitary adenylate cyclase activating peptide-38 (PACAP-38) has been shown to induce migraine in migraineurs, whereas the related peptide vasoactive intestinal (VIP) does not. In present study we examine hypothesis that PACAP-38 and its truncated version PACAP-27 but not VIP cause degranulation of mast cells peritoneum dura mater. Methods: The degranulatory effects PACAP-38, were investigated by measuring amount N-acetyl-β-hexosaminidase released from isolated peritoneal mater...
The isoxazol-3-one tautomer of the bicyclic isoxazole, 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol (THAZ), has previously been shown to be a weak GABA(A) and glycine receptor antagonist. In present study, potential in this scaffold explored through synthesis pharmacological characterization series N- O-substituted THAZ analogues. analogues N-Bn-THAZ (3d) O-Bn-THAZ (4d) were found potent agonists human 5-HT(2A) 5-HT(2C) receptors. Judging from an elaborate profiling at numerous other...
Gluten promotes type 1 diabetes in nonobese diabetic (NOD) mice and likely also humans. In NOD non-diabetes-prone mice, it induces inflammation the pancreatic lymph nodes, suggesting that gluten can initiate locally. Further, gliadin fragments stimulate insulin secretion from beta cells directly. We hypothesized may cross intestinal barrier to be distributed organs other than gut. If present pancreas, could interact directly with immune system development. orally intravenously administered...
3-Hydroxycyclopent-1-enecarboxylic acid (HOCPCA, 1) is a potent ligand for the high-affinity GHB binding sites in CNS. An improved synthesis of 1 together with very efficient [(3)H]-1 described. The radiosynthesis employs situ generated lithium trimethoxyborotritide. Screening against different CNS targets establishes high selectivity, and we demonstrate vivo brain penetration. In vitro characterization shows specificity to sites.
γ-Hydroxybutyric acid (GHB) is a psychotropic compound endogenous to the brain. Despite its potential physiological significance, complete molecular mechanisms of action remain unexplained. To facilitate isolation and identification high-affinity GHB binding site, we herein report design synthesis first 125I-labeled radioligands in field, one which contains photoaffinity label enables it bind irreversibly sites.
γ-Hydroxybutyric acid (GHB) is a therapeutic drug, drug of abuse, and an endogenous substance that binds to low- high-affinity sites in the mammalian brain. To target specific GHB binding sites, we have developed <sup>125</sup>I-labeled analog characterized its rat brain homogenate slices. Our data show [<sup>125</sup>I]4-hydroxy-4-[4-(2-iodobenzyloxy)phenyl]butanoate ([<sup>125</sup>I]BnOPh-GHB) one site cortical membranes with low nanomolar affinity (<i>K</i><sub>d</sub>, 7 nM;...
3-Hydroxycyclopent-1-ene-1-carboxylic acid (HOCPCA (1)) is a potent ligand for high-affinity γ-hydroxybutyric binding sites in the central nervous system. Various approaches to introduction of hydrogen label onto HOCPCA skeleton are reported. The outcomes feasible C─H activation olefin carbon (C-2) by iridium catalyst compared with reduction carbonyl group (C-3) freshly prepared borodeuterides. most efficient catalysts proved be Kerr bulky phosphine N-heterocyclic species providing...
Although the selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor UCPH-101 has become a standard pharmacological tool compound for in vitro and ex vivo studies EAAT research field, its inability to penetrate blood-brain barrier makes it unsuitable studies. In present study, per os (p.o.) administration (40 mg kg(-1) ) of closely related analogue UCPH-102 rats yielded respective plasma brain concentrations 10.5 6.67 μm after h. Three series were designed synthesized improve...
In the interest of developing efficient methods for tritium labelling peptides, we here demonstrate successful PACAP‐38 (pituitary adenylate cyclase‐activating polypeptide), a 38‐mer peptide, using synthetic diiodinated precursor. this example, employ standard hydrogenation chemistry with use heterogeneous palladium catalyst and carrier‐free gas on manifold system. Copyright © 2011 John Wiley & Sons, Ltd.
Abstract In our efforts to develop new reactions for the efficient labelling of peptides and proteins with tritium, we now report use silane hydrides together homogenous Pd(0) catalysis protio‐ deuteriodeiodination an o ‐iodo‐tyrosine containing peptide (angiotensin‐I) performed at room temperature. Copyright © 2010 John Wiley & Sons, Ltd.