Search results for "patch"
showing 10 items of 337 documents
Dolphin morbillivirus epizootic resurgence, Mediterranean Sea
2008
In July 2007, > 100 striped dolphins, Stenella coeruleoalba, were found dead along the coast of the Spanish Mediterranean. Of 10 dolphins tested, 7 were positive for a virus strain closely related to the dolphin morbillivirus that was isolated during a previous epizootic in 1990.
Pharmacological activity of C10-substituted analogs of the high-affinity kainate receptor agonist dysiherbaine
2009
Kainate receptor antagonists have potential as therapeutic agents in a number of neuropathologies. Synthetic modification of the convulsant marine toxin neodysiherbaine A (NDH) previously yielded molecules with a diverse set of pharmacological actions on kainate receptors. Here we characterize three new synthetic analogs of NDH that contain substituents at the C10 position in the pyran ring of the marine toxin. The analogs exhibited high-affinity binding to the GluK1 (GluR5) subunit and lower affinity binding to GluK2 (GluR6) and GluK3 (GluR7) subunits in radioligand displacement assays with recombinant kainate and AMPA receptors. As well, the natural toxin NDH exhibited approximately 100-f…
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
2008
Drugs used to treat various disorders target GABA A receptors. To develop alpha subunit selective compounds, we synthesized 5-(4-piperidyl)-3-isoxazolol (4-PIOL) derivatives. The 3-isoxazolol moiety was substituted by 1,3,5-oxadiazol-2-one, 1,3,5-oxadiazol-2-thione, and substituted 1,2,4-triazol-3-ol heterocycles with modifications to the basic piperidine substituent as well as substituents without basic nitrogen. Compounds were screened by [(3)H]muscimol binding and in patch-clamp experiments with heterologously expressed GABA A alpha ibeta 3gamma 2 receptors (i = 1-6). The effects of 5-aminomethyl-3 H-[1,3,4]oxadiazol-2-one 5d were comparable to GABA for all alpha subunit isoforms. 5-pipe…
Efficacy of fentanyl transdermal patch in pain control after lower third molar surgery: A preliminary study
2015
Background Surgical removal of impacted lower third molars is a common oral surgical procedure, generally followed by moderate to severe postoperative pain. Transdermal drug delivery as a concept offers interesting possibilities for postoperative pain control. The aim of this study was to evaluate the efficacy of transdermal system with fentanyl in relieving pain following impacted lower third molar surgery. Material and Methods Seventeen patients with bilateral impacted lower third molars were included in this preliminary study. For postoperative pain control, patients randomly received a fentanyl patch plus placebo tablet after the first operation and regular (placebo) patch and an analge…
Complement lysis: a hole is a hole.
1991
recent experimental advances 21, it is now possible to produce MACs with a precise molecular composition 7 for better designed experiments. In my judgement, however, it will always be problematic to propose a single unifying mechanism for MAC action simply because MAC effects are not uniform. The reason for attempting to classify MACs as leaky patch or channel formers is a desire to wield Occam's razor and carve out the simplest unifying theory. But this razor often cuts one's throat, especially when it comes to immunological processes. A system that degranulates platelets, 'kills' such widely diverse targets as artificial liposomes, 'dead' viruses and erythrocytes, metabolically active cel…
Reduced presynaptic efficiency of excitatory synaptic transmission impairs LTP in the visual cortex of BDNF-heterozygous mice
2006
The neurotrophin brain-derived neurotrophic factor (BDNF) plays an important role in neuronal survival, axonal and dendritic growth and synapse formation. BDNF has also been reported to mediate visual cortex plasticity. Here we studied the cellular mechanisms of BDNF-mediated changes in synaptic plasticity, excitatory synaptic transmission and long-term potentiation (LTP) in the visual cortex of heterozygous BDNF-knockout mice (BDNF(+/-)). Patch-clamp recordings in slices showed an approximately 50% reduction in the frequency of miniature excitatory postsynaptic currents (mEPSCs) compared to wild-type animals, in the absence of changes in mEPSC amplitudes. A presynaptic impairment of excita…
Estimation of ambient GABA levels in layer I of the mouse neonatal cortex in brain slices
2010
GABAergic synapses on Cajal–Retzius neurons in layer I of the murine neocortex experience GABAB receptor (GABABR)-mediated tonic inhibition. Extracellular GABA concentration ([GABA]o) that determines the strength of GABABR-mediated inhibition is controlled by GABA transporters (GATs). In this study, we hypothesized that the strength ofpresynaptic GABABR activation reflects [GABA]o in the vicinity of synaptic contacts. Slices obtained from two age groups were used, namely postnatal days (P)2–3 and P5–7. GABAergic postsynaptic currents (IPSCs) were recorded using the whole-cell patch-clamp technique. Minimal electrical stimulation in layer I was applied to elicit evoked IPSCs (eIPSCs) using a…
Resonance properties of different neuronal populations in the immature mouse neocortex
2012
In vivo recordings in the immature neocortex revealed spontaneous and sensory-driven oscillatory activity from delta (0.5-4 Hz) to gamma (30-100 Hz) frequencies. In order to investigate whether the resonance properties of distinct neuronal populations in the immature neocortex contribute to these network oscillations, we performed whole-cell patch-clamp recordings from visually identified neurons in tangential and coronal neocortical slices from postnatal day (P)0-P7 C57Bl/6 mice. Subthreshold resonance was analysed by sinusoidal current injection of varying frequency. All Cajal-Retzius cells showed subthreshold resonance, with an average frequency of 2.6 ± 0.1 Hz (n = 60), which was massiv…
Allosterically potentiating ligands of nicotinic receptors as a treatment strategy for Alzheimer's disease.
2000
Abstract One of the most prominent cholinergic deficit in Alzheimer’s disease (AD) is the reduced number of nicotinic acetylcholine receptors (nAChR) in the hippocampus and cortex of AD patients, as compared to age-matched controls. This deficit results in reduced nicotinic cholinergic excitation which may not only impair postsynaptic depolarization but also presynaptic neurotransmitter release and Ca 2+ -dependent intracellular signaling, including transcriptional activity. Presently, the most common approach to correct the nicotinic cholinergic deficit in AD is the application of cholinesterase inhibitors. Due to the resulting increase in synaptic acetylcholine levels, both in concentrati…
Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation
2003
In HEK293 cells stably expressing alpha4beta2 nAChRs, naltrexone, but not naloxone, blocked alpha4beta2 nAChRs via an open-channel blocking mechanism. In primary hippocampal cultures, naltrexone inhibited alpha7 nAChRs up-regulated by nicotine, and in organotypic hippocampal cultures naltrexone caused a time-dependent up-regulation of functional alpha7 nAChRs that was detected after removal of the drug. These results indicate that naltrexone could be used as a smoking cessation aid.