A5071387984- Ion Channels and Receptors
- Ion channel regulation and function
- Nicotinic Acetylcholine Receptors Study
- Lipid Membrane Structure and Behavior
- Neuroscience and Neuropharmacology Research
- Pain Mechanisms and Treatments
- Herbal Medicine Research Studies
- Bioactive Compounds and Antitumor Agents
- Phytochemicals and Antioxidant Activities
- Receptor Mechanisms and Signaling
- Neurobiology and Insect Physiology Research
- Cardiac electrophysiology and arrhythmias
- Biochemical Analysis and Sensing Techniques
- Cancer Treatment and Pharmacology
- Cellular transport and secretion
- Photoreceptor and optogenetics research
- RNA and protein synthesis mechanisms
- Cholinesterase and Neurodegenerative Diseases
- Protein Structure and Dynamics
- Computational Drug Discovery Methods
- Neuropeptides and Animal Physiology
- Plant-based Medicinal Research
- Piperaceae Chemical and Biological Studies
- Endoplasmic Reticulum Stress and Disease
- X-ray Diffraction in Crystallography
Universitat de Miguel Hernández d'Elx
2016-2025
Instituto de Biologia Molecular e Celular
2008-2016
Universidad Marista
2016
Hospital General Universitario de Elche
2016
Instituto de Neurociencias
2011
Universitat de Barcelona
2007
Institute for Research in Biomedicine
2007
Centro Nacional de Biotecnología
2002-2003
Hospital Universitario Virgen del Rocío
2002
University of Alicante
1989-1997
Abstract TRPA1 and TRPM8 are transient receptor potential channels expressed in trigeminal neurons that related to pathophysiology migraine models. Here we use a mouse model of nitroglycerine-induced chronic displays sexually dimorphic phenotype, characterized by mechanical hypersensitivity develops males females, is persistent up day 20 female mice, but disappears 18 male mice. required for development whereas contributes the faster recovery from males. TRPM8-mediated antinociception...
Transient receptor potential vanilloid subtype 1 (TRPV1) is an ionotropic activated by temperature and chemical stimuli. The C-terminal region that adjacent to the channel gate, recognized as TRP domain, a molecular determinant of assembly. However, role this intracellular domain in function remains elusive. Here, we show replacement TRPV1 with cognate TRPV channels (TRPV2–TRPV6) did not affect assembly trafficking cell surface, although those receptors containing distantly related TRPV5...
Transient receptor potential vanilloid subtype I (TRPV1) is an ion channel gated by physical and chemical stimuli that belongs to the TRPV protein family. receptors contain a highly conserved, 6-mer segment near gate, known as TRP box, whose function remains unknown. Here, we performed alanine scanning mutagenesis of box TRPV1 (IWKLQR) found mutation this motif affected gating raising free energy activation. Functional characterization mutants showed substitution I696, W697, R701 severely...
Here, we report for the first time a series of compounds potentially useful management oxaliplatin-induced neuropathy (OINP) able to modulate human Carbonic Anhydrases (hCAs) as well Transient Receptor Potential Vanilloid 1 (TRPV1). All showed effective in vitro inhibition activity toward main hCAs involved such pathology, whereas selected items reported moderate agonism TRPV1. X-ray crystallographic experiments assessed binding modes two enantiomers (R)-37a and (S)-37b within hCA II cleft....
Aim: To expand the understanding of structure-activity relationship within a family amino acid-derived β-lactam TRPM8 (transient receptor potential melastatin channel, subtype 8) antagonists, this work investigated both configuration-dependence potency and selectivity, explored strategies for increasing total polar surface area (TPSA). Methods: Diastereoisomeric compounds derived from H-Phe-OtBu, analogues incorporating differently substituted benzoyl groups, were synthesized by...
Transient receptor potential cation channel subfamily M member 8 (TRPM8) is a nonselective thermosensory expressed in peripheral nociceptor terminals where it transduces cold temperatures and cooling agents such as menthol. TRPM8 dysfunction has been involved disabling sensory symptoms, allodynia. In addition, its widespread expression signaled this pivotal therapeutic target for variety of diseases, from neuropathies to cancer. Thus, the design validation antagonists an important endeavor...
Background: Genetic variations in the Trpm8 gene that encodes cold receptor TRPM8 have been linked to protection against polygenic migraine, a disabling condition primarily affecting women. Noteworthy, has recently found brain areas related emotional processing, suggesting an unrecognized role migraine comorbidities. Here, we use mouse behavioural models investigate of migraine-related phenotypes. Subsequently, test efficacy rapamycin, clinically relevant agonist, these traits and human...
Different patterns of channel activity have been detected by patch clamping excised membrane patches from reconstituted giant liposomes containing purified KcsA, a potassium prokaryotes. The more frequent pattern has characteristic low opening probability and exhibits many other features reported for KcsA into planar lipid bilayers, including moderate voltage dependence, blockade Na(+), strict dependence on acidic pH opening. predominant gating event in this corresponds to the positive...
Pharmacological modulation of the transient receptor potential melastatin type 8 (TRPM8) is currently under investigation as a new approach for treatment pain and other diseases. In this study, series N-substituted tryptamines was prepared to explore structural requirements determining TRPM8 modulation. Using fluorescence-based screening assay, we identified two compounds acting an activator (2-(1H-indol-3-yl)-N-(4-phenoxybenzyl)ethanamine, 21) or inhibitor...
TRPM8 has been implicated in nociception and pain is currently regarded as an attractive target for the pharmacological treatment of neuropathic syndromes. A series analogues N, N'-dibenzyl tryptamine 1, a potent antagonist, was prepared screened using fluorescence-based vitro assay based on menthol-evoked calcium influx stably transfected HEK293 cells. The tryptophan derivative 14 identified (IC50 0.2 ± nM) selective antagonist. In vivo, showed significant coverage both icilin-induced WDS...
Paclitaxel produces a chemotherapy-induced peripheral neuropathy that persists in 50-60% of cancer patients upon treatment. Evidence from animal models suggests an axonopathy A- and C-type fibres affects their excitability. However, direct effects paclitaxel on sensory neuron excitability sexual dimorphism remain poorly understood.We used long-lasting (10 days vitro) primary culture rat dorsal root ganglion (DRG) neurons to investigate the time course effect electrical activity IB4(-) IB4(+)...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTA Role for Cholesterol as a Structural Effector of the Nicotinic Acetylcholine ReceptorGregorio Fernandez-Ballester, Jose Castresana, Asia M. Fernandez, Jose-Luis R. Arrondo, A. Ferragut, and Gonzalez-RosCite this: Biochemistry 1994, 33, 13, 4065–4071Publication Date (Print):April 5, 1994Publication History Published online1 May 2002Published inissue 5 April...
Despite being an old molecule, capsaicin is still a hot topic in the scientific community, and development of new capsaicinoids promising pharmacological approach management skin disorders related to inflammation pruritus. Here we report synthesis evaluation soft drugs that undergo deactivation by hydrolyzing activity esterases. The implanting ester group lipophilic moiety Passerini multicomponent reaction affords both agonists antagonists retain transient receptor potential vanilloid 1...