Abstract
P2X3 purinoreceptors expressed in mammalian sensory neurons play a key role in several processes, including pain perception. From the venom of the Central Asian spider Geolycosa sp., we have isolated a novel peptide, named purotoxin-1 (PT1), which is to our knowledge the first natural molecule exerting powerful and selective inhibitory action on P2X3 receptors. PT1 dramatically slows down the removal of desensitization of these receptors. The peptide demonstrates potent antinociceptive properties in animal models of inflammatory pain.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenosine Triphosphate / pharmacology
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Animals
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Animals, Newborn
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Cells, Cultured
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Chondrus
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Cytidine Triphosphate / pharmacology
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Disease Models, Animal
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Dose-Response Relationship, Drug
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Ganglia, Spinal / cytology
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Humans
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Magnetic Resonance Spectroscopy / methods
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Membrane Potentials / drug effects
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Membrane Potentials / genetics
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Neurogenic Inflammation / chemically induced
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Neurogenic Inflammation / complications
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Pain / drug therapy*
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Pain / etiology
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Pain / metabolism*
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Patch-Clamp Techniques / methods
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Peptides / therapeutic use*
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Purinergic P2 Receptor Antagonists
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Rats
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Rats, Wistar
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Receptors, Purinergic P2 / genetics
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Receptors, Purinergic P2 / metabolism*
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Receptors, Purinergic P2X3
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Sensory Receptor Cells / drug effects
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Sensory Receptor Cells / physiology
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Spider Venoms / chemistry*
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Transfection / methods
Substances
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P2RX3 protein, human
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Peptides
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Purinergic P2 Receptor Antagonists
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Receptors, Purinergic P2
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Receptors, Purinergic P2X3
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Spider Venoms
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purotoxin-1, Geolycosa
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Cytidine Triphosphate
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Adenosine Triphosphate