A tarantula peptide against pain via ASIC1a channels and opioid mechanisms.
Psalmotoxin 1, a peptide extracted from the South American tarantula Psalmopoeus cambridgei, has very potent analgesic properties against thermal, mechanical, chemical, inflammatory and neuropathic pain in rodents. It exerts its action by blocking acid-sensing ion channel 1a, and this blockade results in an activation of the endogenous enkephalin pathway. The analgesic properties of the peptide are suppressed by antagonists of the mu and delta-opioid receptors and are lost in Penk1-/- mice.
Mazzuca
Michel
M
Institut de Pharmacologie Moléculaire et Cellulaire, Centre National de la Recherche Scientifique (CNRS), Institut Paul Hamel, Université de Nice-Sophia-Antipolis, 660 Route des Lucioles 06560 Valbonne, France.
Heurteaux
Catherine
C
Alloui
Abdelkrim
A
Diochot
Sylvie
S
Baron
Anne
A
Voilley
Nicolas
N
Blondeau
Nicolas
N
Escoubas
Pierre
P
Gélot
Agnès
A
Cupo
Anny
A
Zimmer
Andreas
A
Zimmer
Anne M
AM
Eschalier
Alain
A
Lazdunski
Michel
M
D062565:Acid Sensing Ion Channels; D000700:Analgesics / Q000627:therapeutic use*; D000818:Animals; D019540:Area Under Curve; D001522:Behavior, Animal; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D004745:Enkephalins / Q000172:deficiency / Q000502:physiology*; D008565:Membrane Proteins / Q000172:deficiency / Q000502:physiology*; D051379:Mice; D018345:Mice, Knockout; D009020:Morphine / Q000008:administration & dosage; D009270:Naloxone / Q000008:administration & dosage; D009271:Naltrexone / Q000008:administration & dosage; D009292:Narcotic Antagonists / Q000008:administration & dosage; D009419:Nerve Tissue Proteins / Q000172:deficiency / Q000502:physiology*; D009474:Neurons / Q000187:drug effects / Q000502:physiology; D010146:Pain / Q000188:drug therapy*; D010147:Pain Measurement / Q000379:methods; D010455:Peptides; D011498:Protein Precursors / Q000172:deficiency; D011930:Reaction Time / Q000187:drug effects; D015222:Sodium Channels / Q000172:deficiency / Q000502:physiology*; D013111:Spider Venoms / Q000627:therapeutic use*; D013116:Spinal Cord / Q000473:pathology; D013997:Time Factors
C568267:ASIC1 protein, mouse; D062565:Acid Sensing Ion Channels; D000700:Analgesics; D004745:Enkephalins; D008565:Membrane Proteins; D009292:Narcotic Antagonists; D009419:Nerve Tissue Proteins; C413209:PcTX1 protein, Psalmopoeus cambridgei; D010455:Peptides; D011498:Protein Precursors; D015222:Sodium Channels; D013111:Spider Venoms; D009270:Naloxone; D009271:Naltrexone; D009020:Morphine; C033660:preproenkephalin