title: Expression and localization of delta-, kappa-, and mu-opioid receptors in human spermatozoa and implications for sperm motility.
abstract: BACKGROUND
  Endogenous opioid peptides signal through delta-, kappa-, and mu-opioid receptors. Some of these peptides such as endorphins and enkephalins are present in the male reproductive tract, but the presence of the corresponding receptors in human sperm cells has not yet been reported.
  
  
  OBJECTIVE
  Our objective was to study the expression and localization of delta-, kappa-, and mu-opioid receptors on human spermatozoa and the implication in sperm motility.
  
  
  METHODS
  The expression of receptors was studied by RT-PCR, Western blot, and immunofluorescence techniques. We evaluated the effects of activation of each opioid receptor by specific agonist and antagonist.
  
  
  RESULTS
  Human spermatozoa express delta-, kappa-, and mu-opioid receptors. These receptors were located in different parts of the head, in the middle region, and in the tail of the sperm. Progressive motility of spermatozoa, an important parameter to evaluate male fertility, was found to be significantly reduced after incubation with the mu-receptor agonist morphine, whereas this effect was antagonized in the presence of the corresponding antagonist naloxone. The delta-receptor antagonist naltrindole significantly reduced progressive motility immediately after its addition. However, the delta-receptor agonist DPDPE had no significant effect. Finally, neither the kappa-receptor agonist U50488 nor its antagonist nor-binaltorphimine significantly affected the progressive motility of human spermatozoa.
  
  
  CONCLUSIONS
  We report for first time the presence of functional delta-, kappa-, and mu-opioid receptors in human sperm membranes. These findings are indicative of a role for the opioid system in the regulation of sperm physiology.
authors.affiliation: Department of Physiology, Faculty of Medicine and Dentistry, University of the Basque Country, PO Box 699, Bilbao, 48080 Bizkaia, Spain. e.agirregoitia@ehu.es
authors.forename: Ekaitz
authors.initials: E
authors.lastname: Agirregoitia
authors.forename: Asier
authors.initials: A
authors.lastname: Valdivia
authors.forename: Arkaitz
authors.initials: A
authors.lastname: Carracedo
authors.forename: Luis
authors.initials: L
authors.lastname: Casis
authors.forename: Javier
authors.initials: J
authors.lastname: Gil
authors.forename: Nerea
authors.initials: N
authors.lastname: Subiran
authors.forename: Carmen
authors.initials: C
authors.lastname: Ochoa
authors.forename: Jon
authors.initials: J
authors.lastname: Irazusta
mesh_terms: D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer / Q000494:pharmacology; D000328:Adult; D000701:Analgesics, Opioid / Q000494:pharmacology; D006801:Humans; D008297:Male; D009020:Morphine / Q000494:pharmacology; D009270:Naloxone / Q000494:pharmacology; D009271:Naltrexone / Q000031:analogs & derivatives / Q000494:pharmacology; D009292:Narcotic Antagonists / Q000494:pharmacology; D017465:Receptors, Opioid, delta / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism* / Q000502:physiology; D017473:Receptors, Opioid, kappa / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism* / Q000502:physiology; D017450:Receptors, Opioid, mu / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism* / Q000502:physiology; D013081:Sperm Motility / Q000187:drug effects / Q000502:physiology*; D013094:Spermatozoa / Q000166:cytology / Q000378:metabolism*; D014018:Tissue Distribution
chemical_list: D000701:Analgesics, Opioid; D009292:Narcotic Antagonists; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D009270:Naloxone; C051844:norbinaltorphimine; D009271:Naltrexone; D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D009020:Morphine