Differentiation between rat brain and mouse vas deferens δ opioid receptors

Linda K. Vaughn, William S. Wire, Peg Davis, Yasuyuki Shimohigashi, Geza Toth, Richard J. Knapp, Victor J. Hruby, Thomas F. Burks, Henry I. Yamamura

Research output: Contribution to journalArticle

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Abstract

Certain enkephalin analogues, including those which contain the conformationally restricted amino acid E-(2R,3S)-cyclopropylphenylalanine ((2R,3S)-{down triangle, open}EPhe), have been shown to have high affinity for brain δ opioid receptors but are much less active in mouse vas deferens bioassays. To investigate whether there are differences between δ opioid receptors in brain and mouse was deferens, the ability of a selective δ opioid compound. [D-Pen2,pCl-Phe4,D-Pen5]enkephalin (pCl-DPDPE), and [D-Ala2,(2R,3S)-{down triangle, open}EPhe4,Leu5]enkephalin methyl ester (CP-OMe), to inhibit [3H]pCl-DPDPE binding in both rat brain and mouse vas deferens were measured. pCl-DPDPE recognized brain and mouse vas deferences binding sites with equal affinity, however, CP-OMe showed 33 fold lower affinity in mouse vas deferens compared to brain. This suggests that mouse vas deferens δ opioid receptors may be distinct from brain δ opioid receptors.

Original languageEnglish (US)
Pages (from-to)99-101
Number of pages3
JournalEuropean Journal of Pharmacology
Volume177
Issue number1-2
DOIs
StatePublished - Feb 20 1990

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Keywords

  • Brain (rat)
  • Enkephalin analogues
  • Vas deferens (mouse)
  • δ Opioid receptors

ASJC Scopus subject areas

  • Pharmacology

Cite this

Vaughn, L. K., Wire, W. S., Davis, P., Shimohigashi, Y., Toth, G., Knapp, R. J., Hruby, V. J., Burks, T. F., & Yamamura, H. I. (1990). Differentiation between rat brain and mouse vas deferens δ opioid receptors. European Journal of Pharmacology, 177(1-2), 99-101. https://doi.org/10.1016/0014-2999(90)90556-L