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 language | English (US) |
|---|---|
| Pages (from-to) | 99-101 |
| Number of pages | 3 |
| Journal | European Journal of Pharmacology |
| Volume | 177 |
| Issue number | 1-2 |
| DOIs | |
| State | Published - Feb 20 1990 |
| Externally published | Yes |
Keywords
- Brain (rat)
- Enkephalin analogues
- Vas deferens (mouse)
- δ Opioid receptors
ASJC Scopus subject areas
- Pharmacology
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