Abstract：
:Certain enkephalin analogues, including those which contain the conformationally restricted amino acid E-(2R,3S)-cyclopropylphenylalanine [2R,3S)-delta E Phe), have been shown to have high affinity for brain delta opioid receptors but are much less active in mouse vas deferens bioassays. To investigate whether there are differences between delta opioid receptors in brain and mouse was deferens, the ability of a selective delta opioid compound, [D-Pen2,pCl-Phe4,D-Pen5]enkephalin (pCl-DPDPE), and [D-Ala2,(2R,3S)-delta E Phe4,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 deferens 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 delta opioid receptors may be distinct from brain delta opioid receptors.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Vaughn LK,Wire WS,Davis P,Shimohigashi Y,Toth G,Knapp RJ,Hruby VJ,Burks TF,Yamamura HIdoi
10.1016/0014-2999(90)90556-lsubject
Has Abstractpub_date
1990-02-20 00:00:00pages
99-101issue
1-2eissn
0014-2999issn
1879-0712pii
0014-2999(90)90556-Ljournal_volume
177pub_type
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