Differentiation between rat brain and mouse vas deferens delta opioid receptors.
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.
Vaughn
L K
LK
Department of Pharmacology, University of Arizona, Tucson.
Wire
W S
WS
Davis
P
P
Shimohigashi
Y
Y
Toth
G
G
Knapp
R J
RJ
Hruby
V J
VJ
Burks
T F
TF
Yamamura
H I
HI
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D004743:Enkephalin, Leucine / Q000031:analogs & derivatives / Q000494:pharmacology; D016308:Enkephalin, Leucine-2-Alanine / Q000031:analogs & derivatives*; D004745:Enkephalins / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D009130:Muscle, Smooth / Q000187:drug effects / Q000378:metabolism*; D009928:Organ Specificity; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000378:metabolism*; D017465:Receptors, Opioid, delta; D013045:Species Specificity; D014649:Vas Deferens / Q000187:drug effects / Q000378:metabolism
D004745:Enkephalins; D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; C064220:enkephalin-Leu methyl ester, Ala(2)-cyclopropyl-Phe(4)-; C064219:enkephalin, Pen(2,5)-4-chloro-Phe(4)-; D004743:Enkephalin, Leucine; D016308:Enkephalin, Leucine-2-Alanine