TY - JOUR
T1 - Differentiation between rat brain and mouse vas deferens δ opioid receptors
AU - Vaughn, Linda K.
AU - Wire, William S.
AU - Davis, Peg
AU - Shimohigashi, Yasuyuki
AU - Toth, Geza
AU - Knapp, Richard J.
AU - Hruby, Victor J.
AU - Burks, Thomas F.
AU - Yamamura, Henry I.
PY - 1990/2/20
Y1 - 1990/2/20
N2 - 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.
AB - 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.
KW - Brain (rat)
KW - Enkephalin analogues
KW - Vas deferens (mouse)
KW - δ Opioid receptors
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U2 - 10.1016/0014-2999(90)90556-L
DO - 10.1016/0014-2999(90)90556-L
M3 - Article
C2 - 2160370
AN - SCOPUS:0025098127
SN - 0014-2999
VL - 177
SP - 99
EP - 101
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
IS - 1-2
ER -