TY - JOUR
T1 - Interaction of [d-Pen2, d-Pen5]enkephalin and [d-Ala2, Glu4]deltorphin with δ-opioid receptor subtypes in vivo
AU - Vanderah, T.
AU - Takemori, A. E.
AU - Sultana, M.
AU - Portoghese, P. S.
AU - Mosberg, H. I.
AU - Hruby, V. J.
AU - Haaseth, R. C.
AU - Matsunaga, T. O.
AU - Porreca, F.
PY - 1994/2/3
Y1 - 1994/2/3
N2 - The interaction of [d-Pen2, d-Pen5]enkephalin (DPDPE) and [d-Ala2, Glu4]deltorphin with δ-opioid receptor subtypes was investigated. Pretreatment of mice with the δ1-opioid receptor antagonists, [d-Ala2, Leu5, Cys6]enkephalin (DALCE), produced a virtually complete antagonism of the antinociceptive actions of DPDPE, but had no effect on those of [d-Ala2, Glu4]deltorphin. In DALCE pretreated mice (i.e., δ1-opioid receptors blocked), DPDPE was able to significantly antagonize the antinociceptive effects of [d-Ala2, Glu4]deltorphin. Pretreatment of mice with the δ2-opioid receptor antagonist, na naltrindole-5′-isothiocynate (5′-NTII) produced a virtually complete antagonism of the antinociceptive effects of [d-Ala2, Glu4]deltorphin, but had no effect on the antinociception produced by DPDPE. In 5′-NTII pretreated mice (i.e., δ2-opioid receptors blocked), [d-Ala2, Glu4]deltorphin had no effect on the antinociception produced by DPDPE. These data suggest that [d-Ala2, Glu4]deltorphin is highly selective for the δ2-opioid receptor in vivo, and that neither agonist nor antagonist actions can be demonstrated at δ1-opioid receptors for this peptide. In contrast, under appropriate conditions, DPDPE can be shown to interact with both δ1- and δ2-opioid receptor subtypes; DPDPE may have limited efficacy (i.e., is a partial agonist) at the δ2-opioid receptor.
AB - The interaction of [d-Pen2, d-Pen5]enkephalin (DPDPE) and [d-Ala2, Glu4]deltorphin with δ-opioid receptor subtypes was investigated. Pretreatment of mice with the δ1-opioid receptor antagonists, [d-Ala2, Leu5, Cys6]enkephalin (DALCE), produced a virtually complete antagonism of the antinociceptive actions of DPDPE, but had no effect on those of [d-Ala2, Glu4]deltorphin. In DALCE pretreated mice (i.e., δ1-opioid receptors blocked), DPDPE was able to significantly antagonize the antinociceptive effects of [d-Ala2, Glu4]deltorphin. Pretreatment of mice with the δ2-opioid receptor antagonist, na naltrindole-5′-isothiocynate (5′-NTII) produced a virtually complete antagonism of the antinociceptive effects of [d-Ala2, Glu4]deltorphin, but had no effect on the antinociception produced by DPDPE. In 5′-NTII pretreated mice (i.e., δ2-opioid receptors blocked), [d-Ala2, Glu4]deltorphin had no effect on the antinociception produced by DPDPE. These data suggest that [d-Ala2, Glu4]deltorphin is highly selective for the δ2-opioid receptor in vivo, and that neither agonist nor antagonist actions can be demonstrated at δ1-opioid receptors for this peptide. In contrast, under appropriate conditions, DPDPE can be shown to interact with both δ1- and δ2-opioid receptor subtypes; DPDPE may have limited efficacy (i.e., is a partial agonist) at the δ2-opioid receptor.
KW - (Mouse)
KW - Antinociception
KW - DPDPE ([d-Pen, d-Pen]enkephalin)
KW - Opioid
KW - [d-Ala, Glu]Deltorphin
KW - δ-Opioid receptor subtype
UR - http://www.scopus.com/inward/record.url?scp=0028180106&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0028180106&partnerID=8YFLogxK
U2 - 10.1016/0014-2999(94)90588-6
DO - 10.1016/0014-2999(94)90588-6
M3 - Article
C2 - 8157053
AN - SCOPUS:0028180106
SN - 0014-2999
VL - 252
SP - 133
EP - 137
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
IS - 2
ER -
