Abstract
The interactions of a proposed, selective delta receptor antagonist (ICI 174, 864) and selective agonists at mu and delta receptors, [D-Ala2, NMePhe4, Gly-ol]-enkephalin (DAGO) and [D-Pen2, D-Pen5]-enkephalin (DPDPE), respectively, have been studied using the electrically-stimulated mouse isolated vas deferens (MVD) and the guinea-pig isolated ileum (GPI). Incubation of increasing concentrations of ICI 174, 864 (10, 30, 100 and 300 nM) produced a dose-related and parallel rightward displacement of the DPDPE dose-response curve in the MVD. In contrast, ICI 174, 864 (300-3000 nM) failed to affect the DAGO dose-response curve in the same tissue. Analysis of the DPDPE-ICI 174, 864 interaction in the MVD using the pA2 method revealed a Schild plot slope of -0.68 suggesting the involvement of more than one population of receptors. ICI 174, 864 (300 nM) failed to antagonize DPDPE in the GPI at doses up to 30 uM. These results suggest that (a) ICI 174, 864 acts as a selective delta antagonist in the MVD; (b) DPDPE interacts with mu receptors in the MVD but only at very high concentrations, and (c) delta receptors appear not to be of functional importance in the GPI.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 383-386 |
| Number of pages | 4 |
| Journal | Neuropeptides |
| Volume | 5 |
| Issue number | 4-6 |
| DOIs | |
| State | Published - 1985 |
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ASJC Scopus subject areas
- Biochemistry
- Endocrinology
- Endocrinology, Diabetes and Metabolism
- Clinical Neurology
- Neuroscience(all)
- Cellular and Molecular Neuroscience
Cite this
Studies in vitro with ICI 174, 864, [D-Pen2, D-Pen5]-enkephalin (DPDPE) and [D-Ala2, NMePhe4, Gly-ol]-enkephalin (DAGO). / Hirning, Lane D.; Mosberg, Henry I.; Hurst, Robin; Hruby, Victor J; Burks, Thomas F.; Porreca, Frank.
In: Neuropeptides, Vol. 5, No. 4-6, 1985, p. 383-386.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Studies in vitro with ICI 174, 864, [D-Pen2, D-Pen5]-enkephalin (DPDPE) and [D-Ala2, NMePhe4, Gly-ol]-enkephalin (DAGO)
AU - Hirning, Lane D.
AU - Mosberg, Henry I.
AU - Hurst, Robin
AU - Hruby, Victor J
AU - Burks, Thomas F.
AU - Porreca, Frank
PY - 1985
Y1 - 1985
N2 - The interactions of a proposed, selective delta receptor antagonist (ICI 174, 864) and selective agonists at mu and delta receptors, [D-Ala2, NMePhe4, Gly-ol]-enkephalin (DAGO) and [D-Pen2, D-Pen5]-enkephalin (DPDPE), respectively, have been studied using the electrically-stimulated mouse isolated vas deferens (MVD) and the guinea-pig isolated ileum (GPI). Incubation of increasing concentrations of ICI 174, 864 (10, 30, 100 and 300 nM) produced a dose-related and parallel rightward displacement of the DPDPE dose-response curve in the MVD. In contrast, ICI 174, 864 (300-3000 nM) failed to affect the DAGO dose-response curve in the same tissue. Analysis of the DPDPE-ICI 174, 864 interaction in the MVD using the pA2 method revealed a Schild plot slope of -0.68 suggesting the involvement of more than one population of receptors. ICI 174, 864 (300 nM) failed to antagonize DPDPE in the GPI at doses up to 30 uM. These results suggest that (a) ICI 174, 864 acts as a selective delta antagonist in the MVD; (b) DPDPE interacts with mu receptors in the MVD but only at very high concentrations, and (c) delta receptors appear not to be of functional importance in the GPI.
AB - The interactions of a proposed, selective delta receptor antagonist (ICI 174, 864) and selective agonists at mu and delta receptors, [D-Ala2, NMePhe4, Gly-ol]-enkephalin (DAGO) and [D-Pen2, D-Pen5]-enkephalin (DPDPE), respectively, have been studied using the electrically-stimulated mouse isolated vas deferens (MVD) and the guinea-pig isolated ileum (GPI). Incubation of increasing concentrations of ICI 174, 864 (10, 30, 100 and 300 nM) produced a dose-related and parallel rightward displacement of the DPDPE dose-response curve in the MVD. In contrast, ICI 174, 864 (300-3000 nM) failed to affect the DAGO dose-response curve in the same tissue. Analysis of the DPDPE-ICI 174, 864 interaction in the MVD using the pA2 method revealed a Schild plot slope of -0.68 suggesting the involvement of more than one population of receptors. ICI 174, 864 (300 nM) failed to antagonize DPDPE in the GPI at doses up to 30 uM. These results suggest that (a) ICI 174, 864 acts as a selective delta antagonist in the MVD; (b) DPDPE interacts with mu receptors in the MVD but only at very high concentrations, and (c) delta receptors appear not to be of functional importance in the GPI.
UR - http://www.scopus.com/inward/record.url?scp=0021988646&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0021988646&partnerID=8YFLogxK
U2 - 10.1016/0143-4179(85)90034-4
DO - 10.1016/0143-4179(85)90034-4
M3 - Article
C2 - 2987739
AN - SCOPUS:0021988646
VL - 5
SP - 383
EP - 386
JO - Neuropeptides
JF - Neuropeptides
SN - 0143-4179
IS - 4-6
ER -