Inhibition of the antisecretory effects of [D-Ala2,D-Leu5]enkephalin in the guinea-pig ileum by a selective δ opioid antagonist

Rakesh Vinayek; David R. Brown; Richard J. Miller

doi:10.1016/0014-2999(83)90455-7

Inhibition of the antisecretory effects of [D-Ala²,D-Leu⁵]enkephalin in the guinea-pig ileum by a selective δ opioid antagonist

Rakesh Vinayek, David R. Brown, Richard J. Miller

Veterinary and Biomedical Sciences

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

Abstract

The novel opioid antagonist [dially-Tyr¹,(CH₂)S-Phe⁴,Leu⁵]enkephalin (M154,129) was examined for its ability to block the antisecretory effects of [D-Ala²,D-Leu⁵]enkephalin (DADLE) in isolated mucosal segments of the guinea-pig ileum, actions mediated predominantly through the δ opiate receptor. DADLE reduced transepithelial potential difference and short-circuit current (ED₅₀ 18 nM); these effects were competitively antagonized by M154,129 with a K_e value of 746 nM. These results are consistent with others demonstrating that M154,129 is a relatively selective although not highly potent blocker of δ opiate receptors.

Original language	English (US)
Pages (from-to)	159-161
Number of pages	3
Journal	European Journal of Pharmacology
Volume	94
Issue number	1-2
DOIs	https://doi.org/10.1016/0014-2999(83)90455-7
State	Published - Oct 14 1983

Bibliographical note

Funding Information:
This work is supported in part by U.S.P.H.S. grant DA-02121 and an Alfred P. Sloan Fellowship to R.J.M. and by N.I.M.H. Postdoctoral Training Fellowship MH 14274 to D.R.B. We thank Dr. Michael Turnbull (ICI Pharmaceuticals) for the gift of M154,129 and Dr. David C. Draper (Department of Statistics, University of Chicago) for his assistance in the data analysis.

Keywords

(CH)S-Phe
D-Leu]enkephalin
Leu]enkephalin
[D-Ala
[Dially-Tyr
δ Opiate receptor Intestinal electrolyte transport

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This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/0014-2999(83)90455-7

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@article{166d782de69d4d059a396919add8fa6e,

title = "Inhibition of the antisecretory effects of [D-Ala2,D-Leu5]enkephalin in the guinea-pig ileum by a selective δ opioid antagonist",

abstract = "The novel opioid antagonist [dially-Tyr1,(CH2)S-Phe4,Leu5]enkephalin (M154,129) was examined for its ability to block the antisecretory effects of [D-Ala2,D-Leu5]enkephalin (DADLE) in isolated mucosal segments of the guinea-pig ileum, actions mediated predominantly through the δ opiate receptor. DADLE reduced transepithelial potential difference and short-circuit current (ED50 18 nM); these effects were competitively antagonized by M154,129 with a Ke value of 746 nM. These results are consistent with others demonstrating that M154,129 is a relatively selective although not highly potent blocker of δ opiate receptors.",

keywords = "(CH)S-Phe, D-Leu]enkephalin, Leu]enkephalin, [D-Ala, [Dially-Tyr, δ Opiate receptor Intestinal electrolyte transport",

author = "Rakesh Vinayek and Brown, {David R.} and Miller, {Richard J.}",

note = "Funding Information: This work is supported in part by U.S.P.H.S. grant DA-02121 and an Alfred P. Sloan Fellowship to R.J.M. and by N.I.M.H. Postdoctoral Training Fellowship MH 14274 to D.R.B. We thank Dr. Michael Turnbull (ICI Pharmaceuticals) for the gift of M154,129 and Dr. David C. Draper (Department of Statistics, University of Chicago) for his assistance in the data analysis.",

year = "1983",

month = oct,

day = "14",

doi = "10.1016/0014-2999(83)90455-7",

language = "English (US)",

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pages = "159--161",

journal = "European Journal of Pharmacology",

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T1 - Inhibition of the antisecretory effects of [D-Ala2,D-Leu5]enkephalin in the guinea-pig ileum by a selective δ opioid antagonist

AU - Vinayek, Rakesh

AU - Brown, David R.

AU - Miller, Richard J.

N1 - Funding Information: This work is supported in part by U.S.P.H.S. grant DA-02121 and an Alfred P. Sloan Fellowship to R.J.M. and by N.I.M.H. Postdoctoral Training Fellowship MH 14274 to D.R.B. We thank Dr. Michael Turnbull (ICI Pharmaceuticals) for the gift of M154,129 and Dr. David C. Draper (Department of Statistics, University of Chicago) for his assistance in the data analysis.

PY - 1983/10/14

Y1 - 1983/10/14

N2 - The novel opioid antagonist [dially-Tyr1,(CH2)S-Phe4,Leu5]enkephalin (M154,129) was examined for its ability to block the antisecretory effects of [D-Ala2,D-Leu5]enkephalin (DADLE) in isolated mucosal segments of the guinea-pig ileum, actions mediated predominantly through the δ opiate receptor. DADLE reduced transepithelial potential difference and short-circuit current (ED50 18 nM); these effects were competitively antagonized by M154,129 with a Ke value of 746 nM. These results are consistent with others demonstrating that M154,129 is a relatively selective although not highly potent blocker of δ opiate receptors.

AB - The novel opioid antagonist [dially-Tyr1,(CH2)S-Phe4,Leu5]enkephalin (M154,129) was examined for its ability to block the antisecretory effects of [D-Ala2,D-Leu5]enkephalin (DADLE) in isolated mucosal segments of the guinea-pig ileum, actions mediated predominantly through the δ opiate receptor. DADLE reduced transepithelial potential difference and short-circuit current (ED50 18 nM); these effects were competitively antagonized by M154,129 with a Ke value of 746 nM. These results are consistent with others demonstrating that M154,129 is a relatively selective although not highly potent blocker of δ opiate receptors.

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KW - Leu]enkephalin

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KW - [Dially-Tyr

KW - δ Opiate receptor Intestinal electrolyte transport

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