Dynorphin A: Inhibitory effect on other opiate ligand bindings in the mouse brain

J. Garźon; P. Sánchez-Blázquez; J. Gerhart; H. H. Loh; N. M. Lee

doi:10.1016/0006-2952(84)90633-6

Dynorphin A: Inhibitory effect on other opiate ligand bindings in the mouse brain

J. Garźon, P. Sánchez-Blázquez, J. Gerhart, H. H. Loh, N. M. Lee

Pharmacology

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Abstract

The opioid peptide dynorphin A antagonizes morphine-induced analgesia in vivo and inhibits opiate binding in vitro, although most of it is rapidly degraded under both conditions. The inhibitory effect was present even in tissue treated in vivo with dynorphin A and assayed in vitro without it. Shorter fragments of this peptide lacked these effects, indicating that the apparent potency did not result from a metabolite. Na⁺ ion specifically reversed both agonist and antagonist binding from in vitro inhibition by dynorphin A. These results are discussed in terms of current opioid receptor theories.

Original language	English (US)
Pages (from-to)	2609-2614
Number of pages	6
Journal	Biochemical Pharmacology
Volume	33
Issue number	16
DOIs	https://doi.org/10.1016/0006-2952(84)90633-6
State	Published - Aug 15 1984

Bibliographical note

Funding Information:
Acknowledgements---Supported by NIDA 02643 and 2K02-DA-70554 (HHL) and 2-K02-DA-00020 (NML). PSB is a recipient of a Fulbright-MEC Fellowship. JG is a recipient of a NIH Fellowship 705-TW-03080. We thank Professor J. Del Rio for the facilities given in the preparation of this manuscript.

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title = "Dynorphin A: Inhibitory effect on other opiate ligand bindings in the mouse brain",

abstract = "The opioid peptide dynorphin A antagonizes morphine-induced analgesia in vivo and inhibits opiate binding in vitro, although most of it is rapidly degraded under both conditions. The inhibitory effect was present even in tissue treated in vivo with dynorphin A and assayed in vitro without it. Shorter fragments of this peptide lacked these effects, indicating that the apparent potency did not result from a metabolite. Na+ ion specifically reversed both agonist and antagonist binding from in vitro inhibition by dynorphin A. These results are discussed in terms of current opioid receptor theories.",

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AU - Garźon, J.

AU - Sánchez-Blázquez, P.

AU - Gerhart, J.

AU - Loh, H. H.

AU - Lee, N. M.

N1 - Funding Information: Acknowledgements---Supported by NIDA 02643 and 2K02-DA-70554 (HHL) and 2-K02-DA-00020 (NML). PSB is a recipient of a Fulbright-MEC Fellowship. JG is a recipient of a NIH Fellowship 705-TW-03080. We thank Professor J. Del Rio for the facilities given in the preparation of this manuscript.

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Y1 - 1984/8/15

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AB - The opioid peptide dynorphin A antagonizes morphine-induced analgesia in vivo and inhibits opiate binding in vitro, although most of it is rapidly degraded under both conditions. The inhibitory effect was present even in tissue treated in vivo with dynorphin A and assayed in vitro without it. Shorter fragments of this peptide lacked these effects, indicating that the apparent potency did not result from a metabolite. Na+ ion specifically reversed both agonist and antagonist binding from in vitro inhibition by dynorphin A. These results are discussed in terms of current opioid receptor theories.

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Dynorphin A: Inhibitory effect on other opiate ligand bindings in the mouse brain

Abstract

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