Cited by 883Neuropeptides and Animal PhysiologyNeuroendocrine regulation and behaviorChemical Synthesis and Analysis

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Dynorphin-(1-13), an extraordinarily potent opioid peptide.

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Goldstein, A, Tachibana, S, Lowney, L I, Hunkapiller, M, Hood, L·1979·Proceedings of the National Academy of Sciences

DOI 10.1073/pnas.76.12.6666PMC PMC411929

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Abstract

We describe the opioid properties of a tridecapeptide, the sequence of which corresponds to the NH2-terminal sequence of dynorphin, a novel porcine pituitary endorphin. It contains [Leu]enkephalin. In the guinea pig ileum longitudinal muscle preparation it is about 700 times more potent than [Leu]enkephalin. Its effects in this tissue are blocked completely by naloxone, but the apparent affinity of naloxone is 1/13th that for blockade of [Leu]enkephalin or normorphine. In the mouse vas deferens, this peptide is 3 times more potent than [Leu]enkephalin. Well-washed rat brain membranes degrade the peptide rapidly, suggesting the presence of a membrane-bound degradative enzyme. The peptide displays considerable immunoreactivity in assays with antisera that have been used for the immunohistochemical localization of [Leu]enkephalin. The remarkable enhancement of the potency of [Leu]enkephalin by the COOH-terminal extension -Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys-OH suggests new interpretations concerning the structure of opiate receptors and the function of the enkephalin pentapeptides.

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Biology and Chemistry of the Dynorphin Peptides**Research described here that was carried out in my laboratory was supported by grants DA-1199 from the National Institute on Drug Abuse, NS-18098 from the National Institutes of Health, and BNS-81-07237 from the National Science Foundation.
D, A. G. M. (1984) · Elsevier eBooks · doi:10.1016/b978-0-12-304206-4.50014-9 · Cited by 38
Opioid Peptides in Human Plasma: Evidence for Multiple Forms*
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Neuropeptides. Their Distribution and Function in the Brain
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Endomorphins and related opioid peptides
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Electrospray ionization mass spectrometric and liquid chromatographic–mass spectrometric studies on the metabolism of synthetic dynorphin A peptides in brain tissue in vitro and in vivo
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Selective involvement of kappa opioid and phencyclidine receptors in the analgesic and motor effects of dynorphin-A-(1–13)-Tyr-Leu-Phe-Asn-Gly-Pro
Shukla, V. K., Bansinath, M., Dumont, M., & Lemaire, S. (1992) · Brain Research · doi:10.1016/0006-8993(92)90994-k · Cited by 36
Enkephalins in the Rat Pituitary Gland: Immunohistochemical and Biochemical Observations
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Electroacupuncture Effects in a Rat Model of Complete Freund’s Adjuvant-Induced Inflammatory Pain: Antinociceptive Effects Enhanced and Tolerance Development Accelerated
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“This result suggests that opioid systems, especially dynorphin and j-receptor system, might be involved in the 100 Hz EA antinociception in the CFA-induced inflammatory nociception rats as in normal rats as reported previously [ 5 , 7].”
Background
Dynorphin induced magnetic ordering in lipid bilayers as studied by 31P NMR spectroscopy
Naito, A., Nagao, T., Obata, M., Shindo, Y., Okamoto, M., Yokoyama, S., Tuzi, S., & Saitô, H. (2002) · Biochimica et Biophysica Acta (BBA) - Biomembranes · doi:10.1016/s0005-2736(01)00420-5 · Cited by 35
Effect of Ethanol Drinking on the Gene Expression of Opioid Receptors, Enkephalinase, and Angiotensin‐Converting Enzyme in Two Inbred Mice Strains
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Centrally-administered opioid selective agonists inhibit drinking in the rat
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Non-cholinesterase effects of anticholinesterases
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Peptides and Nociception
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[3H]dynorphin a binding and κ selectivity of prodynorphin peptides in rat, guinea-pig and monkey brain
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“The discovery of dynorphin (Goldstein et al., 1979), the elucidation of its precursor (Kakidani et al., 1982), and the realization that multiple active opioids are derived from it (Weber et al., 1982; Suda et al., 1982; Kilpatrick et al., 1982; Fischli et al., 1982) have led to the attempt to…”
Background
κ-opiates and urination: Pharmacological evidence for an endogenous role of the κ-opiate receptor in fluid and electrolyte balance
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Potency of three opiate antagonists to reverse the inhibitory activity of dynorphin, enkephalins and opioid-like alkaloids on the guinea pig ileum
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Metabolism of Dynorphin A 1-13 in Human Blood and Plasma
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Evolving perspectives on neurobiological research on the addictions: celebration of the 30th anniversary of NIDA
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High-Performance Liquid Chromatography
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Behavioral and Neurochemical Aspects of Pediatric Pain
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Cellular Distribution and Function of Endorphins
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Authors: Goldstein, A., Tachibana, S., Lowney, L. I., Hunkapiller, M., & Hood, L.
Affiliations: California Institute of Technology (US)
ORCID: Hunkapiller, M
Hood, L
Venue: Proceedings of the National Academy of Sciences
Publisher: National Academy of Sciences
Published: 1979-12
Volume: 76
Issue: 12
Pages: 6666-6670
ISSN: 0027-8424 (ISSN-L)
1091-6490
DOI: 10.1073/pnas.76.12.6666
PMC: PMC411929
OpenAlex: W2033680879
Cited by: 882
References: 18
Citations by year: 2026: 8 · 2025: 9 · 2024: 8 · 2023: 14 · 2022: 10 · 2021: 14 · 2020: 23 · 2019: 13 · 2018: 8 · 2017: 9 · 2016: 6 · 2015: 8 · 2014: 16 · 2013: 23 · 2012: 18
FWCI: 24.93
Type: journal article
Language: en
Open access: green
europepmc.org
Locations: Proceedings of the National Academy of Sciences (publishedVersion)
Europe PMC (PubMed Central) (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
CaltechAUTHORS (California Institute of Technology) (submittedVersion)
Topics: Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Neuroendocrine regulation and behavior
Physical Sciences › Chemistry › Organic Chemistry › Chemical Synthesis and Analysis
Keywords: dynorphin A(1-13), opioid peptides, leu-enkephalin, enkephalin, naloxone, opioid receptors, vas deferens, peptide degradation, immunoreactivity
MeSH terms: Amino Acid Sequence, Animals, Biological Assay, Dose-Response Relationship, Drug, Endorphins, Guinea Pigs, Ileum, Radioligand Assay, Receptors, Opioid, Structure-Activity Relationship, Swine, Rats

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Dynorphin-(1-13), an extraordinarily potent opioid peptide.

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