Advances in Endogenous and Exogenous Opioids

Advances in Endogenous and Exogenous Opioids

Proceedings of the International Narcotic Research Conference (Satellite Symposium of the 8th International Congress of Pharmacology) Held in Kyoto, Japan on July 26–30, 1981

1st Edition - January 1, 1981

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  • Editors: Hiroshi Takagi, Eric J. Simon
  • eBook ISBN: 9781483161594

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Advances in Endogenous and Exogenous Opioids contains the proceedings of the International Narcotic Research Conference (Satellite Symposium of the 8th International Congress of Pharmacology) held in Kyoto, Japan on July 26-30, 1981. The conference provided a forum for discussing advances that have been made in the understanding of endogenous and exogenous opioids and tackled a wide array of topics ranging from novel opiate binding sites selective for benzomorphan drugs to the purification of opioid receptors and sequellae of receptor binding. Comprised of 156 chapters, this book begins with an analysis of the interaction of opioid peptides and alkaloid opiates with mu-, delta-, and kappa-binding sites. The reader is then systematically introduced to biochemical evidence for kappa and sigma opiate receptors; the action of morphine and oxymorphone as partial agonists on the field-stimulated rat vas deferens; mechanisms of supersensitivity in the enkephalinergic system; and properties of the solubilized opiate receptor from human placenta. Subsequent chapters explore the biosynthesis of opioid peptides as well as their localization, release, and degradation; physiological and pharmacological actions of opioids; and the use of analgesia in acupuncture. Results of behavioral and clinical studies of endogenous and exogenous opioids are also presented, and the structure-activity relationships of opioids are examined. This monograph will be of interest to students, practitioners, and researchers in the fields of psychiatry and pharmacology.

Table of Contents


  • Preface

    Acknowledgments

    List of Participants

    Multiple Opioid Receptors

    The Interaction of Opioid Peptides and Alkaloid Opiates with μ-, δ- and κ-Binding Sites

    Characterization of Novel Opiate Binding Sites Selective for Benzomorphan Drugs

    Biochemical Evidence for Kappa and Sigma Opiate Receptors

    Characterization of Dynorphin Receptor Specificity in the Guinea Pig Ileum

    Opiate Receptors in the Guinea-Pig Ileal Mucosa

    Opiate Binding Sites in the Lumbo-Sacral Spinal Cord from Various Species

    Effects of Opioid Peptides and Kappa-Receptor Agonists on in Vitro Isolated Preparations

    Multiple Benzomorphan Binding Sites in a Clonal Cell Line

    Morphine and Oxymorphone Act as Partial Agonists on the Field Stimulated Rat Vas Deferens

    Specific Opiate Binding Sites in Human Placenta

    Multiple Binding Sites for 3H-Ethylketocyclazocine on the Lumbo-Sacral Portion of the Guinea-Pig Spinal Cord

    Differential Interactions of Dynorphin(1-13), β-Endorphin, and Enkephalin-Related Peptides at μ and δ Sites in Different Brain Regions

    Differential Effects of Isomers of Opioid Antagonists Upon μ-, κ- and δ- Agonist Analgesia: Comparison with Oxotremorine

    Potencies of "Mu" and "Kappa" Agonists on Smooth Muscle Preparations Relative to Displacement of 3H-Etorphine in Isolated Rat Brain Neural Membranes

    Comparison of 3H-Etorphine and 3H-Diprenorphine Receptor Binding in Vivo and in Vitro

    Tentative Identification of High Affinity Opioid Binding Sites in the Pedal Ganglia of the Marine Mussel Mytilus edulis

    Opioid Receptors on Rat Mast Cells

    Mechanisms of Supersensitivity in the Enkephalinergic System

    Postnatal Development of Opioid Mechanisms in Rat Vas Deferens

    Developmental Differences of Methionine Enkephalin and Naloxone Binding Sites in Regions of Rat Brain

    μ, δ and κ Opiate Receptors: Interconvertible Forms of the Same Receptor

    Purification and Nature of Opioid Receptors and Sequellae of Receptor Binding

    Characterization of Solubilized Active Opiate Receptors from Toad Brain

    Multiple Etorphine Binding Proteins from Brain

    Differences Between the Opiate Receptor and the Enkephalin Receptor in Rat Brain

    Properties of the Solubilized Opiate Receptor from Human Placenta

    Isolation of an Opiate Receptor and the Effect of Membrane Lipids on Isolated Receptor Binding

    Phosphatidyl Inositol as a Binding Component of Opioid Receptor

    Selectivity of Opiate and Opioid Peptide Interaction with Cerebroside Sulfate

    Irreversible Photoactivation of the Opiate Receptors in the Guinea-Pig Ileum by Some Enkephalin Derivatives

    Effects of Sulfhydryl-Protecting Reagents on Opioid Receptor Binding Site(s)

    Stimulation and Desensitization of cGMP Formation by Opioid Agonists in Cloned Neuroblastoma Cells

    Ascorbate Suppresses Opiate Induces Compensatory Increase in Cyclic AMP Levels in Neuroblastoma X Glioma Hybrid Cells

    A Case Against Receptor Occupancy as the Sole Determinant in the Opiate Regulation of Adenylate Cyclase Activity in Neuroblastoma Cells

    Increase in Plasma Cyclic Nucleotide Levels Induced by Morphine in Male Mice

    Biosynthesis of Opioid Peptides

    Structural Organization of the Corticotropin-β-Lipotropin Precursor Gene

    Biosynthesis and Maturation of Pro-Opiomelanocortin

    Multiple Forms of Beta-Endorphin (βE) in Pituitary and Brain: Effects of Stress

    Calcitonin-Like Peptide in Pro-Opiocortin: Functional Aspects

    Effect of Morphine or Alcohol Treatment on the Biosynthesis of β-Endorphin by the Neurointermediate Lobe

    Membranes of Bovine Chromaffin Granules Contain Enkephalin Precursors Larger than 100,000 Daltons

    Proenkephalin and Intermediates in the Biosynthesis of Enkephalins

    "Big" Enkephalins from Bovine Adrenomedullary Gland

    Conversion of Met-Enkephalin-Arg6-Phe7 to Met-Enkephalin by Dipeptidyl Carboxy-Peptidase

    Endogenous Novel Opioid Peptides

    Search for Morphine-Antagonistic Agents in Human CSF and Brain

    H-Endorphin, a Novel Endogenous Opioid with Unconventional Naloxone Interactions

    Isolation and Identification of Two New Peptides Related to β-Endorphin

    Isolation of Dynorphin-Like Peptide from Gut Extract

    Substantial Amounts of Immunoreactive BAM-12P and BAM-22P are Present in Bovine Adrenal Medulla but not in the Brain

    Detection of α-N-Acetyl β-Endorphins in Pituitary by Specific Antibodies

    Localization, Release and Degradation of Opioid Peptides

    Regional Distribution of Immunoreactive "Big" Leu-Enkephalins in Brain and Pituitary

    Anatomical and Biochemical Studies of Dynorphin

    β-Endorphin in the Brain and Pituitary; Evidence for Two Specific Processing Patterns

    Measurement of Met-Enkephalin (Arg6, Phe7) in Rat Brain by Specific Radioimmunoassay Directed at Methionine Sulphoxide Enkephalin (Arg6, Phe7)

    Opioid Peptide in the Dog Canine Pulp?

    Subcellular Localization of Analgesic Dipeptide, Kyotorphin (Tyr-Arg) in the Rat Brain

    Release of Endogenous Opioids from Spinal Cord in Vivo Following Sciatic Nerve Stimulation

    Noxious Stimulus-Induced Release of Met-Enkephalin from the Nucleus Reticularis Gigantocellularis of the Rat

    Intestinal Opioids May Modulate the Action of Acetylcholine on Peristalsis in Vitro. Release Studies Point to a Possible Role for Dynorphin in the Control of Peristalsis

    Inhibition of their Breakdown and Release of Endogenous Opioid Peptides from the Myenteric Plexus-Longitudinal Muscle of the Guinea Pig Ileum

    Properties of Enkephalinase from Mouse and Human Brain

    Discrete Regional Distribution for Enkephalinase and Aminopeptidase in Microdissected Rat Brain

    Physiological and Pharmacological Actions of Opioids

    Opiates Cause Activation of a Calcium-Dependent Potassium Conductance

    Enkephalinergic Presynaptic Inhibition in Mammalian Sympathetic Ganglia

    Actions of Enkephalin on Single Neurons in Ciliary Ganglia

    The Distribution of Receptors for Enkephalin and Morphine in the Dorsal Horn of the Cat

    Mutual Inhibition of Spinal Nociceptive Pathways

    Differential Effects of Opioids on Single Neurones in Rat Brain

    Possible Existence of Enkephalinergic Neurons in the Striato-Pallidal Pathway in the Rat Brain

    Excitatory Action of Microelectrophoretically Applied Kyotorphin (Tyr-Arg) on Unitary Activity in the Rat Cerebral Cortex

    Endorphins as Mediators of Ethanol Actions: Multidisciplinary Tests

    The Modulatory Effect of Morphine and Monoamine Oxidase β (MAO-β) System on Enkephalin-Induced Seizures

    Use of the Novel Opiate, β-Funal Trexamine (β-FNA) in the Elucidation of Receptor Types Involved in Opiate-Mediated Respiratory Depression

    Diurnal Rhythm in Response to Noxious Stimuli — Increase of Met-Enkephalin in Globus Pallidus

    Effects of Psychotropic Drugs on the Levels of Enkephalins, their Receptors and Enkephalinase in Rat Brain

    Changes of Brain Immunoreactive Dynorphin Content Following Amygdaloid-Kindled and Recurrent Seizures

    Effects of Feeding and Drinking on Immunoreactive Beta-Endorphin and ACTH Levels in Plasma and Hypothalamus in Rats

    Pituitary Endorphin Levels Following the Administration of Benzamide Substitutes

    Opioid and Dopamine Receptor Interactions in Mammalian Brain

    The Role of Dopaminergic System on Morphine Analgesia in Mice

    Morphine Produces Different Effects on Subtypes of Mesencephalic Dopamine Systems

    Effect of Adrenergic Drugs on the Central Antidiuretic Action of Morphine in Rats

    Effect of Morphine on ATP-Stimulated 45Ca++ Uptake in Subcellular Fractions of Rat Brain

    Analgesia and Acupuncture

    Spinal Mechanisms in the Effects of Fentanyl and Morphine on the Rat Tail Flick

    Strong Analgesic Activity of Leu-Enkephalin after Inhibition of Brain Aminopeptidase: A Pharmacological Study.

    Opioid and Nonopioid Mechanisms of Stress-Induced Analgesia

    Antinociceptive and Toxic Activities of Intracerebroventricularly (ICV) Administered Morphine (M), 6-Acetylmorphine (AM) and 3, 6-Diacetylmorphine (DAM) in Mice

    Possible Involvement of Intrinsic Opioid Peptides and Serotonin in Phenylethylamine Analog-Induced Analgesia

    Analgesic Properties of D-Phenylalanine, Bacitracin and Puromycin in Mice: Relationship to Inhibition of Enkephalinase and Beta Endorphinase

    Changes in Antinociception after Exposure of Animals During Early Development to Chronic Stress and Chronic Administration of Narcotic Analgesics

    Dynorphin: Differential Interactions with Opiates and Peptides in Naive and Morphine Tolerant Mice

    Central Norepinephrine in Acupuncture Analgesia: Differential Effects in Brain and Spinal Cord

    Afferent and Efferent Pathways in Acupuncture Analgesia and their Correlation with Morphine Analgesia

    Suppression by Morphine and Acupuncture on Noxious Information in the Rat Central Nervous System

    Parallel Individual Variations in Effectiveness of Acupuncture, Morphine Analgesia and Dorsal PAG-SPA and their Abolition by D-Phenylalanine

    The Role of Central 5-Hydroxytryptamine in Acupuncture Analgesia and Acupuncture Tolerance

    Central Norepinephrine: Its Implication in the Development of Acupuncture Tolerance

    Aβ Nerve Impulse Produces Electroacupuncture Analgesia in Rat

    Acupuncture Suppresses the Jaw Opening Reflex Related to Noxious Input in Rat

    Effects of Electroacupuncture on the Levels of Endorphins and Substance P in Human Lumbar CSF

    CSF Endorphin Levels in Chronic Pain Patients and in Patients Before and After a Placebo Pain Relief

    β-Endorphin in Obsteric Analgesia

    Descending Inhibition in Human Spinal Cord

    Behavioral and Clinical Studies

    Neuroleptic-Like and Anti-Psychotic Action of γ-Type Endorphins

    Multi-Dimensional Analyses of Behavior in Mice Treated with Endorphins

    Effects of Opioid Drugs on Active Avoidance Behavior of the Rat

    Behavioral Effects of Prolactin: Involvement of Opioid Receptors

    Interaction Between Morphine and PhencycHdine: Intoxication and Cross-Tolerance

    Enkephalinergic Modulation of Circling Behavior Induced by Dopamine in the Nucleus Accumbens and Nucleus Caudatus

    Exogenous Opioids and Drinking and Feeding

    Unusual Behavioral Properties of Some New Opioid Peptides

    The Role of Endorphins in Schizophrenia: Clinical Studies

    Naloxone Reverses Induced Ischemic Neurologic Deficit in Gerbils

    Naltrexone and Psychotherapy

    Patient Control of Methadone Maintenance Dose

    Laam Instead of Take-Home Methadone

    Effects of Chronic Exogenous Opioid Administration on Levels of One Endogenous Opioid (β-Endorphin) in Man

    Naloxone and Thyrotropin Releasing Hormone Have Additive Effects in Reversing Endotoxic Shock

    The Role of Enkephalins in Blood Pressure in the Brain

    Structure-Activity Relationships of Opioids

    Active Sites in the β-Endorphin Structure for Activation of the Epsilon-Opiate Receptor

    Critical Components of Opioid Peptides for Specific Recognition of μ and δ Receptors

    Highly Active Dipeptide and Tripeptide Enkephalin Analogs

    Two New Classes of Cyclic Enkephalin Analogs with High Potency and Specificity for μ-Receptors

    "Minimal Segment" of Enkephalin for Analgesia: Syndyphalin (SD)-33, a Simple Tripeptide Alkylamide with Prolonged Subcutaneous Analgesic Activity

    The Analgesic Effects of Cyclic Dipeptides by Intracerebral Administration in Conscious Mice and Rats

    Synthetic Opioid α-Casein Peptides: Structure Activity Relationship

    Some Structure-Activity Relationships in the 2′-Mercaptobenzomorphan Series

    Chemical Structure and Pharmacological Activities of Diphenylethylpiperazine Derivatives

    Peripheral Selectivity of Quaternary Narcotic Antagonists: Relative Ability to Prevent Gastrointestinal Transit Inhibition and Antinociception in Morphinized Rats

    Structure-Activity Relationship Study of Affinity Labels that are Specific for μ Opioid Receptors

    Arylazido Derivatives of 14B-Aminomorphinone: Potential Photoaffinity Ligands for Opiate Receptors

    Antagonist-Agonist Activity of Some TV-Substituted Benzomorphans

    The Action of 2-Aminotetralin (2-AT) Derivatives on Human Plasma Cholinesterase (HPC)

    How Quantum Chemistry Can Delineate the Differing Molecular Requisites for Interaction with μ, δ, κ σ and Other Opiate Receptors

    Tolerance and Physical Dependence

    Opiate and Clonidine Dependence in the Final Cholinergic Motoneurone of the Guinea-Pig Isolated Ileum

    Cross-Tolerance and Cross-Dependence on Multiple Opiate Receptors of the Guinea-Pig Ileum

    Properties of Opiate Receptor Binding in an Opiate Tolerant State

    Importance of Opiate Receptors of the Substantia Gelatinosa to Morphine Tolerance and Dependence of Cat Dorsal Horn Neurones

    Tolerance to Electroacupuncture and its Cross Tolerance to Morphine

    Acupuncture and Morphine Analgesia Inhibitory Systems and its Correlation with Morphine Tolerance

    Phosphorylation of Striatal Synaptic Plasma Membrane Proteins from Morphine-Tolerant Rats

    Physical Dependence Liability of Tetrapeptide Acylhydrazide Analogs of Enkephalin in Rats

    Naloxone Reversible Effect of Morphine on Substance P Neurons in the Rat Spinal Cord

    Involvement of GABA in the Acute and Chronic Effects of Morphine: Nociceptive GABA Release and Receptor Binding Studies

    The Involvement of Brain Histaminergic Mechanisms in the Withdrawal Phase of Morphine Dependence

    A Potentiation of Physical Dependence by 6-Conjugation of Morphine and Nalorphine

    Transport and Binding in Vivo of 3H-Naloxone in Brains of Morphine Dependent and Withdrawn Mice

    Inhibition of Tolerance to Human Beta Endorphin by a Linear and a Cyclic Peptide

    Differential Effects of Thyroliberin on Tolerance to the Analgesic and Hypothermic Effects of Morphine in Mice

    Induction of Physical Dependence in Rats by Short Treatment of Morphine-Admixed Food

    Tolerance as the Only Sign of Withdrawal in Opiate Dependent Chick Fetuses

    Caffeine Enhances Morphine Dependence in Humans

    Schedule Induced Self Injection of Heroin: Dose-Response Relationships

    Opiate Detoxification Using Lofexidine

    Detection of Morphinone as a New Metabolite of Morphine in Guinea Pig Urine

    Ketamine-Like Discriminative Characteristics of the Stereoisomers of Metazocine, Cyclazocine, and SKF 10,047 in Rhesus Monkeys

    Concluding Remarks

    Author Index

Product details

  • No. of pages: 520
  • Language: English
  • Copyright: © Elsevier 1982
  • Published: January 1, 1981
  • Imprint: Elsevier
  • eBook ISBN: 9781483161594

About the Editors

Hiroshi Takagi

Eric J. Simon

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