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Advances in Endogenous and Exogenous Opioids - 1st Edition - ISBN: 9780444804020, 9781483161594

Advances in Endogenous and Exogenous Opioids

1st Edition

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

Editors: Hiroshi Takagi Eric J. Simon
eBook ISBN: 9781483161594
Imprint: Elsevier
Published Date: 1st January 1981
Page Count: 520
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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



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


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© Elsevier 1982
1st January 1981
eBook ISBN:

About the Editors

Hiroshi Takagi

Eric J. Simon

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