Endogenous and Exogenous Opiate Agonists and Antagonists - 1st Edition - ISBN: 9780080254883, 9781483145266

Endogenous and Exogenous Opiate Agonists and Antagonists

1st Edition

Proceedings of the International Narcotic Research Club Conference, June 11-15, 1979, North Falmouth, Massachusetts, USA

Editors: E. Leong Way
eBook ISBN: 9781483145266
Imprint: Pergamon
Published Date: 1st January 1980
Page Count: 592
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Endogenous and Exogenous Opiate Agonists and Antagonists documents the proceedings of the International Narcotic Research Club Conference, held in North Falmouth, Massachusetts, USA, on 11-15 June 1979. The volume begins with a discussion of the programs of the World Health Organization, with an emphasis on the components of its drug dependence program. The 139 papers discussed at the conference are then presented. These papers are organized into 10 parts. The papers in Part I examine structure-activity relationships. Part II contains studies on receptor binding while Part III deals with the localization and characterization of active sites. Part IV focuses on ligands and receptor isolation. Part 5 examines neurochemical interactions. Part VI presents papers on disposition and metabolism. Parts VII and VIII take up analgetic mechanisms and neuroendocrine relationships, respectively. Part IX focuses on behavioral effects while the studies in Part X cover tolerance and physical dependence.

Table of Contents


Who Role in Drug Addiction

I-Structure-Activity Relationships

Primary Structure and Specificity in Endogenous Opioid Peptides

Synthetic ßh-Endorphin Analogs Modified at the N-Terminal, Positions 2 and 5

Chemical Features for Opiate Agonist and Antagonist

The Synthesis and Agonist Activity of Some 14ß-Substituted Morphine and Codeine Derivatives

4-Aryl-4-Aminocyclohexanone Derivatives: a Chemically Novel Series of Analgesics including Opioid Antagonists and Extremely Potent Agonists

N-methylbenzomorphanalkanones. a Comparison of Their Structure-Activity Relationships and X-ray Crystal Structure with Those of the Bridged Thebaine Derivatives. An Opiate Receptor Proposal

Quantum Chemical Studies of Novel 4-Phenylpiperidine Opiates with Antagonist Activity

Structure-Function Studies in Peptides Related to the ß-LPH61-64 Sequence

Enkephalin Analogs and Physical Dependence

II-Receptor Binding

Interaction of a Model Opiate Anionic Receptor Site with N-Substituents of Rigid Opiates: Pcilo Energy Calculations

Effects of Monovalent Cations on Cerebroside Sulfate Binding to Opiate Agonists and Antagonists

Opiate Binding and Cerebroside Sulfates in Brain and Lung of Developing Chick

Opiate Receptor Binding Studies Influence of a Reversible Sulfhydryl Reagent

Ascorbate Destruction of Opioid Stereospecific Binding: Evidence for Receptor Regulation by Membrane Lipid

The Study of Enkephalin-Receptor Interaction Using Isosterically Modified Analogues

Seasonal Variation in the Apparent Number of H-naloxone Binding Sites

Evidence for Half-of-the-Sites Reactivity in the Binding of Opiate Agonists and Antagonists to the Opiate Receptor

Effects of Anesthetics In Vitro on Brain Receptors for Opiates, Spiroperidol and Ouabain

Opioid Agonists and Antagonists: Action on Multiple Opiate Receptors

Study of Opiate Receptor Multiplicity in Rats by In Vivo Binding Assays

Comparison of the Binding Characteristics of Opiates and Opioid Peptides

Type 1 and Type 2 Opiate Receptors: A Subclassification Scheme Based upon GTP's Differential Effects on Binding

Scatchard Analysis of Opiate Receptor Binding

Multiple Opiate Binding Sites in Rat Brain: Differential Displacement of 3h-Naloxone Binding by Different Opiate Ligands

Phenoxybenzamine, an Irreversible Ligand of Opioid Receptors In Vivo?

Tolerance, Cross-Tolerance and Dependence to µ and k Agonists In Vivo and In Vitro

Specific Protection of µ-and δ Binding Sites in Guinea-Pig Brain, Against the Inhibitory Effect of Phenoxybenzamine, by Agonists Preferentially Interacting with µ-or δ-Sites

Ligand Specificity of Opioid Binding Sites in Brain and Peripheral Tissues

Multiple Opiate Receptors: Evidence for Mediation of Analgesia by a Subpopulation of Receptors

Abnormal Brain Opiate Mechanisms in Schizophrenia

III-Localization and Characterization of Active Sites

Characterization of 3H-ß-Endorphin Binding in Rat Brain

α-MSH in Brain ß-Endorphin Neurons, and Other Neurons as Well

Opioid Receptor Autoradiography in Brains of Humans and Animals

Development of Opiate Tolerance/Dependence in the Guinea-Pig Myenteric Plexus and the Mouse Vas Deferens

Iontophoretically Applied Morphine and Met-Enkephalin May Interact with Different Receptors in the Brain

Local and CNS-Mediated Effects of Morphine and Narcotic Antagonists on Gastrointestinal Propulsion in Rats

Central Effects of ß-Endorphin on Intestinal Transit

Effects of 6-Hydroxydopamine and 5,7-Dihydroxytryptamine Brain-Stem Lesions on Morphine Analgesia in the Rat

Opioid-Induced Hypermotility in Rats

Differences between the Mechanism of Action of Morphine Antinociception in Mice and Rats

Actions of Opioid Peptides on the Responsiveness of Reticular Neurones to Tooth-Pulp Stimulation

Inhibition of Glutamate Induced Cortical Release of Adenine Derivatives by Opiates and Enkephalin

Intrastriatal Injection of Morphine: Effect on EMG-Recorded Activity of the Gastrocnemius-Soleus Muscle of Rats

EEG Alterations Induced in Rats by Ethylketocyclazocine, Cyclazocine, and Morphine: the Differential Effects of Naloxone

Ontogenesis of Enkephalinergic Systems in Rat Brain

Immunohistochemical Localization of Methionine Enkephalin in Old World Primates: Preliminary Observations

Endorphin and Corticotropin Regulate the Activity of Septal-Hippocampal Cholinergic Neurons

Naloxone Excitation of Spinal Dorsal Horn Units Shows Diurnal Variation

IV-Ligands and Receptor Isolation

Partial Purification of Endorphins from Human Cerebrospinal Fluid from Chronic Back Pain and Elective Surgery Patients

Identification of a New Opioid Peptide from the Bovine Brain and its Mechanism of Action

Acupuncture Tolerance in Rats: Anti-Opiate Substrates Implicated

Studies on Possible Precursors for the Enkephalins

Enkephalin Precursors from Guinea-Pig Myenteric Plexus

Characterization of High Molecular Weight Enkephalin Immuno-Reactivity in Rat Brain and Bovine Adrenal Medulla

Tentative Subunit Composition of Enkephalin-Macromolecule Complexes

Characterization of a High Affinity 3h-ßh-Endorphin Receptor in Rat Brain Crude Synaptosomal Fraction

Endorphin-Regulated Protein Phosphorylation as a Functional Entity of the Opiate-Receptor Complex

ß-Casomorphins-Novel Opioid Peptides Derived from Bovine Casein-Isolation and Structure

V—Neurochemical Interactions

The Effect of Opioids on the Phosphorylation 'In Vitro' of Synaptic Membrane Proteins

ß-Lipotropin, Corticotropin and ß-Endorphin: Phosphorylation by Cyclic AMP-Dependent and Independent Protein Kinases

Phosphorylation of Endogenous ß-Lipotropin and Other Peptides by Slices of Pituitary, Adult Brain and Neonate Brain of the Rat

The Role of Na+ and GTP in NG108-15 Opiate Receptor Function

Growth Inhibition Induced by Methadone: Prevention by Dibutyryl Cyclic Adenosine Monophosphate

Calcium Ions and Opioid Action in Neuroblastoma X Glioma Hybrid Cells

Calcium Antagonism of Opiate Action in the Non-Tolerant and Tolerant Guinea Pig Ileum

Opioid-Induced Changes in Cell Surface Composition of Neurotumor Cell Lines

A Role of Lipid in Opiate-Receptor Interaction

Potentiation of Opiate Effects in the Neuroblastoma Cell Line N18tg-2 by Sulfatide Incorporation

Search for a "Sodium Effect" in the Action of Opiates on Human Plasma Cholinesterase

VI-Disposition and Metabolism

Release of Endorphins and their Modulation from Rat Brain In Vitro

In Vitro Biosynthesis and Chemical Characterization of ACTH and ACTH Fragments by the Rat Pars Intermedia

Maturation of the Common Precursor for Beta-Endorphin and Alpha-MSH in the Rat Pars Intermedia

Pain Threshold and Brain Endorphin Levels in Genetically Obese (ob/ob) and Opiate Receptor Deficient (CXBK) Mice

Specific Processing of Endorphins in Rat Brain

Plasma Levels of ß-Endorphin/ß-Lipotropin in Humans under Stress

The Occurrence of ß-Endorphin and of Alpha-Melanotropin in the Secretory Granules of Anterior Pituitary Corticotropin/Endorphin Cells May be Coupled

Corticotropin, ß-Lipotropin/ß-Endorphin and the Non-Corticotropin/ß-Lipotropin Portion of Their Common Precursor Are Present in the Same Secretory Granules

Humoral Endorphin: Endogenous Opiate in Blood Cerebrospinal Fluid and Brain

Demonstration of Placental Endorphins by Radioimmunoassay and Radioreceptor Techniques

Increased Biosynthesis of ß-Endorphin in the Pars Intermedia of Rat Pituitaries after Long-term Treatment with Haloperidol

Biosynthesis of Beta-Endorphin and Alpha-MSH in the Pars Inter-Media of Rat Pituitaries

Endorphin Levels in the Rat Brain after the Tooth Pulp Stimulation

In Vitro Evidence for an Involvement of Intestinal Endorphins in the Control of Peristalsis in the Guinea Pig Ileum. Comparison to Rabbit, Rat, Cat and Dog Small Intestine

Using HPLC and Fluorometric Methods in Studying Endogenous Peptides

Characterization of Enkephalinases

Further Characterization and Kinetics of Appearance of Hydrolysis Products of Met-Enkephalin

Degradation of Enkephalin by Two Brain Enzymatic Activities

Enkephalinase: Preliminary Characterization and Comparison with Angiotensin Converting Enzyme

VII-Analgetic Mechanisms

Antagonism of Morphine Action by Cerebroside Sulfate Antibody

One Way Cross Tolerance from Morphine to Nantradol-A Potent, Non-Opioid Analgetic

Oral Tryptophan as a Potential Adjunctive Therapy in Chronic Pain Patients

Dietary Supplementation with L-Tryptophan Reverses Tolerance to Analgesia Induced by Periaqueductal Gray Stimulation in Humans

Further Studies on the Analgesic Activity of D-Phenylalanine (DPA) in Mice and Humans

The Antipeptidases Increase Electroacupuncture Analgesia and Show Predictable HYP Algesic Effects on Mice with Congenitally Abnormal Endorphin Systems

Biphasic Dose Response to Buprenorphine in the Rat Tail Flick Assay: Effect of Naloxone Pretreatment

Is ß-Endorphin Involved in the Analgesia Generated by Stress?

Central 5-Hydroxytryptamine, Opiate-like Substances and Acupuncture Analgesia

Ultraviolet Radiation-Induced Nociception: Basis for a Novel Analgesic Test in Mice

VIII-Neuroendocrine Relationships

Estrogen Treatment Alters Narcotic Disposition in the Rat

Effects of Morphine on Serum Prolactin Levels and Dopamine Turnover in the Median Eminence: Acute and Chronic Effects

The Effect of Acute Administration of Morphine and Opiate Antagonists on the Indole Content of the Rat Pineal Gland

Changes Induced by an Opioid on Blood Glucose and Insulin in the Rat

Narcotic Antagonists Increase Serum Luteinizing Hormone Levels by a Nontestosterone-Dependent Mechanism

IX—Behavioral Effects

Naloxone's Effects on a Variety of Motivated Behaviors

The Activation of Endorphin(s) by Reward

Discrimination of the Interoceptive Stimuli Produced by Phenyl-Quinone. A Measure of the Affective Component of Pain in the Rat

Generalization Study with Some Narcotic and Nonnarcotic Psychoactive Drugs in Rats Trained to Discriminate between Cyclazocine and Saline

Discriminative and Reinforcing Effects of Some Systematically Active Enkephalin Analogues

Naloxone Antagonism of Morphine-Withdrawal Body Shakes by an Auditory Conditional Stimulus

Possible Gaba Involvement in the Mediation of Narcotic Antagonist-Induced Aversions

Endogenous Opiates as Mediators of Activation and Coping

Similarity between Behavioral Effects of Des-Tyrosine-Y-Endorphin and Haloperidol and of A-Endorphin and Amphetamine

Diurnal Differences in Enkephalin Levels Correlated with Nociceptive Sensitivity

Endorphin-like Responses Provoked by Intracerebroventricular Peptidase Inhibitors in Mildly Stressed Rats

Actions of Hyperalgesic Substances (-) Naloxone, Theophylline and 5-Methoxy-N, N-Dimethyltryptamine on Nociceptive Learning

The Effect of Prototype Opiate Receptor Agonists and Opioid Peptides on Body Temperature and Behavior after Central Administration to Cats

Naloxone Improvement of Shock Pathophysiology: Evidence for Opiate Receptor Involvement

Naloxone Reversal of Hypotension Caused by Spinal Transection

Electroconvulsive Shock (ECS) in Rats: Naloxone Modification of Post-ECS Behaviors Provides Evidence for Functional Endorphin Release

X-Tolerance and Physical Dependence

Evidence for Biochemical Adaptation in Morphine Tolerance Dependence

Serotonin-Substance-P Pathway in the Manifestation of Gut Withdrawal

Development of Tolerance to and Dependence of Opioids in the Isolated Longitudinal Muscle Strips of Guinea Pig Ileum

Lack of Dependence Liability of Dezocine (WY-16225) in the Myenteric Plexus-Longitudinal Muscle Strip of Guinea Pig Ileum

Tolerance, Dependence and Quasi-Dependence in the Guinea-Pig Isolated Ileum

Interactions between Clonidine and a Withdrawal-Inducing Benzazocine upon the Isolated Mouse Vas Deferens and Guinea Pig Ileum

An Eexamination of Tolerance to the Antinociceptive Effects of Morphine, Clonidine and Their Combination in the Mouse Tail Immersion Test

Differential Effects of Leu- and Met-Enkephalin on Narcotic-Induced Enhancement of Naloxone Efficacy

Exaggerated Weight Loss in Genetically Obese (ob/ob) Mice by Withdrawal from Morphine

N-Dealkylation in the CNS: Effect of Tolerance and Opiate Antagonists

Electroacupuncture Hypalgesia is Enhanced in Morphine Dependent Mice; Showing No Cross-Tolerance and Reducing Signs of Withdrawal

Study of Cross-Tolerance to the Effects of Morphine and Methadone on the EEG and Behavior of the L-Alpha-Acetylmethadol (LAAM)-Maintained Rat

Development of Tolerance to Opiates in Explants of Mouse Spinal Cord with Attached Dorsal Root Ganglia

The Effects of Melanocyte-Stimulating Hormone Release Inhibiting Factor and Synthetic Analogs on Tolerance to and Physical Dependence on Morphine

Modification of Development of Physical Dependence on Morphine by Thyrotropin-Releasing Hormone

Inhibition of Tolerance to Morphine by DPHE7-ACTH(1-10)-NH2

Dependence in Non-Addict Humans after a Single Dose of Morphine

Opiates and Social Dependence

Reversal of Clonidine-Induced Hypotension by Opioid Antagonists in Man

Author Index


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E. Leong Way

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