Pharmacology of Opioid Peptides

539 Pages·1995·39.41 MB·\539

by  L F Tseong (Editor)

The Pharmacology of Opioid Peptides

The Pharmacology of Opioid Peptides
edited by
Leon F. Tseng
Medical College of Wisconsin
Wisconsin, USA
Boca Raton London New York
CRC Press is an imprint of the
Taylor & Francis Group, an informa business
First published 1995 by Harwood Academic Publishers
Published 2018 by CRC Press
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© 1995 by Taylor & Francis Group, LLC
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ISBN-13: 978-1-56881-079-9 (hbk)
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British Library Cataloguing in Publication Data
Pharmacology of Opioid Peptides
I. Tseng, Leon F.
612.015756
Contents
PREFACE vii
LISTOFCONTRIBUTORS xi
1. Selectiveligandsfor /xand 8opioidreceptors
Richard J. Knapp, Linda K. Vaughn and Henry L Yamamura 1
2. Kand eopioidreceptor binding
Bruce Nock 29
3. Molecularcharacterization ofopioid receptors
Karen Miotto, Karin Magendzo and Christopher J. Evans 57
4. Pharmacological regulation ofopioidpeptidegene expression:
second andthirdmessenger systems
Keith R. Pennypacker 73
5. Enzymesinvolvedinopioidpeptide biosynthesis
Lloyd Fricker and Lakshmi Devi 87
6. G-Proteins andopioidreceptors' functions
Ping-Yee Law 109
7. Cellularmechanisms ofexcitatory andinhibitory actionsofopioids
Li- Yen Mae Huang 131
8. Regulation ofenkephalins andcatecholamine synthesizing
enzymesintheadrenal medulla
J.S. Hong and MX. Stachowiak 151
9. Functionalrolesofopioidsinthe hippocampus
Carrie T. Drake and Charles Chavkin 169
v
VI Contents
10. Regulation ofenkephalin inglia
Michael McMillian 187
11. Themodulation ofnociceptionby enkephalin-containing
neurons inthebrainstem
Herbert K. Proudfit and David C. Yeomans 197
12. Pharmacological characterization ofopioid 8-and K- receptors
Frank Porreca, Edward J. Bilsky and Josephine Lai 219
13. Mechanisms of/3-endorphin-induced antinociception
Leon F. Tseng 249
14. Theeffects ofdiabetes onopioid-induced antinociception
Junzo Kamei and Yutaka Kasuya 271
15. Opioidpeptides,opioidreceptors andperipheral analgesia
A. Hen 287
16. Modulation ofopioidreceptorsbyanti-opioid peptides
Carl B. Goodman, Gregory I. Elmer, Hsiu-Ying T. Yang,
C.H. Lee and Richard B. Rothman 303
17. Nitrous oxideandendogenous opioidpeptides
Raymond M. Quock and Linda K. Vaughn 321
18. Theroleofopioidpeptidesinenvironmentally-induced analgesia
David J. Mayer and Barton H. Manning 345
19. Opioidpeptidesingastrointestinal functions
Thomas F. Burks 397
20. Theroleofopioidpeptides inimmune function
Virginia M. Sanders 411
21. Opioidpeptidesincardiovascular andrespiratory regulation
Pirkko Paakkari and Giora Feuerstein 425
22. Endogenous opioids and addiction
A. Herz and R. Spanagel 445
23. Cellularmechanisms ofopioidtolerance and dependence
William W. Fleming and David A. Taylor 463
INDEX 503
Preface
About 25 years have passed since Solomon Snyder, Lars Terenius and Eric Simon
independently identified abinding site in the brain membrane for radiolabeled naloxone,
apotent opioidreceptor antagonist.About 15to20yearshaveelapsed sinceJohn Hughes
andHansKosterlitzpurified enkephalins,andataboutthesametimeChohHaoLi purified
the endorphins and Avram Goldstein purified the dynorphins. Since then our knowledge
of the pharmacology of opioids and opioid peptides has expanded enormously. These
developments have been accompanied by a corresponding increase in our understanding
ofthemechanism ofthe actions of opioids and opioid peptides and theirreceptors which
perform theirbiological functions.
Morerefined binding studieshave shownthatopioidreceptors haveatleastfour forms:
8, fi,K and e.Enkephalinshavebeenconsideredtobetheendogenous ligandsfor 8opioid
receptors,dynorphinsfor Kopioidreceptors,and/?-endorphinfor eopioidreceptors.Studies
of the opioid receptors are facilitated by the development of a large number of selective
ligands available that include agonists, antagonists, and irreversible alkylating agents. In
thisbookRichardKnapp,LindaVaughnandHenryYamamuradescribethecharacteristics
of 8and /xopioid receptors, and Bruce Nock describes the K and s opioid receptors and
someoftheirligands.
Thisbookisbeingpublished atatimewhentheopioidreceptors,/x, 8and/c,havebeen
recentlycloned.KarenMiotto,KarinMagendzoandChristopherEvansreviewthehistoryof
thestructuralcharacterizationofopioidreceptorsandtherecentadvancesintheirmolecular
cloning and expression. They tell about the firstfunctionally confirmed isolated opioid 8
receptor. The identification of this 8receptor quickly led to the isolation of other classes
of opioid receptors such as /xand K.Connecting these cloned opioid receptors with the
pharmacologyofopioidreceptoractionsisimportant.Theantisense oligodeoxynucleotides
have proved to be useful pharmacological tools for studying neurotransmitter receptor
activities both in vitroand in vivo. Frank Porreca et al. and Leon Tseng describe the use
ofantisense oligonucleotide inregard to 8receptor mRNA to elucidate therole of neural
mechanisms inopioid-induced analgesia.
Opioidpeptidesareinitiallyproducedaslargerprecursorsthatundergopost-translational
modification and proteolytic cleavages to produce bioactive peptides. A large variety of
peptides,eachwithdistinctbioactiveproperties,areproducedfromthethreeopioidpeptides
precursors: proopiomelanocortin (POMC), proenkephalin and prodynorphin. The opioid
peptide genes produce mRNAs for precursor proteins which are processed at specific
punctuation points by selectiveproteins.KeithR.Pennypacker describes the mechanisms
that regulate transcription of the proenkephalin gene. The regulation of proenkephalin in
vu
vin Preface
the hippocampus with respect to the seizure paradigm and dopaminergic regulation in
the striatum will be emphasized. Michael McMillian emphasizes the second messenger
pathways and receptors involved in preproenkephalin gene regulation. Lloyd Flicker and
Lakshmi Devidescribe theenzyme responsible for theprocessing steps whichplay akey
roleintheregulationofopioidpeptide expression.
The opioid system is a complex intercellular communication system that modulates
physiologic processing such as the stress response, analgesia, immunity, neuroendocrine
function, gastrointestinal and cardiovascular control, and addiction. These diverse effects
aremediatedbythereleaseofendogenousopioidpeptideswhichactivatespecificmembrane
receptors.Wewillnextexplorethefieldsofopioidpharmacologyandphysiologytoillustrate
thecellular and subcellular actions ofopioids and opioid peptides.All ¡i,5,and K opioid
receptorsbelongtoafamily ofG-protein coupledreceptors.Ping-YeeLawgivesageneral
overview of the mechanisms involved and then addresses the question of whether there
is a receptor which acts selectively toward G-proteins and the role of G-proteins in the
chronicactionsoftheopioidpeptides.Li-YenMaeHuangfurtherdiscussessomeinteresting
topics of opioid actions. The adrenal medulla and the hippocampus are the ideal model
systemsforstudyingthecellularmechanismsofopioidactions.JohnS.HongandMicheal
K. Stachowiak describe the regulation of the gene expression of proenkephalin, tyrosine
hydroxylase and phenylethanolamine N-methyltransferase in the adrenal gland cells and
the second messenger systems that mediate those regulations. Carrie Drake and Charles
Chavkindescribethefunctional rolesofopioidsandopioidpeptides inthehippocampus.
Since analgesia or antinociception is one of the most important clinical functions for
opioidsandopioidpeptides,thisbookconcentrates indetailonthemechanisms ofactions
ofopioidsandopioidpeptidesfortheproduction ofanalgesia.HerbertProudfit andDavid
Yeomansreview the current state ofunderstanding related tothe location andfunction of
enkephalin-containing neuronsthatareinvolvedinmodulatingnociception.FrankPorreca
et al.describestheneuralmechanismsofantinociceptioninducedby 8and Kopioidagonists,
andLeonTseng describes themechanism ofactions of antinociception induced by s and
¡iopioid agonists.The antinociception induced by s opioid receptor agonist /*-endorphin
is mediated by the release of Met-enkephalin acting on the 8opioid receptors, while the
antinociceptioninducedby ¡JLopioidreceptoragonistmorphineismediatedbythereleaseof
noradrenaline and serotonin actingona?2adrenoceptors and5-HTreceptors.Junzo Kamei
andYutakaKasuyapresent theevidence thatthe antinociception mediated by \JL receptors
isattenuatedbydiabetesinmice,whiletheantinociceptionmediatedby sand 8receptorsis
enhanced.Theseantinociceptiveeffects ofopioidsaremediatedbythereceptorswithinthe
central nervous system. Albert Herz describes the circumstances — such as hyperalgesia
caused by inflammation — in which peripheral sites of opioid actions also occurs. Carl
Goodman et al.describe some anti-opioid peptides, such asCCK, dynorphins and NPFF
whichmodulate the antinociceptive effects ofopioids.David Mayer and Barton Manning
give a comprehensive review on the role of opioid peptides in environmentally-induced
analgesia. Raymond Quock and Linda Vaughn describe the role of opioid peptides on
nitrousoxide-induced antinociception.
In addition, a set of complementary chapters describe other important aspects of the
pharmacological actionsofopioidsandopioidpeptides.ThomasBurksdescribestheroles
ofopioidpeptidesingastrointestinalfunctions.VirginiaSandersdescribestheroleofopioid
Preface IX
peptides inimmune function. Pirkko Paakkaria and Giora Feuerstein describe the actions
ofopioidpeptides incardiovascular andrespiratory regulation.
Finally,twochaptersaredevotedtodealingwiththeissueoftoleranceanddependenceof
opioids.AlbertHerzandR.Spanageldescribetheroleofendogenousopioidsinaddiction.
The study of the motivational effects of drugs in suitable animal models is essential to
gain better insights into the neurobiological mechanisms of addictive behaviors. William
W.Fleming andDavidTaylorgiveacomprehensive reviewonthecellularmechanisms of
opioidtolerance anddependence.
Thisbookexaminesthemostimportant aspects ofthephysiology andpharmacology of
opioids and opioid peptides. The book is suitable for researchers interested in the neural
mechanisms of the pharmacologic and physiologic functions of the endogenous opioid
system andforclinicians whoareinterested inpainmanagement and assessment.
Ishouldliketothankallthecontributorstothisbookfortheircooperationincompleting
their chapters. Production of this book owes much to the dedicated editorial assistance
of Mrs Candace Tseng as she proofread and edited all the chapters. Much thanks are
alsoextended toDr.JohnP.Kampine,Chairman, Department ofAnesthesiology, Medical
CollegeofWisconsin,forhisencouragement and support.
LeonF.Tseng