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Opioid Peptides: Medicinal Chemistry



NIDA Research Monograph, Number 69 [Printed in 1986]

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Table of Contents

Foreword-----v
Marvin Snyder

Introduction-----1
Rao S. Rapaka

Frontiers of Research in the Medicinal Chemistry and Molecular Pharmacology of Opioid Peptides-----3
Rao S. Rapaka

Synthesis of Opioid Peptide Analogs-----21
John M. Stewart

Structure-Activity Relationships of Opioid Peptides-----42
J. S. Morley and A. S. Dutta

Design Principles: Enkephalins With Predictable Mu/Delta Receptor Specificity-----65
Yasuyuki Shimohigashi

Structure-Activity Relationship and Pharmacology of the Highly Selective -Opioid Agonist, Morphiceptin-----101
Kwen-Jen Chang

Dermorphin: Autonomic Pharmacology and Structure-Activity Relationships-----112
Giora Feuerstein

Design of Conformationally Constrained Cyclic Peptides With High Delta and Mu Opioid Receptor Specificities-----128
Victor J. Hruby

Dehydro and Cyclopropyl Amino Acids and Peptides-----148
Charles H. Stammer

Affinity Labels as Probes for Opioid Receptor Types and Subtypes-----157
Phillip S. Portoghese and A. E. Takemori

Peptide Conformation and Biological Activity: A General Review with Examples of Approaches Relevant to Opioid Peptide Function-----169
Dan W. Urry

Opioid Peptides: Analysis of Specificity and Multiple Binding Modes Through Computer-Aided Drug Design and Structure-Activity Studies-----204
Raoul D. Nelson; David I. Gottlieb; T. M. Balasubramanian; and Garland R. Marshall

Mechanistic Structure-Activity Studies of Peptide and Nonpeptide Flexible Opioids: An Interdisciplinary Approach-----231
Gilda H. Loew; Lawrence Toll; Edward Uyeno; Alice Cheng; Amrit Judd; John Lawson; Christopher Keys; Peter Amsterdam; and Wilma Polgar

Conformations of Opioid Peptides as Determined by Nuclear Magnetic Resonance and Related Spectroscopies-----266
M. Abu Khaled

Conformational Analysis of Opioid Peptides and the Use of Conformational Restriction in the Design of Selective Analogs-----291
Peter W. Schiller

Stereochemically Constrained Enkephalin Analogs Containing X-Aminoisobutyric Acid and 1-Amino-Cyclopentane-l-Carbolylic Acid-----312
Raghuvansh Kishore and Patinabhan Balaram

Enkephalin Conformation in Solution: A Perspective From Vibrational Spectroscopic Studies-----332
V. Renugopalakrishnan; T. W. Collette; L. A. Carreira; and R. S. Rapaka

Conformational Features of the Opioid Peptides in the Solid State: A Review of X-Ray Crystallographic Research-----351
Arthur Camerman and Norman Camerman

The Search for Nonaddicting Strong Analgesics: Hopes and Frustrations-----364
Sydney Archer




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