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Human Hallucinogenic Drug Research: Regulatory, Clinical, and Scientific Issues, 146
RESEARCH
MONOGRAPH SERIES
Hallucinogens:
An Update
146
National Institute on Drug Abuse
U.S. Department of Health and Human Services • Public Health Service • National Institutes of Health
340462870.001.png
Hallucinogens: An Update
Editors:
Geraline C. Lin, Ph.D.
National Institute on Drug Abuse
Richard A. Glennon, Ph.D.
Virginia Commonwealth University
NIDA Research Monograph 146
1994
U.S. DEPARTMENT OF HEALTH AND HUMAN SERVICES
Public Health Service
National Institutes of Health
National Institute on Drug Abuse
5600 Fishers Lane
Rockville, MD 20857
ACKNOWLEDGEMENT
This monograph is based on the papers from a technical review on
“Hallucinogens: An Update” held on July 13-14, 1992. The review meeting
was sponsored by the National Institute on Drug Abuse.
COPYRIGHT STATUS
The National Institute on Drug Abuse has obtained permission from the
copyright holders to reproduce certain previously published material as
noted in the text. Further reproduction of this copyrighted material is
permitted only as part of a reprinting of the entire publication or chapter.
For any other use, the copyright holder’s permission is required. All other
material in this volume except quoted passages from copyrighted sources is
in the public domain and may be used or reproduced without permission
from the Institute or the authors. Citation of the source is appreciated.
Opinions expressed in this volume are those of the authors and do not
necessarily reflect the opinions or official policy of the National Institute on
Drug Abuse or any other part of the U.S. Department of Health and Human
Services.
The U.S. Government does not endorse or favor any specific commercial
product or company. Trade, proprietary, or company names appearing in
this publication are used only because they are considered essential in the
context of the studies reported herein.
National Institute on Drug Abuse
NIH Publication No. 94-3872
Printed 1994
NIDA Research Monographs are indexed in the Index Medicus. They are
selectively included in the coverage of American Statistics Index, Biosciences
information Service, Chemical Abstracts, Current Contents, Psychological
Abstracts, and Psychopharmacology Abstracts.
ii
Contents
Preface
Geraline C. Lin . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 1
Classical Hallucinogens: An Introductory Overview
Richard A. Glennon . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 4
Are Hallucinogens Psychoheuristic?
Stephen Szára . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 33
Lysergamides Revisited
Robert C. Pfaff, Xuemei Huang, Danuta Marona-Lewicka, Robert
Oberlender, and David E. Nichols . . . . . . . . . . . . . . . . . . . . . . . . . 52
Structure-Activity Relationships of Classic Hallucinogens and their
Analogs
Peyton Jacob III and Alexander T. Shulgin . . . . . . . . . . . . . . . . . . 74
Human Hallucinogenic Drug Research: Regulatory, Clinical, and
Scientific Issues
Rick J. Strassman . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 92
Serotonin Receptor Involvement in an Animal Model of the Acute
Effects of Hallucinogens
Mark A. Geyer and Kirsten M. Krebs . . . . . . . . . . . . . . . . . . . . . 124
The Stimulus Effects of Serotonergic Hallucinogens in Animals
Jerrold C. Winter . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 157
Electrophysiological Studies on the Actions of Hallucinogenic
Drugs at 5-HT 2 Receptors in Rat Brain
George K. Aghajanian . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 183
Neurochemical Evidence That Hallucinogenic Drugs Are 5-HT 1C
Receptor Agonists: What Next?
Elaine Sanders-Bush . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 203
Autoradiographic Approaches to Studying Hallucinogens or
Other Drugs
Nathan M. Appel . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 214
iii
Hallucinogens Acting at 5-HT Receptors: Towards a Mechanistic
Understanding at Atomic Resolution
Harel Weinstein, Daqun Zhang, and Juan A. Ballesteros . . . . . . 241
Molecular Modeling of the Interaction of LSD and Other
Hallucinogens with 5-HT 2 Receptors
Richard B. Westkaemper and Richard A. Glennon . . . . . . . . . . . 263
Structure and Function of Serotonin 5-HT 2 Receptors
Jean C. Shih, Kevin Chen, and Timothy K. Gallaher . . . . . . . . . 284
Summary
Richard A. Glennon . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 298
iv

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