The AAPS Journal - Themed Issue

Frontiers in Science: Drug Addiction — From Basic Research to Therapies
Guest Editors: Rao S. Rapaka and Wolfgang Sadée

Table of Contents

Editorial: Theme Issue “Drug Addiction — From Basic Research to Therapies”
Rao S. Rapaka and Wolfgang Sadée

Volume 1. General Topics: Neurochemistry and Neurobiology of Drugs of Abuse

DARPP-32 Mediates the Actions of Multiple Drugs of Abuse
Per Svenningsson, Angus C. Nairn, and Paul Greengard

Drug Discovery From Natural Sources
Young-Won Chin, Marcy J. Balunas, Hee Byung Chai, and A. Douglas Kinghorn

Computational Methods in Drug Design: Modeling G Protein-Coupled Receptor Monomers, Dimers, and Oligomers
Patricia H. Reggio

Symbiotic Relationship of Pharmacogenetics and Drugs of Abuse
Joni L. Rutter

Monoclonal Antibody Form and Function: Manufacturing the Right Antibodies for Treating Drug Abuse
Eric Peterson, S. Michael Owens, and Ralph L. Henry

Cocaine- and Amphetamine-Regulated Transcript Peptides Play a Role in Drug Abuse and Are Potential Therapeutic Targets
Michael J. Kuhar, Jason N. Jaworski, George W. Hubert, Kelly B. Philpot, and Geraldina Dominguez

Selectivity and Potency of Cyclin-dependent Kinase Inhibitors
Jayalakshmi Sridhar, Nagaraju Akula, and Nagarajan Pattabiraman

RNAi-directed Inhibition of DC-SIGN by Dendritic Cells: Prospects for HIV-1 Therapy
Madhavan P.N. Nair, Jessica L. Reynolds, Supriya D. Mahajan, Stanley A. Schwartz, Ravikumar Aalinkeel, B. Bindukumar, and Don Sykes

Ophthalmic Drug Design Based on the Metabolic Activity of the Eye: Soft Drugs and Chemical Delivery Systems
Nicholas Bodor and Peter Buchwald

Viewing Chemokines as a Third Major System of Communication in the Brain
Martin W. Adler, Ellen B. Geller, Xiaohong Chen, and Thomas J. Rogers

Mutant Glycosyltransferases Assist in the Development of a Targeted Drug Delivery System and Contrast Agents for MRI
Pradman K. Qasba, Boopathy Ramakrishnan, and Elizabeth Boeggeman

Targeting the PDZ Domains of Molecular Scaffolds of Transmembrane Ion Channels
Andrea Piserchio, Mark Spaller, and Dale F. Mierke

Searching for Polymorphisms That Affect Gene Expression and mRNA Processing: Example ABCB1 (MDR1)
Danxin Wang and Wolfgang Sadée

Modulating Inhibitory Ligand-Gated Ion Channels
Michael Cascio

Multiple Molecular Targets in Cancer Chemoprevention by Curcumin
Rajesh L. Thangapazham, Anuj Sharma, and Radha K. Maheshwari

Volume 2. Transporters, Stimulants & Hallucinogens

Role of Monoamine Transporters in Mediating Psychostimulant Effects
Evan L. Riddle, Annette E. Fleckenstein, and Glen R. Hanson

Development of the Dopamine Transporter Selective RTI-336 as a Pharmacotherapy for Cocaine Abuse
F. Ivy Carroll, James L. Howard, Leonard L. Howell, Barbara S. Fox, and Michael J. Kuhar

Serotonin Transporters: Implications for Antidepressant Drug Development
Kellie J. White, Crystal C. Walline, and Eric L. Barker

Recent Advances for the Treatment of Cocaine Abuse: Central Nervous System Immunopharmacotherapy
Tobin J. Dickerson and Kim D. Janda

κ Opioids as Potential Treatments for Stimulant Dependence
Thomas E. Prisinzano, Kevin Tidgewell, and Wayne W. Harding

Regulation of Monoamine Transporters: Influence of Psychostimulants and Therapeutic Antidepressants
Lankupalle D. Jayanthi and Sammanda Ramamoorthy

Hallucinogen Actions on 5-HT Receptors Reveal Distinct Mechanisms of Activation and Signaling by G Protein-coupled Receptors
Harel Weinstein

Recognition of Psychostimulants, Antidepressants, and Other Inhibitors of Synaptic Neurotransmitter Uptake by the Plasma Membrane Monoamine Transporters
Christopher K. Surratt, Okechukwu T. Ukairo, and Suneetha Ramanujapuram

Transport Systems for Opioid Peptides in Mammalian Tissues
Vadivel Ganapathy and Seiji Miyauchi

Receptors of Mammalian Trace Amines
Anita H. Lewin

Dual Dopamine/Serotonin Releasers as Potential Medications for Stimulant and Alcohol Addictions
Richard B. Rothman, Bruce E. Blough, and Michael H. Baumann

Volume 3. Drug Design: Nicotine, Opioids and Related Ligands

The Role of Crystallography in Drug Design
Jeffrey R. Deschamps

Opioid Peptide-Derived Analgesics
Peter W. Schiller

Opioid Ligands With Mixed μ/δ Opioid Receptor Interactions: An Emerging Approach to Novel Analgesics
Subramaniam Ananthan

Small-Molecule Agonists and Antagonists of the Opioid Receptor-Like Receptor (ORL1, NOP): Ligand-Based Analysis of Structural Factors Influencing Intrinsic Activity at NOP
Nurulain Zaveri, Faming Jiang, Cris Olsen, Willma Polgar, and Lawrence Toll

Kappa Opioid Antagonists: Past Successes and Future Prospects
Matthew D. Metcalf and Andrew Coop

In Vitro and Direct In Vivo Testing of Mixture-Based Combinatorial Libraries for the Identification of Highly Active and Specific Opiate Ligands
Richard A. Houghten, Colette T. Dooley, and Jon R. Appel

Neuronal Nicotinic Acetylcholine Receptor Expression and Function on Nonneuronal Cells
Lorise C. Gahring and Scott W. Rogers

Current Status of Immunologic Approaches to Treating Tobacco Dependence: Vaccines and Nicotine-specific Antibodies
Mark G. LeSage, Daniel E. Keyler, and Paul R. Pentel

A General Procedure for the Enantioselective Synthesis of the Minor Tobacco Alkaloids Nornicotine, Anabasine, and Anatabine
Joshua T. Ayers, Rui Xu, Linda P. Dwoskin, and Peter A. Crooks

Molecular Modeling of mono- and bis-Quaternary Ammonium Salts as Ligands at the α4β2* Nicotinic Acetylcholine Receptor Subtype Using Nonlinear Techniques
Joshua T. Ayers, Aaron Clauset, Jeffrey D. Schmitt, Linda P. Dwoskin, and Peter A. Crooks

Introduction of Unsaturation into the N-n-Alkyl Chain of the Nicotinic Receptor Antagonists, NONI and NDNI: Effect on Affinity and Selectivity
Sangeetha P. Sumithran, Peter A. Crooks, Rui Xu, Jun Zhu, Agripina G. Deaciuc, Lincoln H. Wilkins, and Linda P. Dwoskin

N-n-Alkylnicotinium Analogs, a Novel Class of Antagonists at α4β2* Nicotinic Acetylcholine Receptors: Inhibition of S(-)-Nicotine-Evoked 86Rb+ Efflux from Rat Thalamic Synaptosomes
Lincoln H. Wilkins, Jr, Dennis K. Miller, Joshua T. Ayers, Peter A. Crooks, and Linda P. Dwoskin

New Paradigms and Tools in Drug Design for Pain and Addiction
Victor J. Hruby, Frank Porreca, Henry I. Yamamura, Gordon Tollin, Richard S. Agnes, Yeon Sun Lee, Minying Cai, Isabel Alves, Scott Cowell, Eva Varga, Peg Davis, Zdzislaw Salamon, William Roeske, Todd Vanderah, and Josephine Lai

Volume 4. Opioids: Neurochemistry and Neurobiology

Neuropeptide-Processing Enzymes: Applications for Drug Discovery
Lloyd D. Fricker

CNS Drug Delivery: Opioid Peptides and the Blood-Brain Barrier
Ken A. Witt and Thomas P. Davis

Cell-permeable, Mitochondrial-targeted, Peptide Antioxidants
Hazel H. Szeto

Targeting Opioid Receptor Heterodimers: Strategies for Screening and Drug Development
Achla Gupta, Fabien M. Décaillot, and Lakshmi A. Devi

Homology Modeling of Opioid Receptor-Ligand Complexes Using Experimental Constraints
Irina D. Pogozheva, Magdalena J. Przydzial, and Henry I. Mosberg

Molecular Recognition of Opioid Receptor Ligands
Brian E. Kane, Bengt Svensson, and David M. Ferguson

Role of Morphine’s Metabolites in Analgesia: Concepts and Controversies
Erica Wittwer and Steven E. Kern

Mu Opioid Receptor Regulation And Opiate Responsiveness
Kirsten M. Raehal and Laura M. Bohn

Agmatine: Biological Role and Therapeutic Potentials in Morphine Analgesia and Dependence
Soundar Regunathan

Modulation of Microglial Pro-inflammatory and Neurotoxic Activity for the Treatment of Parkinson's Disease
Bin Liu

Volume 5. Cannabinoids

The Therapeutic Potential of Drugs That Target Cannabinoid Receptors or Modulate the Tissue Levels or Actions of Endocannabinoids
Roger G. Pertwee

Further Advances in the Synthesis of Endocannabinoid-related Ligands
Anu Mahadevan and Raj K. Razdan

Ajulemic Acid (IP-751): Synthesis, Proof of Principle, Toxicity Studies, and Clinical Trials
Sumner Burstein

Conformational Characteristics of the Interaction of SR141716A with the CB1 Cannabinoid Receptor as Determined through the use of Conformationally-Constrained Analogs
Brian F. Thomas, Yanan Zhang, Marcus Brakeen, Kevin M. Page, S. Wayne Mascarella and Herbert H. Seltzman

Activation of G-proteins in Brain by Endogenous and Exogenous Cannabinoids
Steven R. Childers

2-Arachidonoylglycerol (2-AG) Membrane Transport: History and Outlook
Anita Hermann, Martin Kaczocha, and Dale G. Deutsch

Endocannabinoid Mechanisms of Pain Modulation
Andrea G. Hohmann and Richard L. Suplita, II