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PERSPECTIVES
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4333-4353
| Therapeutic Opportunities for Muscarinic Receptors in the Central Nervous System
Christian C. Felder,
Frank P. Bymaster,
John Ward, and
Neil DeLapp
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4354-4358
Biarylpropylsulfonamides as Novel, Potent Potentiators of 2-Amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic Acid (AMPA) Receptors
Paul L. Ornstein,
Dennis M. Zimmerman,
M. Brian Arnold,
Thomas J. Bleisch,
Buddy Cantrell,
Richard Simon,
Hamideh Zarrinmayeh,
S. Richard Baker,
Mary Gates,
Joseph P. Tizzano, and
David Bleakman
, Allan Mandelzys,
Kieth R. Jarvie,
Ken Ho,
Michelle Deverill, and
Rajender K. Kamboj
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4359-4362
Design, Radiosynthesis, and Biodistribution of a New Potent and Selective Ligand for in Vivo Imaging of the Adenosine A2A Receptor System Using Positron Emission Tomography
Sergio Todde,
Rosa Maria Moresco,
Pasquale Simonelli,
Pier Giovanni Baraldi,
Barbara Cacciari,
Giampiero Spalluto,
Katia Varani,
Angela Monopoli,
Mario Matarrese,
Assunta Carpinelli,
Fulvio Magni,
Marzia Galli Kienle, and
Ferruccio Fazio
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4363-4366
5-[1'-(2'-N-Arylsulfonyl-1',2',3',4'-tetrahydroisoquinolyl)]-4,5-dihydro-2(3H)-furanones: Positive Allosteric Modulators of the GABAA Receptor with a New Mode of Action
Rodolphe Razet,
Urs Thomet,
Roman Furtmüller,
Angèle Chiaroni,
Erwin Sigel,
Werner Sieghart, and
Robert H. Dodd
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4367-4369
Increased DNA Binding Specificity for Antitumor Ecteinascidin 743 through Protein-DNA Interactions?
Raquel García-Nieto,
Ignacio Manzanares,
Carmen Cuevas, and
Federico Gago
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EXPEDITED ARTICLES
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4370-4376
Structure-Function Studies on the New Growth Hormone-Releasing Peptide, Ghrelin: Minimal Sequence of Ghrelin Necessary for Activation of Growth Hormone Secretagogue Receptor 1a
Maria A. Bednarek,
Scott D. Feighner,
Sheng-Shung Pong,
Karen Kulju McKee,
Donna L. Hreniuk,
Maria V. Silva,
Vivien A. Warren,
Andrew D. Howard,
Lex H. Y. Van der Ploeg, and
James V. Heck
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4377-4387
Reduction-Sensitive Lipopolyamines as a Novel Nonviral Gene Delivery System for Modulated Release of DNA with Improved Transgene Expression
Gerardo Byk,
Barbara Wetzer,
Marc Frederic,
Catherine Dubertret,
Bruno Pitard,
Gabrielle Jaslin, and
Daniel Scherman
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ARTICLES
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4388-4397
Novel Design of Nonpeptide AVP V2 Receptor Agonists: Structural Requirements for an Agonist Having 1-(4-Aminobenzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepine as a Template
Kazumi Kondo,
Hidenori Ogawa,
Tomoichi Shinohara,
Muneaki Kurimura,
Yoshihisa Tanada,
Keizo Kan,
Hiroshi Yamashita,
Shigeki Nakamura,
Takahiro Hirano,
Yoshitaka Yamamura,
Toyoki Mori,
Michiaki Tominaga, and
Akiko Itai
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4398-4415
Design, Synthesis, and Biological Evaluation of Potent and Selective Amidino Bicyclic Factor Xa Inhibitors
Qi Han,
Celia Dominguez,
Pieter F. W. Stouten,
Jeongsook M. Park,
Daniel E. Duffy,
Robert A. Galemmo, Jr.,
Karen A. Rossi,
Richard S. Alexander,
Angela M. Smallwood,
Pancras C. Wong,
Matthew M. Wright,
Joseph M. Luettgen,
Robert M. Knabb, and
Ruth R. Wexler
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4416-4427
Multiple-Conformation and Protonation-State Representation in 4D-QSAR: The Neurokinin-1 Receptor System
Angelo Vedani,
Hans Briem,
Max Dobler,
Horst Dollinger, and
Daniel R. McMasters
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4428-4436
Chiral Resolution, Pharmacological Characterization, and Receptor Docking of the Noncompetitive mGlu1 Receptor Antagonist (±)-2-Hydroxyimino- 1a,2-dihydro-1H-7-oxacyclopropa[b]naphthalene-7a-carboxylic Acid Ethyl Ester
David Ott,
Philipp Floersheim,
Werner Inderbitzin,
Natacha Stoehr,
Eric Francotte,
Gabrielle Lecis,
Paul Richert,
Grety Rihs,
Peter Josef Flor,
Rainer Kuhn, and
Fabrizio Gasparini
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4437-4445
Synthesis and Evaluation of 17-Aliphatic Heterocycle-Substituted Steroidal Inhibitors of 17 -Hydroxylase/C17-20-Lyase (P450 17)
Rolf W. Hartmann,
Markus Hector,
Bertil G. Wachall,
Anja Palusczak,
Martina Palzer,
Volker Huch, and
Michael Veith
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4446-4451
Computational Studies on HIV-1 Protease Inhibitors: Influence of Calculated Inhibitor-Enzyme Binding Affinities on the Statistical Quality of 3D-QSAR CoMFA Models
Philippa R. N. Jayatilleke,
Anil C. Nair,
Randy Zauhar, and
William J. Welsh
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4452-4464
Design and Synthesis of Pyrrolidine-5,5-trans-lactams (5-Oxo-hexahydro-pyrrolo[3,2-b]pyrroles) as Novel Mechanism-Based Inhibitors of Human Cytomegalovirus Protease. 1. The -Methyl-trans-lactam Template
Alan D. Borthwick,
S. Jane Angier,
Andrew J. Crame,
Anne M. Exall,
Terry M. Haley,
Graham J. Hart,
Andrew M. Mason,
Andrew M. K. Pennell, and
Gordon G. Weingarten
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4465-4478
Structure-Activity Relationships of 17 -Derivatives of Estradiol as Inhibitors of Steroid Sulfatase
Roch P. Boivin,
Van Luu-The,
Roger Lachance,
Fernand Labrie, and
Donald Poirier
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4479-4487
6-Alkylamino- and 2,3-Dihydro-3'-methoxy-2-phenyl-4-quinazolinones and Related Compounds: Their Synthesis, Cytotoxicity, and Inhibition of Tubulin Polymerization
Mann-Jen Hour,
Li-Jiau Huang,
Sheng-Chu Kuo,
Yi Xia,
Kenneth Bastow,
Yuka Nakanishi,
Ernest Hamel, and
Kuo-Hsiung Lee
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4488-4498
A Selenopyrylium Photosensitizer for Photodynamic Therapy Related in Structure to the Antitumor Agent AA1 with Potent in Vivo Activity and No Long-Term Skin Photosensitization
Kristi A. Leonard,
Jonathan P. Hall,
Marina I. Nelen,
Sherry R. Davies,
Sandra O. Gollnick,
Sue Camacho,
Allan R. Oseroff,
Scott L. Gibson,
Russell Hilf, and
Michael R. Detty
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4499-4507
Molecular Simplification of 1,4-Diazabicyclo[4.3.0]nonan-9-ones Gives Piperazine Derivatives That Maintain High Nootropic Activity
Dina Manetti,
Carla Ghelardini,
Alessandro Bartolini,
Silvia Dei,
Nicoletta Galeotti,
Fulvio Gualtieri,
Maria Novella Romanelli, and
Elisabetta Teodori
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4508-4515
Exploring the Structural Basis of Neurotoxicity in C17-Polyacetylenes Isolated from Water Hemlock
Koji Uwai,
Katsuyo Ohashi,
Yoshiaki Takaya,
Tomihisa Ohta,
Takeshi Tadano,
Kensuke Kisara,
Koichi Shibusawa,
Ryoji Sakakibara, and
Yoshiteru Oshima
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4516-4525
Syntheses of 4'-C-Ethynyl- -D-arabino- and 4'-C-Ethynyl-2'-deoxy- -D-ribo-pentofuranosylpyrimidines and -purines and Evaluation of Their Anti-HIV Activity
Hiroshi Ohrui,
Satoru Kohgo,
Kenji Kitano,
Shinji Sakata,
Eiichi Kodama,
Kazuhisa Yoshimura,
Masao Matsuoka,
Shiro Shigeta, and
Hiroaki Mitsuya
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4526-4533
Solid-Phase Synthesis and Biological Evaluation of a Combinatorial Library of Philanthotoxin Analogues
Kristian Str mgaard,
Tim J. Brier,
Kim Andersen,
Ian R. Mellor,
Alex Saghyan,
Denis Tikhonov,
Peter N. R. Usherwood,
Povl Krogsgaard-Larsen, and
Jerzy W. Jaroszewski
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4534-4541
Classification of Multidrug-Resistance Reversal Agents Using Structure-Based Descriptors and Linear Discriminant Analysis
Gregory A. Bakken and
Peter C. Jurs
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4542-4551
Carbonic Anhydrase Inhibitors: Perfluoroalkyl/Aryl-Substituted Derivatives of Aromatic/Heterocyclic Sulfonamides as Topical Intraocular Pressure-Lowering Agents with Prolonged Duration of Action
Andrea Scozzafava,
Luca Menabuoni,
Francesco Mincione,
Fabrizio Briganti,
Giovanna Mincione, and
Claudiu T. Supuran
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4552-4562
Synthesis, 18F-Labeling, and Biological Evaluation of Piperidyl and Pyrrolidyl Benzilates as in Vivo Ligands for Muscarinic Acetylcholine Receptors
Marc B. Skaddan,
Michael R. Kilbourn,
Scott E. Snyder,
Phil S. Sherman,
Tim J. Desmond, and
Kirk A. Frey
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BRIEF ARTICLES
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4563-4569
Cyanoindole Derivatives as Highly Selective Dopamine D4 Receptor Partial Agonists: Solid-Phase Synthesis, Binding Assays, and Functional Experiments
Harald Hübner,
Johannes Kraxner, and
Peter Gmeiner
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4570-4574
S-Acyl-2-thioethyl Aryl Phosphotriester Derivatives as Mononucleotide Prodrugs
Nathalie Schlienger,
Suzanne Peyrottes,
Tarek Kassem,
Jean-Louis Imbach,
Gilles Gosselin,
Anne-Marie Aubertin, and
Christian Périgaud
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