January 2002 Volume 61 Number 1 ISSN 0026-895X

MOLECULAR PHARMACOLOGY January 2002 Volume 61 Number 1 http://motpharm.aspetjournals.org ISSN 0026-895X

ACCELERATED COMMUNICATIONS Diclofenac Antagonizes Peroxisome Proliferator-Activated Receptor-y Signaling Douglas J. A. Adamson, David Frew, Roger Tatoud, C. Roland Wolf, and Colin N. A. Palmer 7 Diverse Roles of the Nuclear Orphan Receptor CAR in Regulating Hepatic Genes in Response to Phenobarbital Akiko Ueda, Hisham K. Hamadeh, Heather K. Webb, Yukio Yamamoto, Tatsuya Sueyoshi, Cynthia A. Afshari, Jiirgen M. Lehmann, and Masahiko Negishi 1

ARTICLES A Novel Human Nicotinic Receptor Subunit, alO, That Confers Functionality to the a9-Subunit Frederic Sgard, Eric Charpantier, Sonia Bertrand, Nancy Walker, Daniel Caput, David Graham, Daniel fiertrand, and Francois Besnard 150 Potentiation of Human a4/32 Neuronal Nicotinic Acetylcholine Receptor by Estradiol Logos Curtis, Bruno Buisson, Sonia Bertrand, and Daniel Bertrand 127 A Novel Class of Peptides with Facilitating Action on Neuronal Nicotinic Receptors of Rat Chromaffm Cells in Vitro: Functional and Molecular Dynamics Studies Silvia Di Angelantonio, Valeria Costa, Paolo Carloni, Luigi Messori, and Andrea Nistri 43 Loss of Nicotinic Receptors in Monkey Striatum after l-Methyl-4-Phenyl-l,2,3,6-Tetrahydropyridine Treatment Is Due to a Decline in a-Conotoxin Mil Sites Jennifer M. Kulak, J. Michael Mclntosh, and Maryka Quik 230 Molecular Components of Tolerance to Opiates in Single Hippocampal Neurons T. Bushell, T. Endoh, A. A. Simen, D. Ren, V. P. Bindokas, and R. J. Miller 55 Molecular Basis of Differences in (—)(^on.s)-3,4-Dichloro-Ar-methyl-A^-[2-(l-pyrrolidiny)- cyclohexyl]benzeneacetamide-Induced Desensitization and Phosphorylation between Human and Rat K-Opioid Receptors Expressed in Chinese Hamster Ovary Cells Jin Li, Jian-Guo Li, Chongguang Chen, Fengqin Zhang, and Lee-Yuan Liu-Chen 73

Presynaptic H3 Autoreceptors Modulate Histamine Synthesis through cAMP Pathway Jordi Gomez-Ramirez, Jordi Ortiz, and Isaac Blanco 239 Gastrin-Releasing Peptide Mediates Photic Entrainable Signals to Dorsal Subsets of Suprachiasmatic Nucleus via Induction of Period Gene in Mice Reiko Aida, Takahiro Moriya, Miwa Araki, Masashi Akiyama, Keiji Wada, Etsuko Wada, and Shigenobu Shibata

Differences in Signal Transduction of Two 5-HT4 Receptor Splice Variants: Compound Specificity and Dual Coupling with Gas- and Gai/o-Proteins Armelle Pindon, Geert van Hecke, Paul van Gompel, Anne S. Lesage, Josee E. Leysen, and Mirek Jurzak

2+ Allosteric Modulation of j32-Adrenergic Receptor by Zn Gayathri Swaminath, Jacqueline Steenhuis, Brian Kobilka, and Tae Weon Lee 65 Allosteric Site on Muscarinic Acetylcholine Receptors: A Single Amino Acid in Transniembrane Region 7 Is Critical to the Subtype Selectivities of Caracurine V Derivatives and Alkane-Bisammonium Ligands Stefan Buller, Darius Paul Zlotos, Klaus Mohr, and John Ellis 160 Structural Basis of Differences in Isoform-Specific Gating and Lidocaine Block between Cardiac and Skeletal Muscle Sodium Channels Ronald A. Li, Irene L. Ennis, Gordon F. Tomaselli, and Eduardo Marban 136 Inhibition of iV-Methyl-D-aspartate Receptors by Straight-Chain Diols: Implications for the Mechanism of the Alcohol Cutoff Effect Robert W. Peoples and Hong Ren 169 Molecular Basis of Voltage-Dependent Potassium Currents in Porcine Granulosa Cells Diane E. Mason, Kathy E. Mitchell, Yan Li, Melissa R. Finley, and Lisa C. Freeman 201 Defining Minimal Structural Features in Substrates of the H +/Peptide Cotransporter PEPT2 Using Novel Amino Acid and Dipeptide Derivatives Stephan Theis, Bianka Hartrodt, Gabor Kottra, Klaus Neubert, and Hannelore Daniel 214

Molecular Docking of Competitive Phosphodiesterase Inhibitors Orly Dym, Ioannis Xenarios, Hengming Ke, and John Colicelli 20 Soluble Guanylyl Cyclase Activator YC-1 Protects White Matter Axons from Nitric Oxide Toxicity and Metabolic Stress, Probably through Na + Channel Inhibition G. Garthwaite, D. A. Goodwin, S. Neale, D. Riddall, and J. Garthwaite 97

Human Group IIA Secretory Phospholipase A2 Induces Neuronal Cell Death via Apoptosis Tatsurou Yagami, Keiichi Ueda, Kenji Asakura, Satoshi Hata, Takayuki Kuroda, Toshiyuki Sakaeda, Nobuo Takasu, Kazushige Tanaka, Takefumi Gemba, and Yozo Hori 114

Role of Caspase 3-Dependent Bcl-2 Cleavage in Potentiation of Apoptosis by Bcl-2 Ye Liang, Karen D. Nylander, Chaohua Yan, and Nina Felice Schor 142

IKB Kinase Activation Is Involved in Regulation of Paclitaxel-Induced Apoptosis in Human Tumor Cell Lines Yi Huang and Weimin Fan 105

Evidence for Unique Calmodulin-Dependent Nuclear Factor-«B Regulation in WEHI-231 B Cells Stuart D. Shumway, Craig M. Berchtold, Michael N. Gould, and Shigeki Miyamoto 111 Aryl Hydrocarbon Receptor Mediates Sensitivity of MCF-7 Breast Cancer Cells to Antitumor Agent 2- (4-Amino~3-methylphenyl) Benzothiazole Andrea I. Loaiza-Perez, Valentina Trapani, Curtis Hose, Sheo S. Singh, Jane B. Trepel, Malcolm F. G. Stevens, Tracey D. Bradshaw, and Edward A. Sausville 13 Action of (#)-2'-Deoxy-2'-(fluoromethylene)cytidine on DNA Metabolism: Incorporation, Excision, and Cellular Response Yan Zhou, Geetha Achanta, Helene Pelicano, Varsha Gandhi, William Plunkett, and Peng Huang 222 Alternative Mutations at Position 76 of the Vacuolar Transmembrane Protein PfCRT Are Associated with Chloroquine Resistance and Unique Stereospecific Quinine and Quinidine Responses in Plasmodium falciparum Roland A. Cooper, Michael T. Ferdig, Xin-Zhuan Su, Lyann M. B. Ursos, Jianbing Mu, Takashi Nomura, Hisashi Fujioka, David A. Fidock, Paul D. Roepe, and Thomas E. Wellems

35 The a-Glucosidase Inhibitor 1-Deoxynojirimycin Blocks Human Immunodeficiency Virus Envelope Glycoprotein-Mediated Membrane Fusion at the CXCR4 Binding Step Marie-Jeanne Papandreou, Rym Barbouche, Regis Guieu, Marie Paule Kieny, and Emmanuel Fenouillet

186 Contribution of Hepatocyte Nuclear Factor-4 to Down-Regulation of CYP2D6 Gene Expression by Nitric Oxide Hirokazu Hara and Tetsuo Adachi

194 Correction to: "Sorting functions of the individual cytoplasmic domains of the G protein-coupled

vasopressin V2 receptor in Madin Darby canine kidney epithelial cells"

246 Correction to: "Structural mimicry in G protein-coupled receptors: implications of the high-re solution structure of rhodopsin for structure-function analysis of rhodopsin-like receptors"

247 Correction to: "The CYP2D6 humanized mouse: effect of the human CYP2D6 transgene and HNF4a on the disposition of debrisoquine in the mouse" 248