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在“Elsevier电子期刊”中，命中：4,149条，耗时：0.0499768 秒

在所有数据库中总计命中：5,406条

1.Synthesis of novel steroidal agonists, partial agonists, and antagonists for the glucocorticoid receptor

作者：Zhuang Jin^a ; Hua Lin^a ; Sathish Srinivasan^b ; Jerome C. Nwachukwu^b ; Nelson Bruno^b ; Patrick R. Griffin^a ; Kendall W. Nettles^b ; ; Theodore M. Kamenecka^a ; ^{kameneck@scripps.edu}

关键词：AF-1 ; activation function-1 ; AF-2 ; activation function-2 ; AP-1 ; activator protein 1 ; dppp ; 1 ; 3-bis(diphenylphosphino)propane ; DEX ; dexamethasone ; DIEA ; N ; N-diisopropylethylamine ; FKBP5 ; FK506-binding protein 5 ; GR ; glucocorticoid receptor ; GRE ; glucocorticoid-response element ; HATU ; 1-[bis(dimethylamino)methylene]-1H-12 ; 3-triazolo[4 ; 5-b]pyridinium 3-oxid hexafluorophosphate ; IL-6 ; Interleukin-6 ; LBD ; ligand-binding domain ; LPS ; lipopolysaccharide ; MMTV ; mouse mammary tumor virus ; NF-κB ; nuclear

刊名：Bioorganic & Medicinal Chemistry Letters

出版年：2017

2.Development of spiroguanidine-derived α7 neuronal nicotinic receptor partial agonists

作者：Matthew D. Hill ; ^{matthew.hill@bms.com} ; Haiquan Fang ; Sivarao V. Digavalli ; Francine L. Healy ; Lizbeth Gallagher ; Debra Post-Munson ; Ping Chen ; Joanne Natale ; Yulia Benitex ; Daniel Morgan ; Nicholas Lodge ; Linda Bristow ; John E. Macor ; Richard E. Olson

关键词：α7 nicotinic acetylcholine receptor ; Schizophrenia ; 5-HT3A receptor ; Spiroguanidine ; Immediate early genes

刊名：Bioorganic & Medicinal Chemistry Letters

出版年：2017

3.Estimation of the receptor-state affinity constants of ligands in functional studies using wild type and constitutively active mutant receptors: Implications for estimation of agonist bias

作者：Frederick J. Ehlert^a ; ^b ; ^{fjehlert@uci.edu} ; Richard S.L. Stein^b

关键词：Receptor state affinity constants ; Constitutive activity ; Agonist bias ; System bias ; Monod-Wyman-Changeux model ; Observed affinity ; Efficacy ; Receptor activation ; Active state ; Inactive state

刊名：Journal of Pharmacological and Toxicological Methods

出版年：2017

4.From pyrrolidinyl-benzodioxane to pyrrolidinyl-pyridodioxanes, or from unselective antagonism to selective partial agonism at α4β2 nicotinic acetylcholine receptor

作者：Cristiano Bolchi^a ; Francesco Bavo^a ; Cecilia Gotti^b ; Laura Fumagalli^a ; Francesca Fasoli^b ; Matteo Binda^a ; Vanessa Mucchietto^b ; Miriam Sciaccaluga^c ; Simona Plutino^d ; Sergio Fucile^c ; ^d ; Marco Pallavicini^a ; ^{marco.pallavicini@unimi.it}

关键词：α4β2 nAChR ; α3β4 nAChR ; Benzodioxane ; Pyridodioxane ; Partial agonism ; Antagonism

刊名：European Journal of Medicinal Chemistry

出版年：2017

5.Synthesis, biological evaluation and molecular modeling of 1-oxa-4-thiaspiro- and 1,4-dithiaspiro[4.5]decane derivatives as potent and selective 5-HT_1A receptor agonists

作者：Silvia Franchini^a ; Leda Ivanova Manasieva^a ; Claudia Sorbi^a ; Umberto M. Battisti^a ; Paola Fossa^b ; Elena Cichero^b ; Nunzio Denora^c ; Rosa Maria Iacobazzi^c ; ^d ; Antonio Cilia^e ; Lorenza Pirona^e ; Simone Ronsisvalle^f ; Giuseppina Aricò ; ^f ; Livio Brasili^a ; ^{livio.brasili@unimore.it}

关键词：5-HT1A receptor ; Agonist ; Neuroprotection ; BBB penetration ; Analgesic activity

刊名：European Journal of Medicinal Chemistry

出版年：2017

6.Positional isomers of bispyridine benzene derivatives induce efficacy changes on mGlu₅ negative allosteric modulation

作者：Xavier Gó ; mez-Santacana^a ; ^b ; ^c ; ¹ ; James A.R. Dalton^b ; ^d ; Xavier Rovira^e ; ^f ; Jean Philippe Pin^e ; ^f ; Cyril Goudet^e ; ^f ; Pau Gorostiza^c ; ^g ; ^h ; Jesú ; s Giraldo^b ; ^d ; Amadeu Llebaria^a ; ^{amadeu.llebaria@iqac.csic.es}

关键词：mGlu5 ; Isomers ; Partial efficacy ; NAM ; Antagonist ; Inverse agonist

刊名：European Journal of Medicinal Chemistry

出版年：2017

7.New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity

作者：Luca Piemontese^a ; ^b ; Carmen Cerchia^c ; Antonio Laghezza^a ; Pamela Ziccardi^d ; Sabina Sblano^a ; Paolo Tortorella^a ; Vito Iacobazzi^e ; ^f ; Vittoria Infantino^e ; ^g ; Paolo Convertini^e ; ^g ; Fabrizio Dal Piaz^h ; Angelo Lupo^d ; Vittorio Colantuoni^d ; Antonio Lavecchia^c ; ^{antonio.lavecchia@unina.it} ; Fulvio Loiodice^a ; ^{fulvio.loiodice@uniba.it}

关键词：PPAR ; Docking experiments ; Mitochondrial biogenesis ; Anti-proliferative effects ; Gene expression analysis

刊名：European Journal of Medicinal Chemistry

出版年：2017

8.Importance of 5/6-aryl substitution on the pharmacological profile of 4ʹ-((2-propyl-1H-benzo[d]imidazol-1-yl)methyl)-[1,1ʹ-biphenyl]-2-carboxylic acid derived PPARγ agonists

作者：Victoria Obermoser^a ; ¹ ; Robert Mauersberger^a ; ¹ ; Daniela Schuster^a ; Monika Czifersky^a ; Marina Lipova^a ; Monika Siegl^a ; Ulrich Kintscher^b ; Ronald Gust^a ; ^{Ronald.Gust@uibk.ac.at}

关键词：Peroxisome proliferator-activated receptor γ ; Pharmacological profile ; Coactivator recruitment ; Transactivation assay ; Molecular modeling

刊名：European Journal of Medicinal Chemistry

出版年：2017

9.Partial kappa opioid receptor agonist effects in vivo in mice: Biased versus unbiased

作者：Catherine Guariglia ; Amelia Dunn ; Kyle Windisch ; Eduardo Butelman ; Brian Reed ; Mary Jeanne Kreek

刊名：Drug and Alcohol Dependence

出版年：2017

10.Effect of a dopamine D3 receptor partial agonist on cocaine-induced locomotion and self-administration

作者：John Paul Bonadonna¹ ; ; Gregory Powell¹ ; Andrew K. Carlson¹ ; Rachel Mendoza¹ ; Robert H. Mach² ; Robert R. Luedtke³ ; Janet L. Neisewander¹

刊名：Drug and Alcohol Dependence

出版年：2017

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