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在“Elsevier电子期刊”中，命中：14,158条，耗时：0.0549739 秒

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1.A comparison of vasodilation mode among selexipag (NS-304; [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide]), its active metabolite MRE-269 and various prostacyclin receptor agonists in rat, porcine and human pulmonary arteries

作者：Chiaki Fuchikami^a ; ^{c.fuchikami@po.nippon-shinyaku.co.jp} ; Kohji Murakami^a ; Koyuki Tajima^a ; Junko Homan^a ; ^b ; Keiji Kosugi^a ; Kazuya Kuramoto^a ; Michiko Oka^a ; Keiichi Kuwano^b

关键词：Pulmonary arterial hypertension ; NS-304 ; Selexipag ; MRE-269 ; Prostacyclin receptor ; Human

刊名：European Journal of Pharmacology

出版年：2017

2.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

3.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

4.Discovery, structure-activity relationship studies, and anti-nociceptive effects of N-(1,2,3,4-tetrahydro-1-isoquinolinylmethyl)benzamides as novel opioid receptor agonists

作者：Sheng-Ren Chen^a ; ^c ; Yi-Yu Ke^a ; ¹ ; Teng-Kuang Yeh^a ; ¹ ; Shu-Yu Lin^a ; Li-Chin Ou^a ; Shu-Chun Chen^a ; Wan-Ting Chang^a ; Hsiao-Fu Chang^a ; Zih-Huei Wu^a ; Chih-Chien Hsieh^a ; Ping-Yee Law^b ; Horace H. Loh^b ; Chuan Shih^a ; Yiu-Kay Lai^c ; ^{yklai@life.nthu.edu.tw} ; Shiu-Hwa Yeh^a ; ^d ; ^{bau9763@bp.nhri.org.tw} ; Shau-Hua Ueng^a ; ^{shueng@nhri.org.tw}

关键词：μ-opioid receptor agonist ; κ-opioid receptor agonist ; Structure-activity relationship ; Blood-brain barrier ; Penetration ; Anti-nociceptive effects ; Tail-flick test

刊名：European Journal of Medicinal Chemistry

出版年：2017

5.Molecular dynamics simulation of the human estrogen receptor alpha: contribution to the pharmacophore of the agonists

作者：Dessislava Jereva^a ; ^{dessislava.jereva@biomed.bas.bg} ; Filip Fratev^a ; ^b ; ^{fratev@biomed.bas.bg} ; Ivanka Tsakovska^a ; ^{itsakovska@biomed.bas.bg} ; Petko Alov^a ; ^{petko.alov@biophys.bas.bg} ; Tania Pencheva^a ; ^{tania.pencheva@biomed.bas.bg} ; Ilza Pajeva^a ; ^{pajeva@biomed.bas.bg}

关键词：Human estrogen receptor alpha ; Agonist ; Pharmacophore ; Molecular dynamics simulation

刊名：Mathematics and Computers in Simulation

出版年：2017

6.Novel indole-based compounds that differentiate alkylindole-sensitive receptors from cannabinoid receptors and microtubules: Characterization of their activity on glioma cell migration

作者：Susan Fung^a ; ^b ; Cong Xu^a ; Ernest Hamel^c ; James B. Wager-Miller^d ; Grace Woodruff^a ; Aaron Miller^a ; Christina Sanford^a ; Ken Mackie^d ; Nephi Stella^a ; ^e ; ^{nstella@uw.edu}

关键词：2-AG ; arachidonoylglycerol ; AI ; alkylindole ; CB ; cannabinoid ; CB1 ; cannabinoid receptor 1 ; CB2 ; cannabinoid receptor 2 ; CSA4 ; combretastatin A4 ; DBT ; delayed Brain Tumor ; HA ; hemagglutinin ; LPA ; lysophosphatidic acid ; GBM ; glioblastoma multiforme ; SAR ; structure activity relationship ; THC ; tetrahydrocannabinol ; WIN-2 ; WIN55212-2

刊名：Pharmacological Research

出版年：2017

7.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

8.The replacement of the 2-methoxy substituent of N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine improves the selectivity for 5-HT_1A receptor over α₁-adrenoceptor and D₂-like receptor subtypes

作者：Fabio Del Bello^a ; ¹ ; Alessandro Bonifazi^a ; ^b ; ¹ ; Mario Giannella^a ; Gianfabio Giorgioni^a ; Alessandro Piergentili^a ; Riccardo Petrelli^a ; Carlo Cifani^a ; Maria Vittoria Micioni Di Bonaventura^a ; Thomas M. Keck^b ; ^c ; ^d ; Angelica Mazzolari^e ; Giulio Vistoli^e ; Antonio Cilia^f ; Elena Poggesi^f ; Rosanna Matucci^g ; Wilma Quaglia^a ; ^{wilma.quaglia@unicam.it}

关键词：5-HT1A receptor ; α1-Adrenoceptor subtypes ; D2-like receptor subtypes ; Selective 5-HT1A receptor agonists ; Docking studies ; Anxiolytic effect

刊名：European Journal of Medicinal Chemistry

出版年：2017

9.Novel biguanide-based derivatives scouted as TAAR1 agonists: Synthesis, biological evaluation, ADME prediction and molecular docking studies

作者：Michele Tonelli^a ; ^{michele.tonelli@unige.it} ; Stefano Espinoza^b ; Raul R. Gainetdinov^c ; ^d ; Elena Cichero^a ; ^{cichero@unige.it}

关键词：Trace amine-associated receptors (TAARs) ; Murine and human TAAR1 agonists ; Phenyl biguanide derivatives ; Benzyl biguanide derivatives

刊名：European Journal of Medicinal Chemistry

出版年：2017

10.Adenosine A_2A and A_2B Receptors Differentially Modulate Keratinocyte Proliferation: Possible Deregulation in Psoriatic Epidermis

作者：Rosa M. André ; s¹ ; ² ; Marí ; a Carmen Terencio¹ ; ² ; Jorge Arasa¹ ; ² ; Miguel Payá ; ¹ ; ² ; Francisca Valcuende-Cavero³ ; ⁴ ; Pedro Navaló ; n⁵ ; Marí ; a Carmen Montesinos¹ ; ² ; ^{m.carmen.montesinos@uv.es}

关键词：AR ; adenosine receptors ; BAY ; BAY60&ndash ; 6583 ; CGS ; CGS-21680 ; iCa2+ ; intracellular calcium ; MRS ; MRS-1706 ; MTT ; 3-(4 ; 5-dimethylthiazol-2-yl)-2 ; 5-diphenyltetrazolium bromide ; NECA ; 5'-N-ethylcarboxamidoadenosine ; NHEK ; normal human epidermal keratinocyte ; SCH ; SCH-442416 ; TNF ; tumor necrosis factor ; TPA ; 12-O-tetradecanoylphorbol-13-acetate

刊名：Journal of Investigative Dermatology

出版年：2017

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