- S32212, a Novel Serotonin Type 2C Receptor Inverse Agonist/alpha(2)- Adrenoceptor Antagonist and Potential Antidepressant: I. A Mechanistic Characterization
[作者:Millan, MJ; la Cour, CM; Chanrion, B; Dupuis, DS; Di Cara, B; Audinot, V; Cussac, D; Newman-Tancredi, A; Kamal, M; Boutin, JA; Jockers, R; Marin, P; Bockaert, J; Muller, O; Dekeyne, A; Lavielle, G,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:750-764 , 文章类型: Article,,卷期:2012年340-3]
- Although most antidepressants suppress serotonin (5-HT) and/or noradrenaline reuptake, blockade of 5-HT(2C) receptors and alpha(2)-adrenoceptors likewise enhances monoaminergic transmission. These sites are targeted by t...
- Prostaglandin E(2) Promotes Wound-Induced Migration of Intestinal Subepithelial Myofibroblasts via EP2, EP3, and EP4 Prostanoid Receptor Activation
[作者:Iwanaga, K; Okada, M; Murata, T; Hori, M; Ozaki, H,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:604-611 , 文章类型: Article,,卷期:2012年340-3]
- Intestinal subepithelial myofibroblasts (ISMFs) are mesenchymal cells that reside in the subepithelial region throughout the intestine. When the intestine is damaged, the migratory and mitotic responses of ISMFs are cruc...
- Antenatal Phosphodiesterase 4 Inhibition Restores Postnatal Growth and Pulmonary Development in a Model of Chorioamnionitis in Rabbits
[作者:Homer, L; Launay, E; Joram, N; Jacqueline, C; Jarreau, PH; Caillon, J; Moyon, T; Branger, B; Potel, G; Roze, JC; Mehats, C; Gras-LeGuen, C,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:620-628 , 文章类型: Article,,卷期:2012年340-3]
- Chorioamnionitis is implicated in the pathophysiology of bronchopulmonary disease, and the associated inflammatory response is responsible for adverse effects on alveolar development. The aim of this work was to analyze ...
- S32212, a Novel Serotonin Type 2C Receptor Inverse Agonist/alpha(2)-Adrenoceptor Antagonist and Potential Antidepressant: II. A Behavioral, Neurochemical, and Electrophysiological Characterization
[作者:Dekeyne, A; Brocco, M; Loiseau, F; Gobert, A; Rivet, JM; Di Cara, B; Cremers, TI; Flik, G; Fone, KCF; Watson, DJG; Papp, M; Sharp, T; Serres, F; Cespuglio, R; Olivier, B; Chan, JSW; Lavielle, G; Millan, MJ,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:765-780 , 文章类型: Article,,卷期:2012年340-3]
- The present studies characterized the functional profile of N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-1,2-dihydro-3-H-benzo[e]indole-3-carboxamide) (S32212), a combined serotonin (5-HT)(2C) receptor inverse agonist ...
- Characterization of New Stable Ghrelin Analogs with Prolonged Orexigenic Potency
[作者:Maletinska, L; Pychova, M; Holubova, M; Blechova, M; Demianova, Z; Elbert, T; Zelezna, B,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:781-786 , 文章类型: Article,,卷期:2012年340-3]
- Ghrelin, the only known peripherally produced and centrally acting peptide that stimulates food intake, is synthesized primarily in the stomach and acts through the growth hormone secretagogue receptor (GHS-R1a). In addi...
- Prevention of Fibrosis Progression in CCl(4)-Treated Rats: Role of the Hepatic Endocannabinoid and Apelin Systems
[作者:Reichenbach, V; Ros, J; Fernandez-Varo, G; Casals, G; Melgar-Lesmes, P; Campos, T; Makriyannis, A; Morales-Ruiz, M; Jimenez, W,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:629-637 , 文章类型: Article,,卷期:2012年340-3]
- Endocannabinoids behave as antifibrogenic agents by interacting with cannabinoid CB2 receptors, whereas the apelin (AP) system acts as a proangiogenic and profibrogenic mediator in the liver. This study assessed the effe...
- Mitigation of Off-Target Adrenergic Binding and Effects on Cardiovascular Function in the Discovery of Novel Ribosomal S6 Kinase 2 Inhibitors
[作者:Fryer, RM; Muthukumarana, A; Chen, RR; Smith, JD; Mazurek, SN; Harrington, KE; Dinallo, RM; Burke, J; DiCapua, FM; Guo, X; Kirrane, TM; Snow, RJ; Zhang, YL; Soleymanzadeh, F; Madwed, JB; Kashem, MA; Kugler, SZ; O'Neill, MM; Harrison, PC; Reinhart, GA; Boyer, SJ,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:492-500 , 文章类型: Article,,卷期:2012年340-3]
- We previously reported the discovery of a novel ribosomal S6 kinase 2 (RSK2) inhibitor, (R)-5-Methyl-1-oxo-2,3,4,5-tetrahydro-1H-[1,4] diazepino[1,2-a] indole-8-carboxylic acid [1-(3-dimethylamino-propyl)-1H-benzoimidazo...
- LCB 03-0110, a Novel Pan-Discoidin Domain Receptor/c-Src Family Tyrosine Kinase Inhibitor, Suppresses Scar Formation by Inhibiting Fibroblast and Macrophage Activation
[作者:Sun, X; Phan, TN; Jung, SH; Kim, SY; Cho, JU; Lee, H; Woo, SH; Park, TK; Yang, BS,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:510-519 , 文章类型: Article,,卷期:2012年340-3]
- Wound healing generally induces an inflammatory response associated with tissue fibrosis in which activated macrophage and myofibroblast cells are primarily involved. Although this is known to be the underlying mechanism...
- Preclinical Evaluation of an Inhibitor of Cytosolic Phospholipase A(2)alpha for the Treatment of Asthma
[作者:Hewson, CA; Patel, S; Calzetta, L; Campwala, H; Havard, S; Luscombe, E; Clarke, PA; Peachell, PT; Matera, MG; Cazzola, M; Page, C; Abraham, WM; Williams, CM; Clark, JD; Liu, WL; Clarke, NP; Yeadon, M,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:656-665 , 文章类型: Article,,卷期:2012年340-3]
- Asthma is a chronic inflammatory lung disease with considerable unmet medical needs for new and effective therapies. Cytosolic phospholipase A(2)alpha (cPLA(2)alpha) is the rate-limiting enzyme that is ultimately respons...
- Pharmacological Effects of Lu AA21004: A Novel Multimodal Compound for the Treatment of Major Depressive Disorder
[作者:Mork, A; Pehrson, A; Brennum, LT; Nielsen, SM; Zhong, H; Lassen, AB; Miller, S; Westrich, L; Boyle, NJ; Sanchez, C; Fischer, CW; Liebenberg, N; Wegener, G; Bundgaard, C; Hogg, S; Bang-Andersen, B; Stensbol, TB,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:666-675 , 文章类型: Article,,卷期:2012年340-3]
- 1-[2-(2,4-Dimethylphenyl-sulfanyl)-phenyl]-piperazine (Lu AA21004) is a human (h) serotonin (5-HT)(3A) receptor antagonist (K(i) = 3.7 nM), h5-HT(7) receptor antagonist (K(i) = 19 nM), h5-HT(1B) receptor partial agonist ...
- Osteogenic Effects of a Potent Src-over-Abl-Selective Kinase Inhibitor in the Mouse
[作者:Murrills, RJ; Fukayama, S; Boschelli, F; Matteo, JJ; Owens, J; Golas, JM; Patel, D; Lane, G; Liu, YB; Carter, L; Jussif, J; Spaulding, V; Wang, YND; Boschelli, DH; Mckew, JC; Li, XJ; Lockhead, S; Milligan, C; Kharode, YP; Diesl, V; Bai, YC; Follettie, M; Bex, FJ; Komm, B; Bodine, PVN,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:676-687 , 文章类型: Article,,卷期:2012年340-3]
- Src-null mice have higher bone mass because of decreased bone resorption and increased bone formation, whereas Abl-null mice are osteopenic, because of decreased bone formation. Compound I, a potent inhibitor of Src in a...
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