Discovery of potent beta-secretase (bace-1) inhibitors by the synthesis of isophthalamide-containing hybrids.

abstract：AIM:To investigate the effects of angiotensin II (Ang II) on corticotropin-releasing hormone (CRH) and argipressin (AVP) release from median eminence (ME) of hypothalamus during acute hypoxia in rats. METHODS:Simulated hypoxia was performed in a hypobaric chamber. CRH and AVP were determined by radioimmunoassay (RIA)....

journal_title：Acta pharmacologica Sinica

authors： Wu Y,Du JZ

更新日期：2000-11-01 00:00:00

abstract：AIM:To investigate the effects and underlying mechanisms of 118, a novel derivative of mycophenolic acid, in a murine allogeneic skin graft model. METHODS:Skin grafts were conducted by grafting BALB/c donor tail skin into C57BL/6 skin beds (allograft) or by grafting female C57BL/6 donor tail skin into female C57BL/6 s...

journal_title：Acta pharmacologica Sinica

authors： Kong FY,Chen W,He SJ,Lin ZM,Li X,Zhang XH,Yang XQ,Zhu FH,Tong XK,Zhou Y,Tang W,Duan WH,Zuo JP

更新日期：2013-07-01 00:00:00

abstract：:JFCR39 is an informatic anticancer drug discovery system that utilizes a panel of 39 human cancer cells coupled with a drug-activity database. This system not only provides disease-oriented information but can also predict the mechanism of action of a given antitumor agent. Development of a phosphatidylinositol 3-kina...

journal_title：Acta pharmacologica Sinica

authors： Kong DX,Yamori T

更新日期：2010-09-01 00:00:00

abstract：AIM:Filamin binding LIM protein 1, also known as migfilin, is a skeleton organization protein that binds to mitogen-inducible gene 2 at cell-extracellular matrix adhesions. The aim of this study was to investigate the role of migfilin in cisplatin-induced apoptosis in human glioma cells, to determine the functional dom...

journal_title：Acta pharmacologica Sinica

authors： Fan J,Ou YW,Wu CY,Yu CJ,Song YM,Zhan QM

更新日期：2012-10-01 00:00:00

abstract：AIM:The role of caveolin-1 (Cav-1) in angiogenesis remains poorly understood. The endothelial nitric oxide (NO) synthase (eNOS), a caveolin-interacting protein, was demonstrated to play a predominant role in vascular endothelial growth factor (VEGF) -induced angiogenesis. The purpose of our study was to examine the rol...

journal_title：Acta pharmacologica Sinica

authors： Pan YM,Yao YZ,Zhu ZH,Sun XT,Qiu YD,Ding YT

更新日期：2006-12-01 00:00:00

abstract：AIM:To investigate the ability of an antisense RNA eukaryotic expression plasmid pcDNA3.1/survivin in down-regulating the expression level of survivin mRNA and survivin protein and reversed multidrug resistance (MDR) in adriamycin-resistant HL-60/ADR cell line. METHODS:The expression of survivin mRNA was measured by R...

journal_title：Acta pharmacologica Sinica

authors： Wang L,Zhang GM,Feng ZH

更新日期：2003-12-01 00:00:00

abstract：AIM:In order to elucidate the molecular mechanism underlying the cardioprotection afforded by schisandrin B (Sch B), the effect of Sch B treatment on the sensitivity of mitochondria to Ca2+-stimulated permeability transition (PT) was investigated in rat hearts under normal and ischemia-reperfusion (I-R) conditions. RE...

journal_title：Acta pharmacologica Sinica

authors： Chiu PY,Leung HY,Siu AH,Poon MK,Ko KM

更新日期：2007-10-01 00:00:00

abstract：:Hydrogen sulfide (H2S), which is well known traditionally as a toxic gas, has been proven to be produced endogenously by 3 enzymes in mammalian tissues and plays important roles in physiological and pathophysiological conditions. In the central nervous system, H2S functions as not only a neuromodulator, but also a neu...

journal_title：Acta pharmacologica Sinica

authors： Chen CQ,Xin H,Zhu YZ

更新日期：2007-11-01 00:00:00

abstract：AIM:alpha2 nAChR subunit mRNA expression in mice is most intense in the olfactory bulbs and interpeduncular nucleus. We aimed to investigate the properties of alpha2* nAChRs in these mouse brain regions. METHODS:alpha2 nAChR subunit-null mutant mice were engineered. Pharmacological and immunoprecipitation studies were...

journal_title：Acta pharmacologica Sinica

authors： Whiteaker P,Wilking JA,Brown RW,Brennan RJ,Collins AC,Lindstrom JM,Boulter J

更新日期：2009-06-01 00:00:00

abstract：AIM:To investigate the effects of different muscarinic receptor (M) subtypes in the spinal cord on the scores of naloxone-precipitated morphine-withdrawal symptoms and the changes of nNOS expression in locus coeruleus (LC). METHODS:nNOS immunohistochemistry, intrathecal injection (it), and antisense oligonucleotides (...

journal_title：Acta pharmacologica Sinica

authors： Chou WB,Zeng YM,Duan SM,Zhou WH,Gu J,Yang GD

更新日期：2002-08-01 00:00:00

abstract：AIM:To examine the role of cholinergic neurons in the nucleus raphe magnus (NRM) in noxious heat stimulation and in the effects of morphine-induced antinociception by rats. METHODS:After the cholinergic neuron selective toxin, AF64A, was microinjected into the NRM, we examined changes in the antinociceptive threshold ...

journal_title：Acta pharmacologica Sinica

authors： Abe K,Ishida K,Kato M,Shigenaga T,Taguchi K,Miyatake T

更新日期：2002-11-01 00:00:00

abstract：:Conjugated polymer nanomaterials (CPNs), as optically and electronically active materials, hold promise for biomedical imaging and drug delivery applications. This review highlights the recent advances in the utilization of CPNs in theranostics. Specifically, CPN-based in vivo imaging techniques, including near-infrar...

journal_title：Acta pharmacologica Sinica

authors： Qian CG,Chen YL,Feng PJ,Xiao XZ,Dong M,Yu JC,Hu QY,Shen QD,Gu Z

更新日期：2017-06-01 00:00:00

abstract：AIM:To study in vitro release and in vivo effect of four different types of sustained-release naltrexone microspheres on morphine analgesia. METHODS:Release of naltrexone from four types of biodegradable microspheres was investigated by HPLC. Their antagonist effects on morphine analgesia were observed using mouse hot...

journal_title：Acta pharmacologica Sinica

authors： He GA,Hou HM,Liu XJ

更新日期：2001-06-01 00:00:00

abstract：AIM:To investigate effects of CpG oligodeoxynucleotide (CpG ODN) on the mRNA expression of transcription factors GATA binding protein 3 (GATA-3) and T-box expressed in T cells (T-bet) in asthmatic mice. METHODS:An asthmatic mouse model was established and treated with CpG ODN. Total inflammatory cells and eosinophils ...

journal_title：Acta pharmacologica Sinica

authors： Wu ZQ,Xu YP,Xiang H,Shen HH

更新日期：2005-09-01 00:00:00

abstract：AIM:Oral risedronate is effective in the treatment of postmenopausal osteoporosis when administered daily, weekly, or monthly. In this 1-year, randomized, double-blind, multicenter study we compared the weekly 35-mg and daily 5-mg risedronate dosing regimens in the treatment of Chinese postmenopausal women with osteopo...

journal_title：Acta pharmacologica Sinica

authors： Gu JM,Wang L,Lin H,Chen DC,Tang H,Jin XL,Xia WB,Hu YQ,Fu WZ,He JW,Zhang H,Wang C,Yue H,Hu WW,Liu YJ,Zhang ZL

更新日期：2015-07-01 00:00:00

abstract：AIM:Apolipoprotein E (ApoE) plays an important role in the transport and metabolism of lipids. Recent studies show that bone mass is increased in young apoE(-/-) mice. In this study we investigated the bone phenotype and metabolism in aged apoE(-/-) mice. METHODS:Femurs and tibias were collected from 18- and 72-week-o...

journal_title：Acta pharmacologica Sinica

authors： Hong W,Xu XY,Qiu ZH,Gao JJ,Wei ZY,Zhen L,Zhang XL,Ye ZB

更新日期：2015-12-01 00:00:00

abstract：AIM:To investigate the effect of incorporation of an isoleucine zipper (IZ) motif into CD40 on binding activity of CD40 for the CD40 ligand (CD40L). METHODS:Prokaryotic expression vectors for 2 soluble CD40 derivatives, shCD40His and shCD40IZ containing an IZ domain, were constructed and expressed in Escherichia coli....

journal_title：Acta pharmacologica Sinica

authors： He XH,Xu LH,Liu Y

更新日期：2006-03-01 00:00:00

abstract：AIM:To study the effect of semi-synthesized quercetin water-soluble derivatives sodium quercetin-7-sulfate (SQMS) and disodium quercetin-7,4 -disulfate (SQDS) on recombinant human phosphatidylinositol 3-kinase (PI3-K) p110 beta catalytic subunit. METHODS:Recombinant human PI3-K p110 beta catalytic subunit was expresse...

journal_title：Acta pharmacologica Sinica

authors： Liu W,Liang NC

更新日期：2002-04-01 00:00:00

abstract：AIM:Osteopontin (OPN), a multifunctional protein, has been reported to be protoxicant in acetaminophen hepatotoxicity. In this study, the mechanisms underlying the detrimental role of OPN in acetaminophen toxicity were explored. METHODS:Male C57BL/6 (wild-type, WT) and OPN(-/-) mice were administered with acetaminophe...

journal_title：Acta pharmacologica Sinica

authors： He CY,Liang BB,Fan XY,Cao L,Chen R,Guo YJ,Zhao J

更新日期：2012-08-01 00:00:00

abstract：AIM:To investigate the inhibitory effect of the natural product Leukamenin F on liver fibrosis and explore its potential underlying mechanisms. METHODS:Carbon tetrachloride (CCl(4))-treated mouse model in vivo and in hepatic stellate cells (HSC) in vitro were used. The effect on CCl(4)-induced liver fibrosis was studi...

journal_title：Acta pharmacologica Sinica

authors： Liu Q,Wang X,Zhang Y,Li CJ,Hu LH,Shen X

更新日期：2010-07-01 00:00:00

abstract：AIM:To investigate the effects of small interfering RNA of cyclooxygenase-2 (COX-2) on the proliferation and apoptosis of human multiple myeloma RPMI8226 cells and its relation with the Bcl-2 family in vitro. METHODS:Transcription and expression of COX-2 in human myeloma RPMI8226 cells were checked by RT-PCR and Weste...

journal_title：Acta pharmacologica Sinica

authors： Li QB,Chen ZC,You Y,Zou P

更新日期：2007-07-01 00:00:00

abstract：AIM:To ascertain the effects of erlotinib on CYP3A, to investigate the amplitude and kinetics of erlotinib-mediated inhibition of seven major CYP isoforms in human liver microsomes (HLMs) for evaluating the magnitude of erlotinib in drug-drug interaction in vivo. METHODS:The activities of 7 major CYP isoforms (CYP1A2,...

journal_title：Acta pharmacologica Sinica

authors： Dong PP,Fang ZZ,Zhang YY,Ge GB,Mao YX,Zhu LL,Qu YQ,Li W,Wang LM,Liu CX,Yang L

更新日期：2011-03-01 00:00:00

abstract：AIM:Hydrogen peroxide (H2O2) is produced during liver transplantation. Ischemia/reperfusion induces oxidation and causes intracellular Ca2+ overload, which harms liver cells. Our goal was to determine the precise mechanisms of these processes. METHODS:Hepatocytes were extracted from rats. Intracellular Ca2+ concentrat...

journal_title：Acta pharmacologica Sinica

authors： Sato H,Takeo T,Liu Q,Nakano K,Osanai T,Suga S,Wakui M,Wu J

更新日期：2009-01-01 00:00:00

abstract：AIM:KCNQ1 and KCNE1 form a complex in human ventricular cardiomyocytes, which are important in maintaining a normal heart rhythm. In the present study we investigated the effects of a homologous series of 1-alkanols on KCNQ1/KCNE1 channels expressed in Xenopus oocytes. METHODS:ECG recording was made in rats injected w...

journal_title：Acta pharmacologica Sinica

authors： Xie C,Liu HW,Pan N,Ding JP,Yao J

更新日期：2016-01-01 00:00:00

abstract：:For follicular lymphoma (FL) with grade 1/2, the complete response (CR) rate of the first-line R-CHOP treatment was significantly low. In this study, we assessed the rationality of the administration of rituximab for FL patients with grade 1/2 based on concentration-response relationship analyses. Thus, we conducted a...

journal_title：Acta pharmacologica Sinica

authors： Liu S,Huang H,Chen RX,Wang Z,Guan YP,Peng C,Fang XJ,Chen ZJ,Guan SX,Zhu X,Ren QG,Yao YY,Huang HB,Huang M,Wang XD,Lin TY

更新日期：2020-07-31 00:00:00

abstract：AIM:To investigate the proliferation of vascular smooth muscle cells (VSMC) affected by ginsenoside Rg1 and further explore the molecular mechanism of ginsenoside Rg1 using proteomics. METHODS:The proliferation of VSMC was measured by MTS assay kit and flow cytometry. Proteomic alterations were analyzed using two-dime...

journal_title：Acta pharmacologica Sinica

authors： Ma ZC,Gao Y,Wang YG,Tan HL,Xiao CR,Wang SQ

更新日期：2006-08-01 00:00:00

abstract：AIM:The substrate cocktail is frequently used to evaluate cytochrome P450 (CYP) enzyme-mediated drug interactions and potential interactions among the probe substrates. Here, we re-optimized the substrate cocktail method to increase the reliability and accuracy of screening for candidate compounds and expanded the meth...

journal_title：Acta pharmacologica Sinica

authors： Chen ZH,Zhang SX,Long N,Lin LS,Chen T,Zhang FP,Lv XQ,Ye PZ,Li N,Zhang KZ

更新日期：2016-05-01 00:00:00

abstract：:Retinoid X receptor-α (RXRα), a unique member of the nuclear receptor superfamily, represents an intriguing and unusual target for pharmacologic interventions and therapeutic applications in cancer, metabolic disorders and neurodegenerative diseases. Despite the fact that the RXR-based drug Targretin (bexarotene) is c...

journal_title：Acta pharmacologica Sinica

authors： Zhang XK,Su Y,Chen L,Chen F,Liu J,Zhou H

更新日期：2015-01-01 00:00:00

abstract：:Type capital I, Ukrainian natural killer T cells (NKT cells), a subset of CD1d-restricted T cells with invariant Valphabeta TCR, are characterized by prompt production of large amounts of Th1 and/or Th2 cytokines upon primary stimulation through the TCR complex. The rapid release of cytokines implies that type capital...

journal_title：Acta pharmacologica Sinica

authors： Tan JQ,Xiao W,Wang L,He YL

更新日期：2010-09-01 00:00:00

abstract：:Embryonic stem (ES) cells and their differentiated progeny offer tremendous potential for regenerative medicine, even in the field of drug discovery. There is an urgent need for clinically relevant assays that make use of ES cells because of their rich biological utility. Attention has been focused on small molecules ...

journal_title：Acta pharmacologica Sinica

authors： Lou YJ,Liang XG

更新日期：2011-02-01 00:00:00