Potent antidiabetic effects of rivoglitazone, a novel peroxisome proliferator-activated receptor-gamma agonist, in obese diabetic rodent models.

Abstract:

:The pharmacological effects of rivoglitazone, a novel thiazolidinedione-derivative peroxisome proliferator-activated receptor (PPAR)-gamma agonist, were characterized in vitro and in vivo. Rivoglitazone activated human PPARgamma more potently compared with rosiglitazone and pioglitazone and had little effect on PPARalpha and PPARdelta activity in luciferase reporter assays. In Zucker diabetic fatty (ZDF) rats, 14-day administration of rivoglitazone decreased the plasma glucose and triglyceride (TG) levels in a dose-dependent manner. The glucose-lowering effect of rivoglitazone was much more potent than those of pioglitazone (ED(50): 0.19 vs. 34 mg/kg) and rosiglitazone (ED(50): 0.20 vs. 28 mg/kg). In addition, rivoglitazone showed potent antidiabetic effects in diabetic db/db mice. In Zucker fatty rats, rivoglitazone at a dose of 0.1 mg/kg clearly ameliorated insulin resistance and lowered plasma TG levels by accelerating the clearance of plasma TG. Gene expression analysis in the liver and heart of ZDF rats treated with rivoglitazone for 14 days suggested that rivoglitazone may reduce hepatic glucose production and modulate the balance of the cardiac glucose/fatty acid metabolism in diabetic animals. In summary, we showed that rivoglitazone is a potent and selective PPARgamma agonist and has a potent glucose-lowering effect via improvement of the insulin resistance in diabetic animal models.

journal_name

J Pharmacol Sci

authors

Kanda S,Nakashima R,Takahashi K,Tanaka J,Ogawa J,Ogata T,Yachi M,Araki K,Ohsumi J

doi

10.1254/jphs.09084fp

subject

Has Abstract

pub_date

2009-10-01 00:00:00

pages

155-66

issue

2

eissn

1347-8613

issn

1347-8648

pii

JST.JSTAGE/jphs/09084FP

journal_volume

111

pub_type

杂志文章
  • Involvement of endothelin and ET(A) endothelin receptor in mechanical allodynia in mice given orthotopic melanoma inoculation.

    abstract::We investigated whether endothelin (ET) would be involved in skin cancer pain in mice. Orthotopic inoculation of B16-BL6 melanoma cells into the plantar region of the hind paw produced marked mechanical allodynia in C57BL/6 mice. Intraplantar injections of the ET(A)-receptor antagonist BQ-123 (0.3 - 3 nmol/site), but ...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.fp0072051

    authors: Fujita M,Andoh T,Saiki I,Kuraishi Y

    更新日期:2008-02-01 00:00:00

  • Effect of cigarette smoke components on vascular smooth muscle cell migration toward platelet-derived growth factor BB.

    abstract::Cigarette smoking is one of the factors causing accumulation of vascular smooth muscle cells (VSMCs) in atherosclerotic plaques. Changes in cell migration toward platelet-derived growth factor BB were investigated using a Boyden chamber after 48-h preincubation of GBaSM-4 VSMCs with nicotine or nicotine-free cigarette...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.10283sc

    authors: Yoshiyama S,Horinouchi T,Miwa S,Wang HH,Kohama K,Nakamura A

    更新日期:2011-01-01 00:00:00

  • Synergistic interaction between fentanyl and a tramadol: paracetamol combination on the inhibition of nociception in mice.

    abstract::Multimodal analgesic approaches to manage acute and chronic pain are commonly used in humans. Here, we attempted to characterize a synergistic interaction between fentanyl, tramadol, and paracetamol on the inhibition of nociception in a model of visceral pain in mice. The three-drug combined treatment displayed a pote...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.11161sc

    authors: Fernández-Dueñas V,Poveda R,Sánchez S,Ciruela F

    更新日期:2012-01-01 00:00:00

  • Multiple mechanisms for the action of chymase inhibitors.

    abstract::Angiotensin II plays an important role in regulating blood pressure. Moreover, angiotensin II directly promotes organ damage by inducing expression of various genes, such as transforming growth factor (TGF)-β and matrix metalloproteinase (MMP)-9 precursors. Blockade of angiotensin II has been shown to not only lower b...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1254/jphs.11r11cp

    authors: Takai S,Jin D,Miyazaki M

    更新日期:2012-01-01 00:00:00

  • Endothelial progenitor cells: therapeutic target for cardiovascular diseases.

    abstract::Circulating endothelial progenitor cells (EPCs) derived from bone marrow were isolated for the first time in 1997 and characterized. Recent evidence has indicated that EPCs contribute to re-endothelialization of injured vessels as well as neovascularization of ischemic lesions and that a decrease in the number of EPCs...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1254/jphs.08r01cp

    authors: Umemura T,Higashi Y

    更新日期:2008-09-01 00:00:00

  • Effect of aripiprazole on anxiety associated with ethanol physical dependence and on ethanol-induced place preference.

    abstract::In the present study, we investigated the effect of aripiprazole, a dopamine system stabilizer, on ethanol-induced psychological and physiological dependence and anxiety-like behavior. First we determined the effect of aripiprazole, a dopamine system stabilizer, on the development and expression of ethanol-induced pla...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.11201fp

    authors: Shibasaki M,Kurokawa K,Mizuno K,Ohkuma S

    更新日期:2012-01-01 00:00:00

  • Calf Spleen Extractive Injection (CSEI), a small peptides enriched extraction, induces human hepatocellular carcinoma cell apoptosis via ROS/MAPKs dependent mitochondrial pathway.

    abstract::Calf Spleen Extractive Injection (CSEI), a small peptides enriched extraction, performs immunomodulatory activity on cancer patients suffering from radiotherapy or chemotherapy. The present study aims to investigate the anti-hepatocellular carcinoma effects of CSEI in cells and tumor-xenografted mouse models. In HepG2...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2016.08.006

    authors: Jia D,Lu W,Zhang X,Cai G,Teng L,Wang X,Zhang M,Zeng Y,Liang C,Wang D

    更新日期:2016-10-01 00:00:00

  • Effects of mosapride citrate, a 5-HT4-receptor agonist, on gastric distension-induced visceromotor response in conscious rats.

    abstract::Mosapride citrate (mosapride), a prokinetic agent with 5-HT(4)-receptor agonistic activity, is known to enhance gastric emptying and alleviate symptoms in patients with functional dyspepsia (FD). As hyperalgesia and delayed gastric emptying play an important role in the pathogenesis of FD, we used in this study balloo...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.11012fp

    authors: Seto Y,Yoshida N,Kaneko H

    更新日期:2011-01-01 00:00:00

  • Genome-wide association study identifies polymorphisms associated with the analgesic effect of fentanyl in the preoperative cold pressor-induced pain test.

    abstract::Opioid analgesics are widely used for the treatment of moderate to severe pain. The analgesic effects of opioids are well known to vary among individuals. The present study focused on the genetic factors that are associated with interindividual differences in pain and opioid sensitivity. We conducted a multistage geno...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2018.02.002

    authors: Takahashi K,Nishizawa D,Kasai S,Koukita Y,Fukuda KI,Ichinohe T,Ikeda K

    更新日期:2018-03-01 00:00:00

  • Contrasting dose-effects of multi-glycoside of Tripterygium wilfordii HOOK. f. on glomerular inflammation and hepatic damage in two types of anti-Thy1.1 glomerulonephritis.

    abstract::Multi-glycoside, one of the extracted compounds from Tripterygium wilfordii HOOK. f. (GTW), has been shown to be clinically effective in suppressing glomerular inflammation in chronic kidney disease. However, its clinical application is often limited by its cytotoxic actions on the liver. This study was performed to c...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.11157fp

    authors: Wan YG,Zhao Q,Sun W,Zhang HL,Li M,Wei QX,Wu W,Yue LJ,Wang Q

    更新日期:2012-01-01 00:00:00

  • Pathophysiological significance of T-type Ca2+ channels: expression of T-type Ca2+ channels in fetal and diseased heart.

    abstract::Re-expression of fetal genes has been considered to underlie ionic remodeling in diseased heart. T-type Ca(2+) channels have been reported to be functionally expressed in embryonic hearts. In this review, we summarize developmental changes of T-type Ca(2+) channels in mouse ventricles from 9.5 days postcoitum (dpc) to...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1254/jphs.fmj05002x3

    authors: Yasui K,Niwa N,Takemura H,Opthof T,Muto T,Horiba M,Shimizu A,Lee JK,Honjo H,Kamiya K,Kodama I

    更新日期:2005-11-01 00:00:00

  • Negative impact of anesthesia with midazolam, sufentanil, and propofol used in pediatric flexible bronchoscopy on the tracheal ciliary beat frequency in guinea pigs.

    abstract::There is no direct evidence for the exact cilia-inhibitory effects of opioids, which are generally used to achieve general anesthesia in combination with other anesthetic drugs. These are the reasons, why we analysed direct concentration-dependent or systemic effects of anesthetics (propofol, sufentanil, and midazolam...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2020.01.005

    authors: Joskova M,Durdik P,Sutovska M,Grendar M,Koniar D,Hargas L,Banovcin P,Franova S

    更新日期:2020-04-01 00:00:00

  • Haloperidol affects coupling between QT and RR intervals in guinea pig isolated heart.

    abstract::Prolonged QT interval is an independent risk factor for development of ventricular arrhythmias. Haloperidol is one of the drugs inducing QT prolongation. Previous studies showed that haloperidol affects not only QT duration but also heart rate (RR interval). The present work focused on relationship between QT and RR a...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2018.11.004

    authors: Vesely P,Stracina T,Hlavacova M,Halamek J,Kolarova J,Olejnickova V,Mrkvicova V,Paulova H,Novakova M

    更新日期:2019-01-01 00:00:00

  • Carteolol hydrochloride reduces visible light-induced retinal damage in vivo and BSO/glutamate-induced oxidative stress in vitro.

    abstract::The purpose of this study was to determine whether carteolol eye drops, a β-adrenoceptor antagonist used as an intraocular hypotensive agent, has protective effects against the light-induced oxidative stress in retina. Dark-adapted pigmented rats were pre-treated with topical carteolol ophthalmic solution or saline an...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2018.11.010

    authors: Matsuo M,Kuse Y,Takahashi K,Kuwahara K,Tanito M,Kaidzu S,Shimazawa M,Hara H,Ohira A

    更新日期:2019-02-01 00:00:00

  • Discovery of a novel chalcone derivative inhibiting CFTR chloride channel via AMPK activation and its anti-diarrheal application.

    abstract::Secretory diarrhea is one of the most common causes of death world-wide especially in children under 5 years old. Isoliquiritigenin (ISLQ), a plant-derived chalcone, has previously been shown to exert anti-secretory action in vitro and in vivo by inhibiting CFTR Cl- channels. However, its CFTR inhibition potency is co...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2019.07.012

    authors: Yibcharoenporn C,Chusuth P,Jakakul C,Rungrotmongkol T,Chavasiri W,Muanprasat C

    更新日期:2019-07-01 00:00:00

  • Identification and characterization of rat RhoA gene promoter.

    abstract::RhoA upregulation has been suggested in bronchial smooth muscles (BSMs) of asthmatic rats. Here, we cloned/characterized the 5'-promoter region of the rat rhoA. A transcription-initiation site was identified at 66-bp upstream of the reference sequence, GenBank-BC061732. Luciferase assay using interleukin-13 (IL-13)-st...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.09346sc

    authors: Chiba Y,Goto K,Matsusue K,Kimura S,Misawa M

    更新日期:2010-01-01 00:00:00

  • Alleviation of the doxorubicin-induced nephrotoxicity by fasudil in vivo and in vitro.

    abstract:OBJECTIVE:Treatment with the chemotherapeutic agent, doxorubicin (DOX), is limited by side effects. We have previously demonstrated that fasudil, a Rho/ROCK inhibitor, has antioxidant, anti-inflammatory and anti-apoptotic effects in contrast-induced acute kidney injury model. The present study to investigated the possi...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2020.10.002

    authors: Xiang C,Yan Y,Zhang D

    更新日期:2021-01-01 00:00:00

  • Combination effects of ZSET1446/ST101 with memantine on cognitive function and extracellular acetylcholine in the hippocampus.

    abstract::In the novel object recognition task, ZSET1446 (also coded as ST101) enhanced object recognition memory in mice and ameliorated cognitive impairment caused by scopolamine in rats. The enhancement induced by ZSET1446 in mice was abolished by injection of mechamylamine, a nonselective antagonist of nicotinic acetylcholi...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.13042fp

    authors: Yamaguchi Y,Takeda K,Hino M

    更新日期:2013-01-01 00:00:00

  • Ameliorative effects of tannic acid on carbon tetrachloride-induced liver fibrosis in vivo and in vitro.

    abstract::We investigated the ameliorative effects and potential mechanisms of tannic acid (TA) in carbon tetrachloride (CCl4)-intoxicated mice and hepatic stellate cells (HSCs). Liver fibrosis was observed in CCl4 (800 ml/kg)-induced mice, and high viability was observed in CCl4 (10 mM)-intoxicated HSCs. Pre-treatment of mice ...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2015.12.002

    authors: Chu X,Wang H,Jiang YM,Zhang YY,Bao YF,Zhang X,Zhang JP,Guo H,Yang F,Luan YC,Dong YS

    更新日期:2016-01-01 00:00:00

  • Heterocyclic organobismuth(III) compound targets tubulin to induce G2/M arrest in HeLa cells.

    abstract::Our previous study showed that organobismuth compounds induce apoptosis in human promyelocytic leukemia cells, although solid tumor cell lines were relatively resistant. Herein, we investigated the primary cellular target of these compounds in HeLa cells. One organobismuth compound, bi-chlorodibenzo[c,f][1,5]thiabismo...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.09020fp

    authors: Iuchi K,Akagi K,Yagura T

    更新日期:2009-04-01 00:00:00

  • A simple method using anesthetics to test effects of sleep-inducing substances in mice.

    abstract::We investigated the effects of sleep-inducing agents with different mechanisms of action on the loss of the righting reflex induced by isoflurane or a mixture of medetomidine, midazolam, and butorphanol (MMB), followed by atipamezole reversal. Chlorpromazine and brotizolam delayed recovery from both types of anesthesi...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2019.12.003

    authors: Murai H,Suzuki H,Tanji H,Kimura T,Iba Y

    更新日期:2020-02-01 00:00:00

  • The systemic bone protective effects of Gushukang granules in ovariectomized mice by inhibiting osteoclastogenesis and stimulating osteoblastogenesis.

    abstract::Primary osteoporosis (POP), which is caused by unbalanced bone remodeling, leads to significant economic and societal burdens globally. Gushukang (GSK) granule serves as one commonly used prescription for POP in Traditional Chinese Medicine (TCM). The present study aimed to clarify the exact roles of GSK in bone remod...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2018.01.007

    authors: Wang Q,Zhao Y,Sha N,Zhang Y,Li C,Zhang H,Tang D,Lu S,Shi Q,Wang Y,Shu B,Zhao D

    更新日期:2018-03-01 00:00:00

  • Involvement of histamine released from mast cells in acute radiation dermatitis in mice.

    abstract::A possible involvement of histamine in acute radiation dermatitis in mice was investigated. The dose of 40 Gy of gamma irradiation induced erythema and edema in C57BL/6 mice treated with vehicle. However, in C57BL/6 mice treated with chlorpheniramine and WBB6F1-W/Wv mice, erythema and edema were not observed. In all o...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.sc0070127

    authors: Moriyasu S,Yamamoto K,Kureyama N,Okamura K,Ikeda T,Yamatodani A

    更新日期:2007-06-01 00:00:00

  • Cyclic ADP-ribose mediates formyl methionyl leucyl phenylalanine (fMLP)-induced intracellular Ca(2+) rise and migration of human neutrophils.

    abstract::Although cyclic ADP-ribose (cADPR), a novel Ca(2+)-mobilizing mediator, is suggested to be involved in the functions of neutrophils in rodents, its role in human neutrophils remains unclear. The present study examined the ability of cADPR to mobilize Ca(2+) and mediate formyl methionyl leucyl phenylalanine (fMLP)-stim...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.fp0072083

    authors: Morita K,Saida M,Morioka N,Kitayama T,Akagawa Y,Dohi T

    更新日期:2008-03-01 00:00:00

  • Diphenidol has no actual broad antiemetic activity in dogs and ferrets.

    abstract::Previous studies showed that diphenidol was effective on emetogens-induced pica, eating of non-nutritive substances, in rats, a model analogous to emesis in other species. We evaluated the actual antiemetic activity of diphenidol against four emetic stimuli in the dog and ferret, animals that possess an emetic reflex....

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.fpj04035x

    authors: Nakayama H,Yamakuni H,Nakayama A,Maeda Y,Imazumi K,Matsuo M,Mutoh S

    更新日期:2004-11-01 00:00:00

  • alpha7 Nicotinic acetylcholine receptor stimulation inhibits lipopolysaccharide-induced interleukin-18 and -12 production in monocytes.

    abstract::Nicotine inhibited interleukin (IL)-18 and -12 production in lipopolysaccharide (LPS)-stimulated monocytes, and the action of nicotine was antagonized by a non-selective and a selective alpha7 nicotinic acetylcholine receptor (alpha7-nAChR) antagonist, suggesting that the stimulation of alpha7-nAChR may be involved in...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.sc0060074

    authors: Takahashi HK,Iwagaki H,Hamano R,Yoshino T,Tanaka N,Nishibori M

    更新日期:2006-09-01 00:00:00

  • A receptor-independent effect of estrone sulfate on the HERG channel.

    abstract::We recently reported that physiological concentrations of 17beta-estradiol partially down-regulate cardiac rapidly-activating delayed rectifier K(+) currents (hERG currents) independently of estrogen-receptor signaling. To determine if other estrogens have the same effect as that of 17beta-estradiol, we investigated r...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.08257sc

    authors: Kakusaka S,Asayama M,Kaihara A,Sasano T,Suzuki T,Kurokawa J,Furukawa T

    更新日期:2009-01-01 00:00:00

  • Activation of ERK-p53 and ERK-mediated phosphorylation of Bcl-2 are involved in autophagic cell death induced by the c-Met inhibitor SU11274 in human lung cancer A549 cells.

    abstract::SU11274, a small molecule inhibitor of c-Met, was reported to induce apoptosis in human non-small-cell lung cancer (NSCLC) cells. However, SU11274-mediated autophagy in NSCLC cells has rarely been reported. The aim of this study was to elucidate the molecular mechanisms mediating SU11274-induced autophagy in NSCLC A54...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.11181fp

    authors: Liu Y,Yang Y,Ye YC,Shi QF,Chai K,Tashiro S,Onodera S,Ikejima T

    更新日期:2012-01-01 00:00:00

  • Protective effects of pioglitazone against global cerebral ischemic-reperfusion injury in gerbils.

    abstract::Despite of the huge socio-economic burden, stroke still represents an unmet therapeutic need. Researchers failed to reproduce preclinical efficacy in subsequent clinical development. To bridge this translation failure, the Stroke Therapy Academic Industry Round Table (STAIR) has suggested a rigorous, robust, and detai...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.08246fp

    authors: Kaundal RK,Iyer S,Kumar A,Sharma SS

    更新日期:2009-03-01 00:00:00

  • Changes of electrocardiogram and hemodynamics in response to dipyridamole: In vivo comparative analyses using anesthetized beagle dogs and microminipigs.

    abstract::Microminipigs are expected as a novel animal model for cardiovascular pharmacological experiments. Since inherent vulnerability of coronary circulation of microminipigs has not been characterized, we performed dipyridamole-stress test to both microminipigs and beagle dogs, and compared the results. Dipyridamole in dos...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2018.01.002

    authors: Ando K,Takahara A,Nakamura Y,Wada T,Chiba K,Goto A,Lubna NJ,Hagiwara-Nagasawa M,Izumi-Nakaseko H,Hoshiai K,Akie Y,Naito AT,Sugiyama A

    更新日期:2018-02-01 00:00:00