abstract：:Effects of bepridil on the low voltage-activated T-type Ca2+ channel (CaV3.2) current stably expressed in human embryonic kidney (HEK)-293 cells were examined using patch-clamp techniques. Bepridil potently inhibited ICa,T with a markedly voltage-dependent manner; the IC50 of bepridil was 0.4 micromol/l at the holding...

journal_title：Pharmacology

authors： Uchino T,Lee TS,Kaku T,Yamashita N,Noguchi T,Ono K

更新日期：2005-07-01 00:00:00

abstract：:Peroxisome proliferator-activated receptor-gamma (PPARgamma) is a nuclear receptor that regulates lipid metabolism. Recently, PPARgamma was reported to be a negative regulator in the immune system. Eosinophils also express PPARgamma, however, the role of PPARgamma in eosinophil functions is not well understood. Surfac...

journal_title：Pharmacology

authors： Matsuwaki Y,Ueki S,Adachi T,Oyamada H,Kamada Y,Yamaguchi K,Kanda A,Hamada K,Kayaba H,Chihara J

更新日期：2005-07-01 00:00:00

abstract：:We investigated the vascular effects of glucagon-like peptide-1 (GLP-1) and Exendin-4 in type 2 diabetic rat aortae. Studies were performed in a normal control group (NC) (0.2 ml i.p. saline, n = 10), streptozotocin (STZ)/nicotinamide diabetic control group (DC) (a single dose of 80 mg/kg STZ i.p. injection 15 min aft...

journal_title：Pharmacology

authors： Ozyazgan S,Kutluata N,Afşar S,Ozdaş SB,Akkan AG

更新日期：2005-06-01 00:00:00

abstract：:The aims of the present study were to investigate the pharmacological effects induced by Tityus serrulatus venom (TsV) and its fractions and to compare with the effects induced by pure alpha (TsTX-V) and beta (TsTX-I) toxins isolated from TsV on rat retractor penis muscle (RPM). TsV, fractions X, XI, XIIa, XIIb (0.01-...

journal_title：Pharmacology

authors： Bomfim JH,de Godoy MA,Giglio JR,de Oliveira AM,Arantes EC

更新日期：2005-03-01 00:00:00

abstract：:We investigated the antihypertensive effect of 5-HT1A agonist (buspirone) and 5-HT2B antagonists (SB204741 and SB200646) in deoxycorticosterone acetate (DOCA)-salt-induced hypertensive rats. Experiments were divided into two sets: in the first set, sham-operated control and DOCA-treated hypertensive rats received busp...

journal_title：Pharmacology

authors： Shingala JR,Balaraman R

更新日期：2005-03-01 00:00:00

abstract：:As a major Ca(2+) source for muscle contraction, the sarcoplasmic reticulum (SR) of skeletal muscle maintains its Ca(2+) content by uptake of myoplasmic Ca(2+) and by replenishment with extracellular Ca(2+). Since transection of motor nerve alters the functions of SR Ca(2+) pump and sarcolemma ion channels, this study...

journal_title：Pharmacology

authors： Hong SJ,Liang HC,Shen CJ

更新日期：2005-03-01 00:00:00

abstract：:The aim of this study was to determine whether transforming growth factor-beta1 (TGF-beta1) induces the synthesis, release and gene expression of urokinase-type plasminogen activator (uPA) in hepatic stellate cells. In addition to stimulating collagen production, TGF-beta1 induced the morphological and phenotypical ch...

journal_title：Pharmacology

authors： Pérez-Liz G,Flores-Hernández J,Arias-Montaño JA,Reyes-Esparza JA,Rodríguez-Fragoso L

更新日期：2005-01-01 00:00:00

abstract：:We investigated the contribution of the sympathetic nervous system (SNS) in maintaining the blood pressure and in regulating the cardiac function during and after carvedilol administration in rats with heart failure (group F). Left ventricular end-diastolic pressure, percent functional shortening, and rates of intrave...

journal_title：Pharmacology

authors： Abe Y,Watanabe K,Sato S,Nagai Y,Kamal FA,Wahed MI,Wen J,Narasimman G,Ma M,Suresh P,Takahashi T,Tachikawa H,Kashimura T,Tanabe N,Kodama M,Aizawa Y,Yamaguchi K,Miyazaki M,Kakemi M

更新日期：2004-12-01 00:00:00

abstract：:Metabotropic G protein-coupled receptors have recently been recognized as targets for anesthetics and analgesics. In particular, G(q)-coupled receptors such as muscarinic M(1) receptors (M(1)R) and 5-hydroxytryptamine (5-HT) type 2A receptors have been reported to be targets for anesthetics. Much less is known, howeve...

journal_title：Pharmacology

authors： Minami K,Uezono Y,Shiraishi M,Okamoto T,Ogata J,Horishita T,Taniyama K,Shigematsu A

更新日期：2004-11-01 00:00:00

abstract：:Lesopitron acts as a ligand for central serotonin 5-HT1A receptors. Ki obtained from [3H]8-OH-DPAT competition studies was 104.8 +/- 10.6 nmol/l. As lesopitron did not affect the binding of [3H]paroxetine, involvement of the serotonin reuptake system in the effects of lesopitron is rejected. Lesopitron inhibits halope...

journal_title：Pharmacology

authors： Fisas MA,Farré A,Camarasa J,Escubedo E

更新日期：2004-10-01 00:00:00

abstract：:To elucidate potential stereoselective effects of single barbiturate isomers, we compared the inhibitory potency of single thiopentone enantiomers, two isomer-enriched mixtures of methohexitone and racemic mixtures of both barbiturates on the fMLP-induced neutrophil oxidative response. A suppression of the response to...

journal_title：Pharmacology

authors： Wittmann S,Daniels S,Ittner KP,Fröhlich D

更新日期：2004-09-01 00:00:00

abstract：:We previously reported that adenovirus-mediated gene transfer of heme oxygenase-1 (HO-1) inhibits the development of atherosclerosis in apolipoprotein E-deficient mice. This finding implies that HO-1 induction is beneficial for protecting blood vessels. We also found that quercetin, a common polyphenolic compound in f...

journal_title：Pharmacology

authors： Lin HC,Cheng TH,Chen YC,Juan SH

更新日期：2004-06-01 00:00:00

abstract：:In organ transplantation, ischemia-reperfusion injury (IRI) has been implicated in delayed graft function (DGF) as well as in short- and long-term complications. Using an autotransplant pig kidney model, changes in renal function and morphology were determined after different periods of cold ischemia in kidneys preser...

journal_title：Pharmacology

authors： Baumert H,Faure JP,Zhang K,Petit I,Goujon JM,Dutheil D,Favreau F,Barrière M,Tillement JP,Mauco G,Papadopoulos V,Hauet T

更新日期：2004-05-01 00:00:00

abstract：:Several compounds with the backbone of 1,4-naphthoquinone chemical structure have been reported to display antiplatelet and antithrombotic activities, indicating that this congener compound may be a new source in the antithrombotic drug development. In the present study, the possible antiplatelet activity and antithro...

journal_title：Pharmacology

authors： Jin YR,Ryu CK,Moon CK,Cho MR,Yun YP

更新日期：2004-04-01 00:00:00

abstract：:Erythrocytes can take up amino acids from the blood by using a variety of transport systems. GLYT is a key transport protein in the plasma membrane responsible for the Na(2+)-dependent uptake of glycine needed for glutathione biosynthesis. Certain cysteine-specific compounds, particularly mercuric chloride and 5,5'-di...

journal_title：Pharmacology

authors： McCormick SJ,Tunnicliff G

更新日期：2004-03-01 00:00:00

abstract：:The cardioprotective effects of (2S,3R,4S)-N'-benzyl- N"-cyano-N-(3,4-dihydro-2-dimethoxymethyl-3-hydro- xy-2-methyl-6-nitro-2H-benzopyran-4-yl)-guanidine (KR-31372) were evaluated against ischemic/reperfusion injury in isolated rat hearts in vitro and in anesthetized rats and dogs in vivo. In isolated perfused rat he...

journal_title：Pharmacology

authors： Lee BH,Seo HW,Yoo SE

更新日期：2004-02-01 00:00:00

abstract：:We investigated a possible alteration in the ability of leukocytes to produce reactive oxygen species by stobadine, a pyridoindole antioxidant, in streptozotocin-diabetic rats. The production of free radicals from whole blood was assessed by luminol-enhanced chemiluminescence after stimulation by phorbol myristate ace...

journal_title：Pharmacology

authors： Demiryürek AT,Karasu C,Stefek M,Stolc S

更新日期：2004-01-01 00:00:00

abstract：:Combination therapy with antiretroviral drugs is used for the treatment of patients infected with the human immunodeficiency virus. To achieve optimal drug concentrations for viral suppression and avoidance of drug toxicity, monitoring of drug levels has been considered essential. We set up an analytical procedure for...

journal_title：Pharmacology

authors： Donnerer J,Kronawetter M,Kapper A,Haas I,Kessler HH

更新日期：2003-12-01 00:00:00

abstract：:Ketotifen is an antiallergic drug and may have direct inhibitory effects on eosinophils. To investigate the anti-eosinophilic effect of ketotifen, we examined the effect of ketotifen on the production of reactive oxygen species (ROS) from eotaxin-primed human eosinophils. Ketotifen at 10(-10)-10(-6) mol/l significantl...

journal_title：Pharmacology

authors： Yamada Y,Sannohe S,Saito N,Cui CH,Ueki S,Oyamada H,Kanda A,Yamaguchi K,Hamada K,Adachi T,Kayaba H,Chihara J

更新日期：2003-11-01 00:00:00

abstract：:The hypoxia-inducible factor 1alpha (HIF-1alpha), a member of the PAS superfamily, is a global regulator of cellular and systemic O(2) homeostasis as well as embryonic development. As the activity of HIF-1alpha is increased by a lowered oxygen tension in vivo and in vitro, we established a cell line producing high amo...

journal_title：Pharmacology

authors： Meissner U,Allabauer I,Repp R,Rascher W,Dötsch J

更新日期：2003-10-01 00:00:00

abstract：:The aim of this study was to compare the effects of a new thromboxane synthase inhibitor, camonagrel, on platelet aggregation and platelet-subendothelium interaction under flow conditions, in comparison with a standard thromboxane synthase inhibitor (dazoxiben) and a cyclooxygenase inhibitor (acetylsalicylic acid). Wi...

journal_title：Pharmacology

authors： Villalobos MA,De La Cruz JP,Escalante R,Arrebola MM,Guerrero A,Sánchez de la Cuesta F

更新日期：2003-09-01 00:00:00

abstract：UNLABELLED:We have reported that intermediate conductance Ca(2+)-activated K(+) channels (ImK) showed augmented expression in angiotensin II (AII) type 1 receptor-dependent manner in post-ischemic rat heart. ImK has tyrosine phosphorylation sequence in the C-terminus and motifs for NFkappaB and AP1 in the promoter. Whi...

journal_title：Pharmacology

authors： Terata Y,Saito T,Fujiwara Y,Hasegawa H,Miura H,Watanabe H,Chiba Y,Kibira S,Miura M

更新日期：2003-08-01 00:00:00

abstract：:A potential cytokine-drug interaction between interleukin 6 (IL-6) and itraconazole (ITZ) was studied using human hepatocytes in primary culture. Cultures from 5 adult males (mean age 42 +/- 15 years) who had not received any medicines known to interact with CYP3A4 were studied. Cultures were exposed to ITZ 500 ng/ml,...

journal_title：Pharmacology

authors： Gubbins PO,Melchert RB,McConnell SA,Franks AM,Penzak SR,Gurley BJ

更新日期：2003-04-01 00:00:00

abstract：:Self-administration of either nicotine (NIC) or ethanol (ETH) has been extensively studied. This study addressed for the first time the self-administration of both substances when offered together. Male and female rats of different ages were offered NIC and ETH using the two- or three-bottle free-choice method. When N...

journal_title：Pharmacology

authors： Marshall CE,Dadmarz M,Hofford JM,Gottheil E,Vogel WH

更新日期：2003-03-01 00:00:00

abstract：:There is an ongoing debate about possible advantages of the coadministration of caffeine with cyclooxygenase (COX) inhibitors in the treatment of pain. There are results suggesting interference by caffeine with COX expression and activity in rat immune cells. In the present study, we have used, therefore, human endoto...

journal_title：Pharmacology

authors： Ulcar R,Schuligoi R,Heinemann A,Santner B,Amann R

更新日期：2003-02-01 00:00:00

abstract：:The effect of 4-[3,5-bis(trimethylsilyl)benzamido] benzoic acid (TAC-101), one of the synthetic retinoids, on collagen-induced arthritis (CIA) in mice and experimental autoimmune encephalomyelitis (EAE) in rats was studied. TAC-101 at doses of 5 and 20 mg/kg clearly inhibited the development of CIA in terms of the swe...

journal_title：Pharmacology

authors： Miyagawa N,Homma T,Kagechika H,Shudo K,Nagai H

更新日期：2003-01-01 00:00:00

abstract：:Oxygen radicals have been considered to be important regulatory molecules in Helicobacter pylori-induced gastric ulceration and carcinogenesis. H. pylori-induced inflammation has been shown to be associated with cyclooxygenase-2 (COX-2) expression in experimental animals and human patients. This study aimed to determi...

journal_title：Pharmacology

authors： Kim H,Seo JY,Kim KH

更新日期：2002-12-01 00:00:00

abstract：:N-Tosyl-L-phenylalanyl-chloromethyl ketone (TPCK) is neuroprotective in rat pups. We measured bcl-2, Bax and caspase-3 to determine the mechanisms. Seven-day-old rats had the right carotid artery ligated and were subjected to 2.5 h of 8% oxygen. Ten mg/kg of PTCK or vehicle was given intraperitoneally 15 min prior to ...

journal_title：Pharmacology

authors： Feng Y,LeBlanc MH

更新日期：2002-11-01 00:00:00

abstract：:We determined the susceptibility of two ages of rat pups to become tolerant to and dependent on morphine infusions from osmotic minipumps. Neonatal rats (postnatal day 6; P6) were infused for 72 h with morphine at 0.175 or 0.7 mg/kg/h. On P9, morphine's antinociceptive efficacy was reduced in both groups. P14 infant r...

journal_title：Pharmacology

authors： Stoller DC,Thornton SR,Smith FL

更新日期：2002-09-01 00:00:00

abstract：:This study was performed to investigate the effect of muscimol on morphine-induced hyperactivity, reverse tolerance and postsynaptic dopamine receptor supersensitivity in mice. A single administration of morphine induced hyperactivity as measured in mice, and the morphine-induced hyperactivity was inhibited dose-depen...

journal_title：Pharmacology

authors： Yoon IS,Kim HS,Hong JT,Lee MK,Oh KW

更新日期：2002-08-01 00:00:00

abstract：:The involvement of AT1 and AT2 receptor subtypes in the response of the isolated rat uterus to angiotensin II (AngII) was studied throughout the estrous cycle. The AngII potency varied during the different estrous cycle phases, as indicated by significantly different pD2 values. No significant differences were observe...

journal_title：Pharmacology

authors： Accorsi-Mendonça D,Corrêa FM,Anselmo-Franci JA,Paiva TB,de Oliveira AM

更新日期：2002-07-01 00:00:00

abstract：:Based on their anabolic properties in skeletal muscles, beta-adrenergic agonists are of interest as potential countermeasures to microgravity-induced skeletal muscle atrophy. The levels of clenbuterol (Cb), a beta(2)-adrenergic agonist, in both plasma and skeletal muscle were higher in hindlimb-suspended rats than in ...

journal_title：Pharmacology

authors： von Deutsch DA,Abukhalaf IK,Wineski LE,Roper RR,Aboul-Enein HY,Paulsen DF,Potter DE

更新日期：2002-05-01 00:00:00

abstract：:The radioligand binding profiles and in vivo pharmacological characteristics of YM-44781, YM-44778 and YM-49598, novel non-peptide tachykinin receptor antagonists, were examined and compared to those of FK-888 and GR-159897. Since no functional NK(3) receptors were found in the rat bladder, the emphasis will be on the...

journal_title：Pharmacology

authors： Choppin A,Groke G,Bringas A,Stepan G,Dillon MP

更新日期：2002-05-01 00:00:00

abstract：:We investigated the total urinary kallikrein levels, left-ventricular wall thickness and mean arterial blood pressure of nontreated and captopril-treated diabetic and nondiabetic spontaneously hypertensive rats. The mean arterial blood pressure was significantly elevated in diabetic spontaneously hypertensive rats as ...

journal_title：Pharmacology

authors： Sharma JN,Kesavarao U

更新日期：2002-04-01 00:00:00

abstract：:Ulcerative colitis is characterized by dysfunctional motility. Our main objective in this investigation was to study the effect of an acetic acid-induced ulcerative colitis on the expression and function of beta(3)-adrenoceptors in the rat colon. Inflammation was induced by administering acetic acid intrarectally into...

journal_title：Pharmacology

authors： Khan I,Hussein SM,Oriowo M

更新日期：2002-02-01 00:00:00

abstract：:The relationship between alpha(1)-adrenoceptor binding in rat tissues and pharmacodynamic effects of continuous infusion of KMD-3213 was examined. In vivo specific binding of [(3)H]KMD-3213 after continuous intravenous infusion of the ligand (100 pmol/kg/min for 10 min, followed by 30 pmol/kg/min for 60 or 90 min) dif...

journal_title：Pharmacology

authors： Akiyama K,Tatemichi S,Katayama S,Nakajima M,Oki T,Okura T,Yamada S,Kimura R

更新日期：2002-01-01 00:00:00

abstract：:The electrophysiological and mechanical effects of HNS-32, a novel azulene-1-carboxamidine derivative with antiarrhythmic activity, were studied in isolated guinea-pig myocardial preparations. HNS-32 (10(-6)-10(-4) mol/l) concentration-dependently decreased the maximum rate of rise (V(max)) of action potential in isol...

journal_title：Pharmacology

authors： Noguchi K,Kase J,Saitoh M,Masumiya H,Saitoh M,Nakazawa T,Tanaka Y,Tanaka H,Hashimoto K,Shigenobu K

更新日期：2002-01-01 00:00:00

abstract：:Honokiol and magnolol have been identified as modulators of the GABAA receptors in vitro. Our previous study suggested a possible selectivity of honokiol and magnolol on GABAA receptor subtypes. This possibility was examined in the current study by 3H-muscimol and 3H-flunitrazepam binding assays on various rat brain m...

journal_title：Pharmacology

authors： Ai J,Wang X,Nielsen M

更新日期：2001-07-01 00:00:00

abstract：:Previous investigations demonstrated that CYP2D16 was expressed at high levels in guinea pig adrenal microsomes. The studies presented here were done to determine whether adrenal metabolism of bufuralol (BUF), a model CYP2D substrate, was similar to that in the liver. Guinea pig adrenal microsomes converted BUF to 1'-...

journal_title：Pharmacology

authors： Colby HD,Nowak DM,Longhurst PA,Zhang X,Hayes JR,Voigt JM

更新日期：2001-05-01 00:00:00

abstract：:Hyaluronic acid (HA) is an important component of the extracellular matrix of prostate cells. Platelet-derived growth factor bb (PDGFbb) has a mitogenic effect on prostate stromal cells. The effect of PDGFbb on HA production by smooth muscle cells from normal and benign prostatic hyperplasia (BPH) tissue was studied t...

journal_title：Pharmacology

authors： Pullen M,Thomas K,Wu H,Nambi P

更新日期：2001-02-01 00:00:00