Pharmacokinetic evaluation of a novel benzopyridooxathiazepine derivative as a potential anticancer agent.

abstract：BACKGROUND/AIMS:In this study, we evaluated the functional impact of facilitatory presynaptic adenosine A2A and muscarinic M1 receptors in the recovery of neuromuscular tetanic depression caused by the blockage of high-affinity choline transporter (HChT) by hemicholinium-3 (HC-3), a condition that mimics a myasthenia-l...

journal_title：Pharmacology

authors： Castellão-Santana LM,Yumi Abiko P,Ambiel CR,Peixoto AR,Noronha-Matos JB,Correia-de-Sá P,Alves-Do-Prado W

更新日期：2019-01-01 00:00:00

abstract：:Mast cells from different locations are shown to vary in their histochemical, ultrastructural, cytochemical and functional properties. The clinical consequences of this heterogeneity and possible reasons for its origin are discussed. ...

journal_title：Pharmacology

authors： Pearce FL

更新日期：1986-01-01 00:00:00

abstract：:Esculentoside A, a kind of saponin isolated from the root of the Chinese herb Phytolaca esculenta, is reported to possess potent anti-inflammatory effects in acute and chronic experimental models. In the present study, we investigated the effects of esculentoside A on the production of tumor necrosis factor (TNF), int...

journal_title：Pharmacology

authors： Ju DW,Zheng QY,Cao X,Fang J,Wang HB

更新日期：1998-04-01 00:00:00

abstract：:Various stressful stimuli cause mast cell degranulation. Hemorrhagic shock is one such stressful stimulus which may cause mast cell degranulation and histamine release. Histamine may be involved in the pathophysiology of hemorrhage. It was reported that there are large amounts of histamine in the anterior and posterio...

journal_title：Pharmacology

authors： Tikiz H,Tunçel N,Gürer F,Baycu C

更新日期：1991-01-01 00:00:00

abstract：BACKGROUND/AIMS:Fluorofenidone [1-(3-fluorophenyl)-5-methyl-2-(1H)-pyridone, AKF-PD], a novel pyridone agent, showed potent antifibrotic properties. The aim of the present study was to investigate the effects of AKF-PD on diabetic nephropathy and kidney fibrosis, and to obtain an insight into its mechanisms of action. ...

journal_title：Pharmacology

authors： Wang LH,Liu JS,Ning WB,Yuan QJ,Zhang FF,Peng ZZ,Lu MM,Luo RN,Fu X,Hu GY,Wang ZH,Tao LJ

更新日期：2011-01-01 00:00:00

abstract：:We examined the effects of cannabinoid receptor agonists on (45)Ca(2+) uptake in rat brain synaptosomes. A cannabinoid receptor agonist, (R)-(+)-[2,3-dihydro-5-methyl-3-[(4-merpholino)methyl]pyrrolo-[1,2,3-de]-1,4-benzoxazin-6-yl](1-naphthyl)methanone (WIN 55212-2) dose-dependently inhibited (45)Ca(2+) uptake in rat s...

journal_title：Pharmacology

authors： Yoshihara S,Morimoto H,Ohori M,Yamada Y,Abe T,Arisaka O

更新日期：2006-01-01 00:00:00

abstract：AIMS:Basal insulin administered to type-2 diabetic patients with poor glycaemic control when managed with oral anti-diabetics (OADs) alone can lead to an increased risk of weight gain and hypoglycaemia. In the absence of head-to-head trials, an indirect comparison of the once-daily insulin detemir with insulin glargine...

journal_title：Pharmacology

authors： Fakhoury W,Lockhart I,Kotchie RW,Aagren M,LeReun C

更新日期：2008-01-01 00:00:00

abstract：:In anesthetized rats intravenously infused, norepinephrine (NE) was accumulated by the heart, the spleen and the lung in a dose-related manner. With the lower dose of NE (2.5 mg/kg) the organ/blood ratios were more than unity and were generally greater than with higher doses (5 and 10 mg/kg), indicating that accumulat...

journal_title：Pharmacology

authors： Sivaramakrishna N,Gulati OD

更新日期：1975-01-01 00:00:00

abstract：:Induction of endogenous superoxide anion stress by the use of the superoxide dismutase inhibitor diethylthiocarbamate (DETCA; 10 mmol/l) produced a potent inhibition of the ATP (0.3-10 mmol/l) and diadenosine tetraphosphate (AP(4)A) contractile activity in the isolated vas deferens by 29-92 and 24-90%, respectively. P...

journal_title：Pharmacology

authors： Al-Rawi MB,Aleisa AM,Khattab MM

更新日期：2008-01-01 00:00:00

abstract：:The first step in the conversion of spironolactone (SP) to its biologically active metabolites is deacetylation to 7 alpha-thiospirolactone (7 alpha-thio-SL). Studies were done to evaluate the effects of reduced glutathione (GSH) on SP deacetylation by adrenal microsomal preparations. In the absence of GSH, adrenal mi...

journal_title：Pharmacology

authors： Colby HD,LaCagnin LB,Los LE

更新日期：1996-01-01 00:00:00

abstract：:Tacrine (THA) selectively modulates binding of M1 ligands in an allosteric fashion causing positive cooperativity. The binding affinity of THA to M1 and M2 cholinoceptors is similar. It is therefore proposed that the allosteric selectivity of THA is a function of the binding site and not of THA itself. Its interaction...

journal_title：Pharmacology

authors： Szilagyi M,Lau WM

更新日期：1993-10-01 00:00:00

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：:DL-o-, and p-octopamine were tested for beta- and alpha-adrenergic activity in rats. When compared to DL-isoproterenol, a beta-adrenergic agonist, all three isomers failed to show significant beta-adrenergic activity as assessed by intiation of thirst and by increase in tail skin temperature. All three isomers increas...

journal_title：Pharmacology

authors： Fregly MJ,Kelleher DL,Williams CM

更新日期：1979-01-01 00:00:00

abstract：:This study examined effects of intracerebroventricularly (i.c.v.) administered somatostatin (SRIH-14 and SRIH-28) on growth and function of pituitary somatotropes (GH cells) and lactotropes (PRL cells). Male rats received three i.c.v. injections (1 microgram/5 microliters) of SRIH-14 or SRIH-28 every second day. Blood...

journal_title：Pharmacology

authors： Milosević V,Brkić B,Velkovski SD,Sekulić M,Lovren M,Starcević V,Severs WB

更新日期：1998-07-01 00:00:00

abstract：BACKGROUND:Cassia angustifolia L. (senna) is traditionally used as a laxative. Its major components are sennosides that are responsible for the laxative effect. Senna is recommended for the short-term treatment of acute constipation. Nevertheless people use its preparations as self-medication, often for long periods, t...

journal_title：Pharmacology

authors： Vitalone A,Di Giacomo S,Di Sotto A,Franchitto A,Mammola CL,Mariani P,Mastrangelo S,Mazzanti G

更新日期：2011-01-01 00:00:00

abstract：:An increase in pulmonary vascular resistance (PVR) after cyclooxygenase inhibition (COI) is well documented in the dog, but the site of vasoconstriction to chemically distinct cyclooxygenase inhibitors is largely unknown. The purpose of the present study was to examine and compare equimolar concentrations of three che...

journal_title：Pharmacology

authors： Endrédi J,el-Kashef HA,Hofman WF,Ehrhart IC

更新日期：1992-01-01 00:00:00

abstract：:The intracerebroventricular injection of the cholecystokinin-A receptor antagonist L-364,718, at the doses of 0.5, 5, 10 or 20 micrograms/mouse, while having no effect on pain threshold (hot plate, 51 degrees C), antagonized the analgesic activity of morphine (10 mg/kg i.p.). This effect was obtained with a dose of 10...

journal_title：Pharmacology

authors： Poggioli R,Vergoni AV,Sandrini M,Barbafiera L,Marrama D,Bertolini A

更新日期：1991-01-01 00:00:00

abstract：BACKGROUND:Periplaneta americana is one of the ancient insect groups with the strongest vitality. Periplaneta americana extract (PAE) has been explored as an alternative remedy for many diseases. Although much progress has been made in the study about PAE, the role of the drug in renal disease is rarely reported, espec...

journal_title：Pharmacology

authors： Liu J,Zhou L,He L,Zhong Y,Zhang X,Xiao B,Liu G

更新日期：2018-01-01 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：:We studied the action of beta-adrenergic agonists on Japanese quail erythrocyte carbonic anhydrase (CA) in vitro. Earlier we had reported that epinephrine increased CA activity by 14%; the present study focused on an attempt to increase the size of this response. Washed erythrocytes from reserpine-treated (1 mg/kg dai...

journal_title：Pharmacology

authors： Igbo IN,Reigel CE Jr,Greene IM,Kenny AD

更新日期：1994-08-01 00:00:00

abstract：:The depression of evoked cortical potentials caused by brief periods of cerebral ischemia is attenuated by prior intracarotid injection of cytidoline (2, 4 or 8 mg/kg). Studies performed in hypercapnic cats suggest that the protection afforded by cytidoline is of metabolic rather than hemodynamic origin. The participa...

journal_title：Pharmacology

authors： Boismare F,Le Poncin M,Lefrançois J,Lecordier JC

更新日期：1978-01-01 00:00:00

abstract：:Both in vivo and in vitro exposure to morphine have been reported to produce a number of immunomodulatory effects in both laboratory animals and humans. The current study was performed to assess the direct in vitro effect of exposure to morphine or morphine metabolites on immune response parameters. Murine B6C3F1 sple...

journal_title：Pharmacology

authors： Thomas PT,Bhargava HN,House RV

更新日期：1995-01-01 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：:Serotonin-depleting lesions of midbrain raphe (extensive lesions located within dorsal and partly median raphe muclei) induced intraspecific agressiveness in grouped Wistar male rats but failed to increase mouse-killing behaviour. Rats which had lesions in the lateral midbrain did not display intraspecific aggression ...

journal_title：Pharmacology

authors： Kostowski W,Cxlonkowski A,Markowdka L,Markiewicz L

更新日期：1975-01-01 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：AIM:An increase in carotid intima-media thickness (CIMT) represents an early phase of the atherosclerotic process. The aim of our study was to evaluate whether a reduction in CIMT could be seen with 1-year treatment with rosuvastatin (10 mg/day). METHODS AND RESULTS:Forty-five patients with hypercholesterolemia and as...

journal_title：Pharmacology

authors： Riccioni G,Vitulano N,Mancini B,Zanasi A,D'Orazio N

更新日期：2010-01-01 00:00:00

abstract：:Amphetamine is a sympathomimetic and psychotropic drug which is extensively metabolized in liver and in brain. One of its major metabolites, p-hydroxyamphetamine, is accumulated by cortical and striatal synaptosomes. In order to learn whether p-hydroxyamphetamine can be further metabolized to a catecholamine, a sensit...

journal_title：Pharmacology

authors： Hoffman AR,Sastry BV,Axelrod J

更新日期：1979-01-01 00:00:00

abstract：:The antinociceptive effect in mice (hot-plate test) of caerulein (0.15 mg/kg s.c.) was many times more resistant to naloxone than that of morphine (2 mg/kg s.c., equipotent with the caerulein dose). The ED50 (mg/kg s.c.) of naloxone (given simultaneously with an agonist) was with morphine 0.01 and with caerulein 0.07....

journal_title：Pharmacology

authors： Zetler G

更新日期：1982-01-01 00:00:00

abstract：BACKGROUND/AIMS:Morphine causes state-dependent learning that its mechanism and brain-related structures are not fully understood. This study aimed to determine whether lidocaine reversible inactivation of the central nucleus of the amygdala (CeA) could affect acquisition, consolidation, and retrieval of morphine state...

journal_title：Pharmacology

authors： Noorbakhshnia M,Rahmani-Samani P,Eivani M

更新日期：2020-01-01 00:00:00

abstract：AIMS:This study analyzed the role of the amiloride-sensitive component and the participation of the Na(+)/H(+) exchanger in renal responsiveness to vasoconstrictors in the isolated perfused rat kidney. METHODS:The renal responses to vasoconstrictors (angiotensin II, phenylephrine, vasopressin and KCl) were studied und...

journal_title：Pharmacology

authors： Vargas P,Wangensteen R,Rodríguez-Gómez I,Perez-Abud R,Osuna A,Quesada A,Vargas F

更新日期：2011-01-01 00:00:00