Can therapeutic efficacy be predicted from phase I data?

abstract：:During the last decade, a multitude of experimental arguments have led to the concept that EDRF is nitric oxide (NO), a messenger not only involved in the control of vasomotor tone but also in vascular homeostasis, neuronal and immunological functions. Regardless of its origin, endogenous NO is produced through the co...

journal_title：Fundamental & clinical pharmacology

authors： Berdeaux A

更新日期：1993-01-01 00:00:00

abstract：:Vanadium pharmacokinetic parameters and oral bioavailability were determined after administration of vanadyl sulfate, an antidiabetic agent, to male Wistar rats. An optimal sampling design was used over a 21-day period; vanadium was measured in blood by atomic absorption spectrophotometry (AAS). After i.v. bolus injec...

journal_title：Fundamental & clinical pharmacology

authors： Azay J,Brès J,Krosniak M,Teissedre PL,Cabanis JC,Serrano JJ,Cros G

更新日期：2001-10-01 00:00:00

abstract：:Paracetamol is an analgesic commonly used by people of all ages, which is well documented to cause severe hepatotoxicity with acute overexposures. The risk of hepatotoxicity from nonacute paracetamol exposures is less extensively studied, and this is the exposure most common in older adults. Evidence on the effectiven...

journal_title：Fundamental & clinical pharmacology

authors： Kane AE,Huizer-Pajkos A,Mach J,McKenzie C,Mitchell SJ,de Cabo R,Jones B,Cogger V,Le Couteur DG,Hilmer SN

更新日期：2016-06-01 00:00:00

abstract：:Advances in paediatric clinical pharmacology are interdependent with a better understanding of the influence of growth on drug disposition and action. In this field, there is an increasing need for non-invasive drug monitoring approaches. This paper aims to discuss the role of positron emission tomography in such prac...

journal_title：Fundamental & clinical pharmacology

authors： Zimmer L

更新日期：2008-12-01 00:00:00

abstract：:New primaquine (PQ) urea and semicarbazide derivatives 1-4 were screened for the first time for central nervous system (CNS) and antimalarial activity. Behavioural tests were performed on mice. In vitro cytotoxicity on L-6 cells and activity against erythrocytic stages of Plasmodium falciparum was determined. Compound...

journal_title：Fundamental & clinical pharmacology

authors： Kedzierska E,Orzelska J,Perković I,Knežević D,Fidecka S,Kaiser M,Zorc B

更新日期：2016-02-01 00:00:00

abstract：:Haloperidol (HP), an antipsychotic drug, is N-dealkylated by cytochrome P450 (CYP) to 4-fluorobenzoylpropionic acid (FBPA). The purpose of this study was to identify whether CYP3A metabolizes HP to FBPA in hepatic microsomes of rats and to investigate whether an inhibitor or an inducer of CYP3A affects HP pharmacokine...

journal_title：Fundamental & clinical pharmacology

authors： Watanabe M,Tateishi T,Asoh M,Nakura H,Tanaka M,Kumai T,Kobayashi S

更新日期：1999-01-01 00:00:00

abstract：:To date, no reports of hypersensitivity reactions (HSRs) among nonsteroidal anti-inflammatory drugs (NSAIDs) according to cyclo-oxygenase (COX) selectivity and chemical groups have been published in a single study. The present study assessed the reporting frequency of HSRs for NSAIDs based on their relative inhibitory...

journal_title：Fundamental & clinical pharmacology

authors： Bakhriansyah M,Meyboom RHB,Souverein PC,de Boer A,Klungel OH

更新日期：2019-10-01 00:00:00

abstract：:A combination of sub-effective doses of thioperamide (7.5 mg/kg, i.p.) and tacrine (0.5 mg/kg, i.p.) enhanced performance in a spatial memory task in mice. This was shown by a significant increase in their spontaneous alternation scores in a cross maze test. ...

journal_title：Fundamental & clinical pharmacology

authors： Vohora D,Pal SN,Pillai KK

更新日期：2005-10-01 00:00:00

abstract：:Anticonvulsant action of CGP 40116, a competitive antagonist of N-methyl-D-aspartate type of excitatory amino acid receptors, was studied in rats during development (7, 12, 18, 25 and 90 days old). Two types of motor seizures were elicited by a subcutaneous injection of pentylenetetrazol. Pretreatment with CGP 40116 d...

journal_title：Fundamental & clinical pharmacology

authors： Haugvicová R,Mares P

更新日期：1998-01-01 00:00:00

abstract：:The effects of tacrine and physostigmine on catecholamine secretion induced by veratridine and high K+, and on voltage-dependent Na+ and Ca2+ currents, were investigated in guinea-pig adrenal chromaffin cells. In perfused adrenal glands, tacrine (100 microM) caused an inhibition of veratridine-induced catecholamine se...

journal_title：Fundamental & clinical pharmacology

authors： Sugawara T,Kitamura N,Ohta T,Ito S,Nakazato Y

更新日期：1998-01-01 00:00:00

abstract：:Research during recent years has established nitric oxide as a unique signaling molecule that plays important roles in the regulation of the cardiovascular, nervous, renal, immune and other systems. Nitric oxide has also been implicated in the control of the secretion of hormones by the pancreas, hypothalamus, pituita...

journal_title：Fundamental & clinical pharmacology

authors： Reid IA,Chiu YJ

更新日期：1995-01-01 00:00:00

abstract：:The H1-histaminergic agonists 2-pyridylethylamine (2-PEA) and 2-methylhistamine relaxed potassium-constricted, perfused, rabbit middle cerebral arteries at low concentrations (3 x 10(-11) to 3 x 10(-8) M) and constricted them at high concentrations (3 x 10(-7) to 3 x 10(-4) M). The relaxation and the contraction were ...

journal_title：Fundamental & clinical pharmacology

authors： Ea Kim L,Sercombe R,Oudart N

更新日期：1988-01-01 00:00:00

abstract：:Erythropoietin (EPO), the principal hematopoietic cytokine produced by the kidney and the liver in fetuses, regulates mammalian erythropoiesis and exhibits diverse cellular effects in non-hematopoietic tissues. The introduction of recombinant human EPO (rhEPO) has marked a significant advance in the management of anem...

journal_title：Fundamental & clinical pharmacology

authors： Joyeux-Faure M,Godin-Ribuot D,Ribuot C

更新日期：2005-08-01 00:00:00

abstract：:Studies in animals and in healthy volunteers have demonstrated the central serotonergic analgesic mechanism of action of paracetamol involving the inhibition of this analgesia by tropisetron, a 5-HT3 antagonist. This randomized, double-blind, controlled study aims at studying this interaction in post-operative patient...

journal_title：Fundamental & clinical pharmacology

authors： Pickering G,Faure M,Commun F,de Boissy EC,Roche G,Mom T,Simen E,Dubray C,Eschalier A,Gilain L

更新日期：2012-06-01 00:00:00

abstract：:We reported that coronary spasm was induced in the transgenic mice with the increased phospholipase C (PLC)-δ1 activity. We investigated the effect of enhanced PLC-δ1 on Ca2+ influx and its underlying mechanisms. We used human embryonic kidney (HEK)-293 and coronary arteries smooth muscle cells (CASMC). Intracellular ...

journal_title：Fundamental & clinical pharmacology

authors： Murakami K,Osanai T,Tanaka M,Nishizaki K,Kinjo T,Tanno T,Ishida Y,Suzuki A,Endo T,Tomita H,Okumura K

更新日期：2017-08-01 00:00:00

abstract：:Microparticles are membrane vesicles with procoagulant and proinflammatory properties released during cell activation or apoptosis. Microparticles from monocytes have been implicated in atherosclerosis and vascular inflammation, but their direct effects on endothelial cells are not completely elucidated. The present s...

journal_title：Fundamental & clinical pharmacology

authors： Mastronardi ML,Mostefai HA,Soleti R,Agouni A,Martínez MC,Andriantsitohaina R

更新日期：2011-12-01 00:00:00

abstract：:The effect known as the GTP-shift refers to the complete conversion of receptors from the high- to the low agonist-affinity state in the presence of an excess of GTP or one of its analogs. 5'-Guanylylimidodiphosphate (GppNHp) was able to fully suppress the high (-)-isoproterenol-affinity of beta-adrenoceptors (beta AR...

journal_title：Fundamental & clinical pharmacology

authors： Garnier V,Zini R,Tillement JP

更新日期：1999-01-01 00:00:00

abstract：:Incubation of striatal slices with sodium nitroprusside (SNP) or hydroxylamine (HA) for 60 min caused a dose-dependent increase in dopamine (DA) release. This effect was inhibited completely by tetrodotoxin (TTX) (1 microM) if low concentrations of SNP (1 microM) or HA (10 and 100 microM) were tested. Although-higher ...

journal_title：Fundamental & clinical pharmacology

authors： Büyükuysal RL

更新日期：1997-01-01 00:00:00

abstract：:Angiotensin II AT1 receptor blockade (AT1-) has been shown to prolong survival in post-myocardial infarction (MI) heart failure in rats. In this study, we investigated whether an early AT1-induced improvement in coronary vasodilatation reserve (CVR) might be involved in this beneficial effect. Wistar rats with MI were...

journal_title：Fundamental & clinical pharmacology

authors： Gervais M,Richer C,Fornes P,De Gasparo M,Giudicelli JF

更新日期：1999-01-01 00:00:00

abstract：:Brain ageing affects numerous cerebral metabolic pathways such as cerebral glucose consumption or protein synthesis rate. The pharmacological effect of a mixed D1-D2 dopaminergic agonist, piribedil, on this last metabolism is reported. Cerebral Protein Synthesis Rate (CPSR) was measured by the [35S]L-methionine autora...

journal_title：Fundamental & clinical pharmacology

authors： Bustany P,Trenque T,Crambes O,Moulin M

更新日期：1995-01-01 00:00:00

abstract：:The insulin secreting B cell is fitted with the two types of purinergic receptors: P2 (for ATP and/or ADP) and P1 (for adenosine). The activation of P2 purinoceptors by ATP or ADP evokes a biphasic stimulation of insulin secretion from isolated perfused rat pancreas; this stimulation is dose-dependent between 10(-6) a...

journal_title：Fundamental & clinical pharmacology

authors： Hillaire-Buys D,Chapal J,Bertrand G,Petit P,Loubatières-Mariani MM

更新日期：1994-01-01 00:00:00

abstract：:Macrophage inflammatory protein (MIP)-1beta and RANTES (regulated on activation, normal T-cells expressed and secreted) are members of the CC-family of chemokines. Although these two peptides are structurally and functionally related to one another, each exhibits distinct features, which allows it to independently reg...

journal_title：Fundamental & clinical pharmacology

authors： Tavares E,Miñano FJ

更新日期：2004-04-01 00:00:00

abstract：OBJECTIVE:The aim of this study was to investigate the effects of intracoronary bradykinin (BK) infusion on noradrenaline release and ventricular arrhythmias induced by coronary occlusion and reperfusion in the anesthetized dog. METHODS:14 anesthetized adult mongrel dogs of either sex underwent a 60 min occlusion of t...

journal_title：Fundamental & clinical pharmacology

authors： Ribuot C,Yamaguchi N,Godin D,Jetté L,Adam A,Nadeau R

更新日期：1994-01-01 00:00:00

abstract：:We used two validated psychopharmacological methods, the forced swimming test (FST 20 min and 5 min) and the elevated plus-maze (EPM), to quantify depression-like and anxiety-like behavior induced by transient global cerebral ischemia in the rat. We also validated use of these methods for the study of antidepressant (...

journal_title：Fundamental & clinical pharmacology

authors： Bantsiele GB,Bentué-Ferrer D,Amiot N,Allain H,Bourin M,Reymann JM

更新日期：2004-12-01 00:00:00

abstract：:The effects of nifedipine and nicardipine, 2 dihydropyridines (DHP) used in the treatment of cardiovascular disorders, were compared in frog atrial fibers. Rapid photolysis of nifedipine with a single UV flash (1-ms duration) reversed the block, allowing comparison of effects of both drugs on the same preparation, and...

journal_title：Fundamental & clinical pharmacology

authors： Charnet P,Ouadid H,Richard S,Nargeot J

更新日期：1987-01-01 00:00:00

abstract：:The content of informed consent documents (ICD) is a crucial element in the process of providing information to participants in biomedical research. Clear comprehension of the information, i.e. the ability to understand its meaning and its consequences, is of utmost importance. The objective of this study was to descr...

journal_title：Fundamental & clinical pharmacology

authors： Paris A,Cornu C,Auquier P,Maison P,Radauceanu A,Brandt C,Salvat-Melis M,Hommel M,Cracowski JL

更新日期：2006-02-01 00:00:00

abstract：:Surrogate endpoints predict the occurrence and timing of a clinical endpoint of interest (CEI). Substitution of a surrogate endpoint for a CEI can dramatically reduce the time and cost necessary to complete a Phase III clinical trial. However, assurance that use of a surrogate endpoint will result in a correct conclus...

journal_title：Fundamental & clinical pharmacology

authors： Domanski M,Pocock S,Bernaud C,Borer J,Geller N,Revkin J,Zannad F

更新日期：2011-08-01 00:00:00

abstract：:The anticonvulsant effect of compounds that inhibit peptidyl-dipeptidase (PDP) on bicuculline (BIC)- and strychnine (STRYC)-induced seizures was assessed after intracerebroventricular (ICV) or intraperitoneal (IP) administration in Swiss albino mice. STRYC-induced seizures were delayed by ICV injections and high IP do...

journal_title：Fundamental & clinical pharmacology

authors： Miñano FJ,Serrano JS,Sancibrián M,Serrano MI

更新日期：1987-01-01 00:00:00

abstract：:Cyclo-oxygenase (COX) has been reported to play a significant role in neurodegeneration and other brain-related disorders. Recent studies have reported that COX plays a significant role in the pathophysiology of brain-related disorders and COX-2 inhibitors could be useful drug therapy in neurodegenerative disorders. T...

journal_title：Fundamental & clinical pharmacology

authors： Dhir A,Naidu PS,Kulkarni SK

更新日期：2006-06-01 00:00:00

abstract：:The aim of this analysis was to compare vasoreactive properties of internal thoracic arteries (ITA) grafts from diabetic (DM) to those of non-diabetic (ND) patients. Ring segments of ITA, taken from patients undergoing coronary artery bypass grafting, were suspended in organ bath chambers filled with modified Krebs-He...

journal_title：Fundamental & clinical pharmacology

authors： Grapow MT,Reineke DC,Kern T,Müller-Schweinitzer E,Carrel T,Eckstein FS

更新日期：2009-10-01 00:00:00