Search results for "PAM"

CLINICAL AND EXPERIMENTAL STUDIES WITH CHLORPROPAMIDE IN DIABETES MELLITUS, IN NORMAL INDIVIDUALS, AND IN NONDIABETICS WITH HEPATIC DISEASE

1959

In-line capillary electrophoretic evaluation of the enantioselective metabolism of verapamil by cytochrome P3A4

2013

Abstract In this paper a methodology for the in-line evaluation of enantioselective metabolism by capillary electrophoresis has been developed and applied to the study of verapamil metabolism by cytochrome P3A4. The developed methodology comprises an in-capillary reaction step carried out by electrophoretically mediated microanalysis and a separation step in which highly sulfated β-cyclodextrin with partial filling technique has been employed as chiral selector for verapamil and norverapamil enantiomers resolution, joining the advantages of both methodologies in a unique assay. Kinetic parameters of the enzymatic reaction (Km and Vmax) have been evaluated for both verapamil enantiomers by n…

The lack of the effect of DA-1 and DA-2 dopamine agonists on the isolated guinea-pig atria.

1987

1 The effects of dopamine and both DA-1 and DA-2 dopamine receptor agonists have been studied on the contractile force of electrically driven guinea-pig left atria and frequency of spontaneously beating right atria. 2 Pretreatment of animals with reserpine caused a parallel rightward shift of the concentration-response curve to dopamine of either preparation. 3 Propranolol, but not domperidone, shifted to the right the dose-response curve for the positive inotropic and chronotropic effects of dopamine. 4 Neither apomorphine, fenoldopam, bromocriptine nor piribedil had effects on the frequency and contractile force of the isolated guinea-pig atria. 5 These results suggest that DA-1 and DA-2 …

Optical studies on interaction of biliary contrast agents with native and modified human serum albumin.

1981

The interaction of two homologous series of biliary contrast agents with native human and bovine serum albumin and with modified human serum albumin was investigated using circular dichroism and equilibrium dialysis. For most derivatives, extrinsic Cotton effects were observed for the interaction with both albumins. In some cases, these effects were strongly affected by only small changes in the chemical structure of the drugs. These large differences in extrinsic Cotton effects can be explained by definite effects of the chemical structures on the binding site selectivity of some drugs. For example, iopodate preferentially binds to the warfarin binding site of human Scrum albumin, while an…

Influence of pH on the benzodiazepine-human serum albumin complex. Circular dichroism studies.

1974

The influence of pH on the binding of benzodiazepine derivatives to HSA was studied by circular dichroism measurements and by gel filtration. The binding of nearly all benzodiazepines is increased by rising the pH from 6.60 to 8.20. For flurazepam, clonazepam, and nitrazepam this increase in binding is due to an increase of the affinities, while for the other substances the affinity remains constant and the number of binding sites is increased from one to two. The changes in binding of the benzodiazepines by rising the pH are explained by a cationic amino acid residue near or at the benzodiazepine binding site of the HSA molecule. This second binding site is not detectable by circular dichr…

Zvaigžņotā Debess: 2000, Rudens (169)

2000

Contents: M.Zepe. Water Steam in the Venus Atmosphere ; B.Sala, L.Kondraševa. Use of Solar Energy ; A.Balklavs. Century Long Astrophysics ; Z.Alksne, A.Alksnis. Plenty of Extrasolar Planets ; Z.Alksne, A.Alksnis. Unexpected Discovery of Spiral Structure in a Dwarf Elliptical Galaxy ; A.Balklavs. Hunting for the Black Holes ; J.Jaunbergs. Private Enterprise on Mir ; T.Czarnik. Surviving Explosive Decompression ; M.Gills. Space Research 40 Years Ago – Chronicle ; M.Krastiņš. Impressions about Rose Center for the Earth and Space ; K.Bērziņš. On Friendly Terms with Cosmology: Basic Principles and Models of the Universe (continuation) ; V.Flerov, A.Cēbers, D.Docenko, V.Kaščejev. Latvia 24th Open…

(Re) Politizando la Solidariedad Internacional: Pensando la Cooperación como Educación para una Ciudadanía Global Radical

2017

[EN] The present moment of crisis regarding the identity and the resources of development aid calls for a deep reflection in order to recover the sense and the transformative aim of international development. In this work, we consider that we can recover a transformative agenda if we consider development aid as an space in which transformative learning processes take place. These learning processes lead to the construction of what can be called a ¿radical global citizenship¿. In development aid, individuals and organizations work together in social change processes. In these processes, people and organizations change through process of emergent and informal learning. Instead of considering …

Energy regulatory signals and food reward.

2009

The hormones insulin, leptin, and ghrelin have been demonstrated to act in the central nervous system (CNS) as regulators of energy homeostasis, acting at medial hypothalamic sites. Here, we summarize research demonstrating that, in addition to direct homeostatic actions at the hypothalamus, CNS circuitry that subserves reward and is also a direct and indirect target for the action of these endocrine regulators of energy homeostasis. Specifically, insulin and leptin can decrease food reward behaviors and modulate the function of neurotransmitter systems and neural circuitry that mediate food reward, the midbrain dopamine (DA) and opioidergic pathways. Ghrelin can increase food reward behavi…

In vitro P-glycoprotein efflux inhibition by atypical antipsychotics is in vivo nicely reflected by pharmacodynamic but less by pharmacokinetic chang…

2011

Abstract Background P-glycoprotein (P-gp), an efflux transporter of the blood–brain barrier, limits the access of multiple xenobiotics to the central nervous system (CNS). Thus drug-dependent inhibition, induction or genetic variation of P-gp impacts drug therapy. Methods We investigated atypical antipsychotics and their interaction with P-gp. Amisulpride, clozapine, N-desmethylclozapine, olanzapine, and quetiapine were assessed in vitro on their inhibitory potential and in vivo on their disposition in mouse serum and brain, and behaviourally on the RotaRod test. In vivo wildtype (WT) and mdr1a/1b double knockout mice (mdr1a/1b (−/−, −/−); KO) were investigated. Results In rhodamine 123 eff…

Comprehensive analysis of forty yeast microarray datasets reveals a novel subset of genes (APha-RiB) consistently negatively associated with ribosome…

2014

Background The scale and complexity of genomic data lend themselves to analysis using sophisticated mathematical techniques to yield information that can generate new hypotheses and so guide further experimental investigations. An ensemble clustering method has the ability to perform consensus clustering over the same set of genes from different microarray datasets by combining results from different clustering methods into a single consensus result. Results In this paper we have performed comprehensive analysis of forty yeast microarray datasets. One recently described Bi-CoPaM method can analyse expressions of the same set of genes from various microarray datasets while using different cl…