Search

Your search keyword '"Urbán-Szabó K"' showing total 3 results
Start Over Author "Urbán-Szabó K"
3 results on '"Urbán-Szabó K"'

1. Interaction of SSR161421, a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo.

Author

Mikus EG, Boér K, Timári G, Urbán-Szabó K, Kapui Z, Szeredi J, Gerber K, Szabó T, Bátori S, Finet M, Arányi P, and Galzin AM

Subjects
Adenosine administration & dosage, Adenosine pharmacology, Adenosine A3 Receptor Antagonists administration & dosage, Aminoquinolines administration & dosage, Animals, Benzamides administration & dosage, CHO Cells, Cricetinae, Cricetulus, Cyclic AMP metabolism, Disease Models, Animal, Drug Interactions, Edema pathology, Histamine blood, Humans, Inhibitory Concentration 50, Male, Mice, Plasma metabolism, Receptors, Purinergic P1 drug effects, Receptors, Purinergic P1 metabolism, Adenosine analogs & derivatives, Adenosine A3 Receptor Agonists pharmacology, Adenosine A3 Receptor Antagonists pharmacology, Aminoquinolines pharmacology, Benzamides pharmacology, Edema drug therapy
Abstract

A novel adenosine A(3) receptor antagonist (SSR161421) was characterized by both receptor binding assays and pharmacological tests. Binding studies on cloned human adenosine receptors showed that SSR161421 has high affinity for adenosine hA(3) receptors (K(i)=0.37 nM) with at least 1000-fold selectivity compared to hA(1), hA(2A) and hA(2B) receptors. The receptor antagonist nature of SSR161421 was determined in a functional study on Chinese hamster ovarian cells (CHO) cells expressing human adenosine A(3) receptors. SSR161421 competitively antagonized the effect of 2-chloro-N6-(3-iodobenzyl)-adenosine-5'-N-methylcarboxamide (Cl-IB-MECA) on cAMP production with a pA2 value in a luciferase reporter gene construct. In mice, intravenously administered SSR161421 inhibited the N6-(4-aminobenzyl)-adenosine-5'-N-methyl-uronamide dihydrochloride (AB-MECA) induced increase in plasma histamine levels (ED(50)=2.0mg/kg) and the Cl-IB-MECA evoked plasma extravasation (ID(50)=2.9 mg/kg) and oedema formation (ID(50)=4.6 mg/kg) in mouse ear., (Copyright © 2012 Elsevier B.V. All rights reserved.)

Published
2013
Full Text
View/download PDF

2. A novel orally active inhibitor of HLE.

Author

Varga M, Kapui Z, Bátori S, Nagy LT, Vasvári-Debreczy L, Mikus E, Urbán-Szabó K, and Arányi P

Subjects
Administration, Oral, Animals, Asthma chemically induced, Asthma drug therapy, Asthma pathology, Cyclic S-Oxides chemistry, Cyclic S-Oxides metabolism, Cystic Fibrosis chemically induced, Cystic Fibrosis drug therapy, Cystic Fibrosis pathology, Dose-Response Relationship, Drug, Enzyme Inhibitors chemistry, Enzyme Inhibitors metabolism, Hemorrhage chemically induced, Hemorrhage drug therapy, Hemorrhage pathology, Humans, Inflammation chemically induced, Inflammation drug therapy, Inflammation pathology, Leukocyte Elastase administration & dosage, Leukocyte Elastase metabolism, Lung Diseases, Obstructive chemically induced, Lung Diseases, Obstructive drug therapy, Lung Diseases, Obstructive pathology, Mice, Models, Chemical, Pulmonary Emphysema chemically induced, Pulmonary Emphysema drug therapy, Pulmonary Emphysema pathology, Thiazoles chemistry, Thiazoles metabolism, Cyclic S-Oxides pharmacology, Enzyme Inhibitors pharmacology, Leukocyte Elastase antagonists & inhibitors, Thiazoles pharmacology
Abstract

Human leukocyte elastase (HLE) is a serine proteinase, capable of degrading a variety of structural matrix proteins. SSR69071 2-[(4-isopropyl-6-methoxy-1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)methoxy]-9-(2-piperidin-1-ylethoxy)-4H-pyrido[1,2-a]pyrimidin-4-one was selected as a novel orally active HLE inhibitor for treatment of chronic obstructive pulmonary diseases, asthma, emphysema, cystic fibrosis and several inflammatory diseases (WO 01/44245 A1) (J. Pharm. Exp. Ther., submitted for publication).

Published
2003
Full Text
View/download PDF

3. Behavioural effects of selective PDE4 inhibitors in relation to inhibition of catalytic activity and competition for [3H]rolipram binding.

Author

Kapui Z, Bence J, Boronkay E, Mikus E, Urbán Szabó K, Baranyi A, and Arányi P

Subjects
3',5'-Cyclic-AMP Phosphodiesterases chemistry, 3',5'-Cyclic-AMP Phosphodiesterases metabolism, Benzamides pharmacology, Binding, Competitive, Catalytic Domain drug effects, Cyclic Nucleotide Phosphodiesterases, Type 4, Papaverine metabolism, Papaverine pharmacology, Parasympatholytics metabolism, Phosphodiesterase Inhibitors metabolism, Pyridines pharmacology, Rolipram metabolism, Tritium, 3',5'-Cyclic-AMP Phosphodiesterases antagonists & inhibitors, Papaverine analogs & derivatives, Parasympatholytics pharmacology, Phosphodiesterase Inhibitors pharmacology, Rolipram pharmacology
Published
1999

Catalog

Books, media, physical & digital resources
See catalog results