Comparative Pharmacological Studies on the A_2 Adenosine Receptor Agonist 5'-n-Ethyl-carboxamidoadenosine and Its F^<19> Isotope Labelled Derivative

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概要

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• Adenosine receptors are expressed in various mammalian tissues where they mediate the effects of adenosine on cellular functions through a number of signalling mechanisms. 18F-NECA is the positron-emitting derivative of the A2-receptor agonist NECA (5-n-ethyl-carboxamidoadenosine) and is a radioligand for PET imaging of adenosine receptors. Contractility and relaxation studies were performed on guinea pig atrial myocardium, pulmonary artery, and thoracic aorta to compare the pharmacological effects of NECA and F-NECA (a non-emitting derivative) on tissues. Furthermore, the effect of NECA and F-NECA on the potassium conductance was investigated in DDT1 MF-2 smooth muscle cells with the patch-clamp technique. Both NECA and F-NECA reduced the contractile force in atrial myocardium and evoked phasic contraction in pulmonary artery (A1 adenosine-receptor-mediated actions) in a dose dependent manner; however, the apparent affinity was lower for F-NECA. No difference was found in relaxation induced by these compounds in 1 μM noradrenaline-precontracted aorta and pulmonary artery (in the presence of DPCPX, an A1 adenosine receptor antagonist, tissue containing A2B adenosine receptors). NECA (5 μM) and F-NECA (5 μM) also decreased the peak current and accelerated activation and inactivation properties of the potassium channels, but F-NECA was less effective. These results suggest that while NECA and F-NECA are equivalent agonists of vascular A2B receptors, they mediate different changes of some parameters. When evaluating the data obtained by the use of radiolabelled ligands, one has to take into consideration the possible physiological effects of the ligands besides its binding properties to tissues.

• 社団法人 日本薬理学会の論文
• 2003-11-01

著者

• Szekely A

  Department Of Biophysics And Cell Biology Research Center For Molecular Medicine University Of Debre

• Szekely Andrea

  Department Of Biophysics And Cell Biology University Of Debrecen

• RUBOVSZKY Balint

  Department of Biophysics and Cell Biology, University of Debrecen

• Gesztelyi Rudolf

  Dep. Of Pharmacology And Pharmacotherapy Univ. Of Debrecen Medical And Health Sci. Center Hun

• Tron Lajos

  Positron Emission Tomograph Center Research Center For Molecular Medicine University Of Debrecen

• Gaspar Rezso

  Department Of Biophysics And Cell Biology Research Center For Molecular Medicine University Of Debre

• Marian Terez

  Positron Emission Tomograph Center Research Center For Molecular Medicine University Of Debrecen

• Krasznai Zoltan

  Department Of Biophysics And Cell Biology Research Center For Molecular Medicine University Of Debre

• Cseppento Agnes

  Department Of Pharmacology And Pharmacotherapy University Of Debrecen Medical And Health Science Cen

• Gesztelyi Rudolf

  Department Of Pharmacology And Pharmacotherapy University Of Debrecen Medical And Health Science Cen

• SZENTMIKLOSI A.

  Department of Pharmacology and Pharmacotherapy, University of Debrecen, Medical- and Health Science

• SZENTMIKLOSI Jozsef

  Department of Pharmacology and Pharmacotherapy Research Center for Molecular Medicine, University of

• FORIZS Fruzsina

  Department of Biophysics and Cell Biology Research Center for Molecular Medicine, University of Debr

• Szekely Andrea

  Department Of Biophysics And Cell Biology Research Center For Molecular Medicine University Of Debre

• Szentmiklosi Jozsef

  Department Of Pharmacology And Pharmacotherapy Research Center For Molecular Medicine University Of

• Rubovszky Balint

  Department Of Biophysics And Cell Biology Research Center For Molecular Medicine University Of Debre

• Forizs Fruzsina

  Department Of Biophysics And Cell Biology Research Center For Molecular Medicine University Of Debre

• Marian Telez

  Positron Emission Tomograph Center, Research Center for Molecular Medicine, University of Debrecen

• Szentmiklosi A.

  Department of Pharmacology and Pharmacotherapy Research Center for Molecular Medicine, University of Debrecen

• GESZTELYI Rudolf

  Department of Pharmacology and Pharmacotherapy Research Center for Molecular Medicine, University of Debrecen

• CSEPPENTO Agnes

  Department of Pharmacology and Pharmacotherapy Research Center for Molecular Medicine, University of Debrecen

関連論文

• A_1 and A_2 Adenosine Receptor Activation Inversely Modulates Potassium Currents and Membrane Potential in DDT1 MF-2 Smooth Muscle Cells
• Modulation of Adenosine-Induced Responses in the Guinea-Pig Trachea During Long-Term Caffeine Treatment : Possible Role of Epithelium
• Special Sensitization Pattern in Adenosine-Induced Myocardial Resonses After Thuroxine-Treatment
• Comparative Pharmacological Studies on the A_2 Adenosine Receptor Agonist 5'-n-Ethyl-carboxamidoadenosine and Its F^ Isotope Labelled Derivative

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