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Pharmacological classification of adenosine receptors in the sinoatrial and atrioventricular nodes of the guinea-pig. 1998

B J Meester, and N P Shankley, and N J Welsh, and J Wood, and F L Meijler, and J W Black
Analytical Pharmacology, Rayne Institute, King's College School of Medicine & Dentistry, London, UK.

1. The effects of seven agonist and three antagonist adenosine receptor ligands were compared on the guinea-pig sinoatrial (SA) node (isolated right atrium) and atrioventricular (AV) node (perfused whole heart). Single agonist concentration-effect curves were obtained to 5'-N-ethylcarboxamidoadenosine (NECA), R(-)-N6-(2-phenylisopropyl)adenosine (R-PIA), N6-cyclohexyladenosine (CHA), 2-chloroadenosine (CADO),),S(+)-N6-(2-phenylisopropyl)adenosine (L-PIA), 2-phenylaminoadenosine (CV 1808) and N6-aminoadenosine (MeAdo). Adenosine and/or NECA curves were obtained in the absence and presence of the antagonists 8-cyclopentyl-1,3-dipropylxanthine (DPCPX), 9-chloro-2 (2-furanyl)-5,6-dihydro-1,2,4-triazolo[1,5-c]quinazolin-5-imine (CGS15943) and N6-(endonorbornan-2-yl)-9-methyladenine (N-0861). 2. A formal comparison of the agonist and antagonist potency data was made by fitting the data to a straight line using a least squares procedure based on principal components analysis to account for the variance on both axes. The antagonist affinity estimates made on the two assays did not deviate significantly from the line of identity. 3. The agonist p[A]50 data obtained on the two assays did not deviate from the line of identity, indicating that there were no significant differences in potencies between the two assays. The p[A]50 ratio of R-PIA and S-PIA was 1.24+/-0.09 in the SA node and 1.36+/-0.11 in the AV node, indicating no difference in the stereoselectivity of the PIA isomers between the two tissues. 4. The agonist potency and antagonist affinity data obtained are consistent with previous findings showing that the AV and SA node data are pharmacologically indistinguishable and belong to the adenosine A1-receptor class. No evidence for the reported A3-receptor was found.

UI MeSH Term Description Entries
D008297 Male Males
D006168 Guinea Pigs A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research. Cavia,Cavia porcellus,Guinea Pig,Pig, Guinea,Pigs, Guinea
D006339 Heart Rate The number of times the HEART VENTRICLES contract per unit of time, usually per minute. Cardiac Rate,Chronotropism, Cardiac,Heart Rate Control,Heartbeat,Pulse Rate,Cardiac Chronotropy,Cardiac Chronotropism,Cardiac Rates,Chronotropy, Cardiac,Control, Heart Rate,Heart Rates,Heartbeats,Pulse Rates,Rate Control, Heart,Rate, Cardiac,Rate, Heart,Rate, Pulse
D000241 Adenosine A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter. Adenocard,Adenoscan
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001283 Atrioventricular Node A small nodular mass of specialized muscle fibers located in the interatrial septum near the opening of the coronary sinus. It gives rise to the atrioventricular bundle of the conduction system of the heart. AV Node,A-V Node,Atrio-Ventricular Node,A V Node,A-V Nodes,AV Nodes,Atrio Ventricular Node,Atrio-Ventricular Nodes,Atrioventricular Nodes,Node, A-V,Node, AV,Node, Atrio-Ventricular,Node, Atrioventricular,Nodes, A-V,Nodes, AV,Nodes, Atrio-Ventricular,Nodes, Atrioventricular
D012849 Sinoatrial Node The small mass of modified cardiac muscle fibers located at the junction of the superior vena cava (VENA CAVA, SUPERIOR) and right atrium. Contraction impulses probably start in this node, spread over the atrium (HEART ATRIUM) and are then transmitted by the atrioventricular bundle (BUNDLE OF HIS) to the ventricle (HEART VENTRICLE). Sinuatrial Node,Sinus Node,Sino-Atrial Node,Sinu-Atrial Node,Node, Sino-Atrial,Node, Sinoatrial,Node, Sinu-Atrial,Node, Sinuatrial,Node, Sinus,Nodes, Sino-Atrial,Nodes, Sinoatrial,Nodes, Sinu-Atrial,Nodes, Sinuatrial,Nodes, Sinus,Sino Atrial Node,Sino-Atrial Nodes,Sinoatrial Nodes,Sinu Atrial Node,Sinu-Atrial Nodes,Sinuatrial Nodes,Sinus Nodes
D013237 Stereoisomerism The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed) Molecular Stereochemistry,Stereoisomers,Stereochemistry, Molecular,Stereoisomer
D043684 Receptor, Adenosine A3 A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of locations including the BRAIN and endocrine tissues. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP. Adenosine A3 Receptors,Adenosine A3 Receptor,A3 Receptor, Adenosine,A3 Receptors, Adenosine,Receptors, Adenosine A3
D058906 Purinergic P1 Receptor Agonists Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS. Adenosine Receptor Agonists,P1 Purinoceptor Agonists,Agonists, Adenosine Receptor,Agonists, P1 Purinoceptor,Purinoceptor Agonists, P1,Receptor Agonists, Adenosine

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