title: Characterization of the K(+)-channel-coupled adenosine receptor in guinea pig atria.
abstract: In the present work we studied the pharmacological profile of adenosine receptors in guinea pig atria by investigating the effect of different adenosine analogues on 86Rb(+)-efflux from isolated left atria and on binding of the antagonist radioligand 8-cyclopentyl-1,3-[3H]dipropylxanthine [( 3H]DPCPX) to atrial membrane preparations. The rate of 86Rb(+)-efflux was increased twofold by the maximally effective concentrations of adenosine receptor agonists. The EC50-values for 2-chloro-N6-cyclopentyladenosine (CCPA), R-N6-phenylisopropyladenosine (R-PIA), 5'-N-ethylcarboxamidosadenosine (NECA), and S-N6-phenylisopropyladenosine (S-PIA) were 0.10, 0.14, 0.24 and 12.9 microM, respectively. DPCPX shifted the R-PIA concentration-response curve to the right in a concentration-dependent manner with a KB-value of 8.1 nM, indicating competitive antagonism. [3H]DPCPX showed a saturable binding to atrial membranes with a Bmax-value of 227 fmol/mg protein and a KD-value of 1.3 nM. Competition experiments showed a similar potency for the three agonists CCPA, R-PIA and NECA. S-PIA is 200 times less potent than R-PIA. Our results suggest that the K+ channel-coupled adenosine receptor in guinea pig atria is of an A1 subtype.
authors.affiliation: Pharmakologisches Institut der Universität, Heidelberg, Federal Republic of Germany.
authors.forename: H
authors.initials: H
authors.lastname: Tawfik-Schlieper
authors.forename: K N
authors.initials: KN
authors.lastname: Klotz
authors.forename: V A
authors.initials: VA
authors.lastname: Kreye
authors.forename: U
authors.initials: U
authors.lastname: Schwabe
mesh_terms: D000241:Adenosine / Q000031:analogs & derivatives / Q000494:pharmacology; D000818:Animals; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007700:Kinetics; D008566:Membranes / Q000378:metabolism; D009206:Myocardium / Q000378:metabolism*; D015221:Potassium Channels / Q000378:metabolism*; D011983:Receptors, Purinergic / Q000378:metabolism*; D012414:Rubidium Radioisotopes; D014970:Xanthines
chemical_list: D015221:Potassium Channels; D011983:Receptors, Purinergic; D012414:Rubidium Radioisotopes; D014970:Xanthines; C051360:1,3-dipropyl-8-cyclopentylxanthine; D000241:Adenosine