caa a22 4500 469077948 CHVBK 20180323132940.0 cr unu---uuuuu 170328e19921201xx s 000 0 eng 10.1007/BF00168741 doi (NATIONALLICENCE)springer-10.1007/BF00168741 Effects of adenosine derivatives on human and rabbit platelet aggregation [Elektronische Daten] Correlation of adenosine receptor affinities and antiaggregatory activity [Silvio Dionisotti, Cristina Zocchi, Katia Varani, Pier Borea, Ennio Ongini] Summary: The inhibitory effects of several adenosine analogues, including the new A2-selective agonists 2-[p-(2-carboxyethyl)phenethylamino]-5′-N-ethylcarboxamido-adenosine (CGS 21680) and 2-hexynyl-5′-N-ethylcarbox-amidoadenosine (2-hexynyl-NECA), were investigated in vitro on human and rabbit platelet aggregation. The compounds examined inhibited ADP-induced platelet aggregation over a wide range of potency. The rank order of activity was similar between the two species thus showing that the rabbit is a useful animal model for studying the effects of adenosine derivatives on platelet aggregation. 2-Hexynyl-NECA was found to be the most potent adenosine compound of those currently available, having IC50 values of 0.10 and 0.07 μM in human and rabbit platelets, respectively. Conversely, the A1 agonists R(−)-N-6-(2-phenylisopropyl) adenosine (R-PIA), S(+)-N6-(2phenylisopropyl) adenosine (S-PIA) and 2-chloro-N6-cyclopentyl-adenosine (CCPA) were the least potent compounds with IC50 values in the micromolar range. The potency of the compounds in inhibiting platelet aggregation was found to be highly correlated with their affinity for A2 receptors as measured using 3H-CGS 21680 binding in rat brain striatum. Springer-Verlag, 1992 A2 Adenosine receptors nationallicence Platelet aggregation nationallicence Adenosine analogues nationallicence CGS 21680 nationallicence Dionisotti Silvio Research Laboratories, Schering-Plough S.p.A., I-20060, Comazzo, Milan, Italy aut Zocchi Cristina Research Laboratories, Schering-Plough S.p.A., I-20060, Comazzo, Milan, Italy aut Varani Katia Institute of Pharmacology, University of Ferrara, Ferrara, Italy aut Borea Pier Institute of Pharmacology, University of Ferrara, Ferrara, Italy aut Ongini Ennio Research Laboratories, Schering-Plough S.p.A., I-20060, Comazzo, Milan, Italy aut Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 346/6(1992-12-01), 673-676 0028-1298 346:6<673 1992 346 210 https://doi.org/10.1007/BF00168741 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF00168741 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Dionisotti Silvio Research Laboratories, Schering-Plough S.p.A., I-20060, Comazzo, Milan, Italy aut NATIONALLICENCE 700 1- Zocchi Cristina Research Laboratories, Schering-Plough S.p.A., I-20060, Comazzo, Milan, Italy aut NATIONALLICENCE 700 1- Varani Katia Institute of Pharmacology, University of Ferrara, Ferrara, Italy aut NATIONALLICENCE 700 1- Borea Pier Institute of Pharmacology, University of Ferrara, Ferrara, Italy aut NATIONALLICENCE 700 1- Ongini Ennio Research Laboratories, Schering-Plough S.p.A., I-20060, Comazzo, Milan, Italy aut NATIONALLICENCE 773 0- Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 346/6(1992-12-01), 673-676 0028-1298 346:6<673 1992 346 210 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer