The activity of the xanthine derivative bamifylline on central adenosine A1 and A2 receptors has been evaluated with radio-receptor binding in rat brain in comparison with other structure-related compounds. Bamifylline displaced3H-Cyclo-hexyl-adenosine and3H-Diethyl-8-phenyl-xanthine with a potency similar to that of 8-phenyl-theophylline, suggesting a high activity on A1-receptor subtype. In contrast, when3H-N-Ethyl-car{ballot box}amido adenosine was used to label A2 adenosine receptors in rat striatum, bamifylline displayed a lower activity comparable to that of enprofylline, an alkylxanthine considered a very weak antagonist of adenosine receptors. By calculating for each xanthine derivative its relative potency at A1 and A2 receptors (A2/A1 ratio), bamifylline turned out being the most selective A1 adenosine receptor antagonist so far tested.

SELECTIVE ACTIVITY OF BAMIFYLLINE ON ADENOSINE-A1-RECEPTORS IN RAT-BRAIN / M.P. ABBRACCHIO, F. CATTABENI. - In: PHARMACOLOGICAL RESEARCH COMMUNICATIONS. - ISSN 0031-6989. - 19:8(1987), pp. 537-545.

SELECTIVE ACTIVITY OF BAMIFYLLINE ON ADENOSINE-A1-RECEPTORS IN RAT-BRAIN

M.P. ABBRACCHIO
Primo
;
F. CATTABENI
Ultimo
1987

Abstract

The activity of the xanthine derivative bamifylline on central adenosine A1 and A2 receptors has been evaluated with radio-receptor binding in rat brain in comparison with other structure-related compounds. Bamifylline displaced3H-Cyclo-hexyl-adenosine and3H-Diethyl-8-phenyl-xanthine with a potency similar to that of 8-phenyl-theophylline, suggesting a high activity on A1-receptor subtype. In contrast, when3H-N-Ethyl-car{ballot box}amido adenosine was used to label A2 adenosine receptors in rat striatum, bamifylline displayed a lower activity comparable to that of enprofylline, an alkylxanthine considered a very weak antagonist of adenosine receptors. By calculating for each xanthine derivative its relative potency at A1 and A2 receptors (A2/A1 ratio), bamifylline turned out being the most selective A1 adenosine receptor antagonist so far tested.
Settore BIO/14 - Farmacologia
Article (author)
File in questo prodotto:
Non ci sono file associati a questo prodotto.
Pubblicazioni consigliate

Caricamento pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/186856
Citazioni
  • ???jsp.display-item.citation.pmc??? 2
  • Scopus 13
  • ???jsp.display-item.citation.isi??? 17
social impact