Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors.
The synthesis and the preliminary biological evaluation of the first high affinity radioligand antagonist for the human A3 adenosine receptor, named [3H]-MRE 3008-F20 are reported. [3H]-MRE 3008-20 bound human A3 receptors expressed in CHO cells with K(D) and Bmax value of 0.82 +/- 0.08 nM and 297 +/- 28 fmol/mg of protein, respectively. [3H]-MRE 3008-F20 represents a useful tool for a further characterization of A3 adenosine receptor subtype.
Baraldi
P G
PG
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy. pgb@dns.unife.it
Cacciari
B
B
Romagnoli
R
R
Varani
K
K
Merighi
S
S
Gessi
S
S
Borea
P A
PA
Leung
E
E
Hickey
S L
SL
Spalluto
G
G
D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D006801:Humans; D010671:Phenylurea Compounds / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D058915:Purinergic P1 Receptor Antagonists; D011869:Radioligand Assay; D043684:Receptor, Adenosine A3; D018047:Receptors, Purinergic P1 / Q000378:metabolism; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D014230:Triazoles / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D014316:Tritium
C405605:MRE 3008-F20; D010671:Phenylurea Compounds; D058915:Purinergic P1 Receptor Antagonists; D043684:Receptor, Adenosine A3; D018047:Receptors, Purinergic P1; D011994:Recombinant Proteins; D014230:Triazoles; D014316:Tritium