Send to

Choose Destination
Eur J Pharmacol. 1993 Oct 15;247(2):103-10.

The binding of the adenosine A2 receptor selective agonist [3H]CGS 21680 to rat cortex differs from its binding to rat striatum.

Author information

Department of Pharmacology, Karolinska Institutet, Stockholm, Sweden.


The binding of the reportedly A2A selective agonist CGS 21680 (2-[p-(2-carboxyethyl)phenylethylamino]-5'N-ethylcarboxamidoadenos ine) to cortex and striatum was examined in parallel using quantitative receptor autoradiography. [3H]CGS 21680 bound to a single site in rat striatum with KD 2.3 nM and Bmax 320 fmol/mg grey matter. In addition [3H]CGS 21680 bound to a single site in the cerebral cortex with KD 47 nM and Bmax 100 fmol/mg grey matter. In cat cortex [3H]CGS 21680 (2 nM) binding was strong and particularly evident in the most superficial layers. The potency order for inhibition of 2 nM [3H]CGS 21680 binding to rat striatum was NECA (5'-N-ethylcarboxamidoadenosine; IC50 9.0 nM) > 2-CADO (2-chloroadenosine; 87 nM) > R-PIA (N6-(R)-phenylisopropyladenosine; 110 nM). The potency order for inhibition of 2 nM [3H]CGS 21680 binding to rat cortex was NECA (3.0 nM) > 2-CADO (14 nM) > or = R-PIA (16 nM). Gpp(NH)p (5'-guanylyl imidodiphosphate) inhibited [3H]CGS 21680 binding to both cortex and striatum, but more potently in cortex (IC50 100 nM vs. 470 nM). The present results show that there is a cortical binding site for [3H]CGS 21680 which appears to be different from the the striatal A2A receptor, the A2B receptor and the A1 receptor.

[Indexed for MEDLINE]

Supplemental Content

Loading ...
Support Center