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Adenosine receptors in post‐mortem human brain
Author(s) -
James Stephen,
Xuereb John H.,
Askalan Rand,
Richardson Peter J.
Publication year - 1992
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1992.tb14240.x
Subject(s) - striatum , cgs 21680 , cholinergic , binding site , adenosine , human brain , adenosine receptor , biology , receptor , adenosine a2a receptor , biochemistry , neuroscience , chemistry , dopamine , agonist
1 Adenosine A 2 ‐like binding sites were characterized in post‐mortem human brain membranes by examining several compounds for their ability to displace [ 3 H]‐CGS 21680 (2[ p ‐(2 carboxyethyl)‐phenethylamino]‐5′‐N‐ethylcarboxamido adenosine) binding. 2 Two A 2 ‐like binding sites were identified in the striatum. 3 The more abundant striatal site was similar to the A 2a receptor previously described in rat striatum, both in its pharmacological profile and striatal localization. 4 The less abundant striatal site had a pharmacological profile similar to that of the binding site characterized in the other brain regions examined. This was intermediate in character between A 1 and A 2 and may represent another adenosine receptor subtype. 5 The co‐purification of [ 3 H]‐CGS 21680 binding during immunoisolation of human striatal cholinergic membranes was used to assess the possible cholinergic localization of A 2 ‐like binding sites in the human striatum. Only the more abundant striatal site co‐purified with cholinergic membranes. This suggests that this A 2a ‐like site is present on cholinergic neurones in the human striatum.