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Distribution of adenosine receptors in the postmortem human brain: An extended autoradiographic study
Author(s) -
Svenningsson Per,
Hall Håkan,
Sedvall Göran,
Fredholm Bertil B.
Publication year - 1997
Publication title -
synapse
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.809
H-Index - 106
eISSN - 1098-2396
pISSN - 0887-4476
DOI - 10.1002/(sici)1098-2396(199712)27:4<322::aid-syn6>3.0.co;2-e
Subject(s) - cgs 21680 , adenosine , globus pallidus , adenosine receptor , adenosine a2a receptor , adenosine a1 receptor , medicine , receptor , nucleus accumbens , chemistry , endocrinology , biology , neuroscience , agonist , basal ganglia , central nervous system
Whole‐hemisphere sections from six subjects were used in a quantitative autoradiographic study to characterize and to investigate the distribution of adenosine receptors, using [ 3 H]DPCPX, [ 3 H]CGS 21680, and [ 3 H]SCH 58261 as radioligands. [ 3 H]DPCPX‐binding showed the pharmacology expected for adenosine A 1 receptors and is therefore taken to mirror adenosine A 1 receptors. Adenosine A 1 receptors were widely distributed, with the highest densities in the stratum radiatum/pyramidale of the hippocampal region CA 1. Adenosine A 1 receptors were nonhomogeneously distributed in nucleus caudatus, globus pallidus, and cortical areas: In the cingulate and frontal cortex the deep layers showed the highest labeling, while in the occipital, parietal, temporal, and insular cortex it was highest in the superficial layers. In addition, we found very high levels of adenosine A 1 receptors in structures known to be important for cholinergic transmission, especially the septal nuclei. The B max values and K D values for [ 3 H]DPCPX‐binding in stratum radiatum/pyramidale of CA1 and the superficial layer of insular cortex were 598 and 430 fmol/mg gray matter and 9.9 and 14.2 nM, respectively. [ 3 H]CGS 21680‐binding was multiphasic, but showed the pharmacology expected for adenosine A 2A receptors and was taken to represent them. Adenosine A 2A receptors were abundant in putamen, nucleus caudatus, nucleus accumbens, and globus pallidus pars lateralis. Specific [ 3 H]CGS 21680‐binding was also found in certain thalamic nuclei and throughout the cerebral cortex. The adenosine A 2A receptor antagonist radioligand [ 3 H]SCH 58261 was also found to label these extrastriatal structures. Thus, adenosine A 2A receptors seem to be more widely distributed in the human brain than previously recognized. Synapse 27:322–335, 1997. © 1997 Wiley‐Liss, Inc.