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[3H]5′-N-ethylcarboxamide adenosine binds to both Ra and Ri adenosine receptors in rat striatum

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Summary

Adenosine analogs such as 5′-N-ethylcarboxamide adenosine and N6-cyclohexyladenosine stimulate or inhibit adenosine cyclase activity in preparations of rat striatum depending on the assay conditions. N6-cyclohexyladenosine inhibits but does not stimulate adenosine cyclase activity in preparations of hippocampus. These findings suggest that the striatum contains both R a (stimulatory) and R i (inhibitory) adenosine receptors while the hippocampus contains only R i receptors. We have previously shown that [3H]N6-cyclohexyladenosine binds to R i receptors in rat hippocampus (Yeung and Green 1983). Comparisons of the characteristics of [3H]5′-N-ethylcarboxamide adenosine and [3H]N6-cyclohexyladenosine binding to hippocampus show that [3H]5′-N-ethylcarboxamide adenosine also binds to R i receptors with high affinity. [3H]5′-N-ethylcarboxamide adenosine binds to R i receptors in the striatum and to a second site that is present in striatum but not hippocampus. High affinity binding of both ligands to R i receptors can be blocked by treatments with N-ethylmaleimide that do not markedly affect [3H]5′-N-ethylcarboxamide adenosine binding to the second site in the striatum. The pharmacological characteristics of the second site indicate that it is the R a adenosine receptor.

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Abbreviations

NEM:

N-ethylmaleimide

Gpp(NH)p:

5′-guanylylimidodiphosphate

NECA:

5′-N-ethylcarboxamide adenosine

l-PIA:

N6-(l-phenylisopropyl)adenosine

d-PIA:

N6-(d-phenylisopropyl) adenosine

DPX:

1,3-diethyl-8-phenylxanthine

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Authors and Affiliations

  1. Department of Pharmacology, University of Illinois at Chicago, College of Medicine, 835 S. Wolcott, 60612, Chicago, IL, USA

    Siu-Mei H. Yeung & Richard D. Green

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  1. Siu-Mei H. Yeung
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  2. Richard D. Green
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Yeung, SM.H., Green, R.D. [3H]5′-N-ethylcarboxamide adenosine binds to both Ra and Ri adenosine receptors in rat striatum. Naunyn-Schmiedeberg's Arch. Pharmacol. 325, 218–225 (1984). https://doi.org/10.1007/BF00495947

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  • DOI: https://doi.org/10.1007/BF00495947

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