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PMID: 6328332 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

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

Naunyn-Schmiedeberg's archives of pharmacology ·Vol. 325 ·No. 3 ·1984-03-00 ·Pages 218-25

Yeung SM, Green RD

Abstract

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 Ra (stimulatory) and Ri (inhibitory) adenosine receptors while the hippocampus contains only Ri receptors. We have previously shown that [3H]N6-cyclohexyladenosine binds to Ri 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 Ri receptors with high affinity. [3H]5'-N- ethylcarboxamide adenosine binds to Ri receptors in the striatum and to a second site that is present in striatum but not hippocampus. High affinity binding of both ligands to Ri 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 Ra adenosine receptor.

MeSH Terms
Adenosine/analogs & derivatives,metabolism,pharmacology Adenosine-5'-(N-ethylcarboxamide) Adenylyl Cyclase Inhibitors Adenylyl Cyclases/metabolism Animals Binding Sites/drug effects Cell Membrane/metabolism Corpus Striatum/metabolism,ultrastructure Ethylmaleimide/pharmacology Female Hippocampus/metabolism,ultrastructure In Vitro Techniques Male Rats Rats, Inbred Strains Receptors, Cell Surface/metabolism Receptors, Purinergic Synaptic Membranes/metabolism Vasodilator Agents/metabolism,pharmacology
Chemicals
Adenylyl Cyclase Inhibitors Receptors, Cell Surface Receptors, Purinergic Vasodilator Agents Adenosine-5'-(N-ethylcarboxamide) N(6)-cyclohexyladenosine Adenylyl Cyclases Adenosine Ethylmaleimide
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Yeung S M
Green R D
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28 references, click to expand
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Article Info
Journal
Naunyn-Schmiedeberg's archives of pharmacology
Abbr.
Naunyn Schmiedebergs Arch Pharmacol
ISSN
0028-1298
DOI
10.1007/BF00495947
Published
1984-03-00
Pages
218-25
Language
English
Region
Germany
NLM ID
0326264
Subset
IM
External Links
PubMed source DOI: 10.1007/BF00495947 View journal details
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