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The antinociceptive effect of intrathecally administered adenosine analogs in mice correlates with the affinity for the A1-adenosine receptor.

Authors
  • Karlsten, R
  • Post, C
  • Hide, I
  • Daly, J W
Type
Published Article
Journal
Neuroscience Letters
Publisher
Elsevier
Publication Date
Jan 02, 1991
Volume
121
Issue
1-2
Pages
267–270
Identifiers
PMID: 2020383
Source
Medline
License
Unknown

Abstract

In the present study, the antinociceptive effects after intrathecal injection of each of 6 N6-substituted adenosine analogs and of 2-phenylaminoadenosine were compared with the affinity for the A1- and A2-adenosine receptors. Adenosine analogs, substituted in the N6-position, had stereoselective structure-dependent antinociceptive effects in the tail flick and hot plate assays after intrathecal injection in mice. The antinociceptive activity for N6-R- and S-phenylisopropyladenosine (R- and S-PIA), N6-R- and S-1-phenylethyladenosine, N6-1,1-dimethyl-2-phenylethyladenosine (methylPIA), and N6-cyclooctyladenosine correlated with the affinity for central A1-adenosine receptors. An adenosine analog, 2-phenylaminoadenosine, selective for A2-adenosine receptors was inactive in the two tests. These results strongly suggest that spinal A1-adenosine receptors are responsible for the antinociceptive effects of adenosine and its analogs after intrathecal injection.

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