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Effect of 9‐(6,7‐Dideoxy‐ β ‐D‐ Allo ‐Hept‐5‐Ynofuranosyl)Adenine On Noradrenaline Release From Vascular Sympathetic Nerves
Author(s) -
Shinozuka Kazumasa,
IshiiNozawa Reiko,
Takeuchi Koichi,
Minakawa Noriaki,
Matsuda Akira,
Nakata Hiroyasu,
Kunitomo Masaru
Publication year - 2001
Publication title -
clinical and experimental pharmacology and physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.752
H-Index - 103
eISSN - 1440-1681
pISSN - 0305-1870
DOI - 10.1046/j.1440-1681.2001.03445.x
Subject(s) - purinergic receptor , chemistry , agonist , xanthine , endocrinology , medicine , receptor , biology , biochemistry , enzyme
SUMMARY 1. The effects of 9‐(6,7‐dideoxy‐β‐ D ‐ allo ‐hept‐5‐ynofuranosyl)adenine (HAK2701), a selective and potent ligand for P3 receptor‐like protein, on the release of endogenous noradrenaline (NA) from electrically stimulated rat mesenteric artery and rabbit ear artery were compared with those of a number of purinoceptor agonists. 2. In the rat mesenteric artery, the P1 receptor agonists 2‐chloroadenosine (2CA) and 5 ′ ‐ N ‐ethylcarboxamidoadenosine (NECA) and the P2 purinoceptor agonists β , γ ‐methylene ATP ( βγ mATP) and 2‐methylthio ATP (2mSATP) significantly inhibited the release of NA in a xanthine‐sensitive manner. HAK2701 did not significantly inhibit the release of NA, the relative order of potency being βγ mATP > NECA > 2CA > 2mSATP >> HAK2701. 3. In the rabbit ear artery, both P1 and P2 receptor agonists significantly facilitated the release of NA in a xanthine‐sensitive manner. HAK2701 also significantly facilitated the release of NA, the relative order of potency being HAK2701 > βγ mATP > 2CA > 2mSATP > NECA. 4. These findings suggest that HAK2701 may be a potent and selective agonist for facilitatory prejunctional purinoceptors, but not for inhibitory purinoceptors, on adrenergic nerve terminals.