Displacement of opioid receptor binding ligands from the rat brain by N3-(2',5'-dimethoxyphenacyl) arabinofuranosyluracil.
N3-(2',5 '-Dimethoxyphenacyl)arabinofuranosyluracil (N3-(2',5 '-DiMeOPhAc)AraU) is a pyrimidine nucleoside derivative which possesses antinociceptive effect by intracerebroventricular (i.c.v.) administration to mice. The compound (100 microM) significantly decreased the specific binding of [3H]D-Ala2, N-Me-Phe4, Gly5-ol-enkephalin (DAMGO) and [3H]D-Pen2, D-Pen5-enkephalin (DPDPE) at the mu- and delta-opioid receptor, respectively, but has no effect on the binding of [3H]U-69,593 at the kappa-opioid receptor of rat brain slices. The autoradiographic studies also demonstrated that [3H]DAMGO and [3H]DPDPE bindings on the rat brain slice were displaced by N3-(2',5'-DiMeOPhAc)AraU. These results indicate that N3-(2',5'-DiMeOPhAc)AraU interacts with mu- and delta-opioid receptors.
Shimizu
Tomomi
T
Department of Hygienic Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University, Ho-3, Kanagawa-machi, Kanazawa 920-1181, Japan.
Kimura
Toshiyuki
T
Funahashi
Tatsuya
T
Watanabe
Kazuhito
K
Ho
Ing Kang
IK
Yamamoto
Ikuo
I
D000701:Analgesics, Opioid / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D001086:Arabinofuranosyluracil / Q000031:analogs & derivatives* / Q000494:pharmacology; D001345:Autoradiography; D044482:Benzeneacetamides / Q000378:metabolism / Q000494:pharmacology; D001667:Binding, Competitive / Q000187:drug effects*; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)- / Q000378:metabolism / Q000494:pharmacology; D020881:Enkephalin, D-Penicillamine (2,5)- / Q000378:metabolism / Q000494:pharmacology; D007276:Injections, Intraventricular; D008024:Ligands; D008297:Male; D011759:Pyrrolidines / Q000378:metabolism / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D011957:Receptors, Opioid / Q000378:metabolism*; D017465:Receptors, Opioid, delta / Q000187:drug effects; D017473:Receptors, Opioid, kappa / Q000187:drug effects; D017450:Receptors, Opioid, mu / Q000187:drug effects
D000701:Analgesics, Opioid; D044482:Benzeneacetamides; D008024:Ligands; C528972:N3-(2',5 '-dimethoxyphenacyl)arabinofuranosyluracil; D011759:Pyrrolidines; D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D001086:Arabinofuranosyluracil; D020881:Enkephalin, D-Penicillamine (2,5)-; C045444:U 69593