N3-phenacyluridine as a new type of antinociceptive compound in mice.
The antinociceptive activity of N3-phenacyluridine, a novel hypnotic, was examined with tail pinch, hot plate and acetic acid-induced abdominal constriction methods by intracerebroventricular (i.c.v.) injection to mice. In the first method, N3-phenacyluridine exerted antinociceptive activity after the i.c.v. injection at a dose of 0.5 micromol/mouse, although this activity was comparable to the activity of morphine (0.01 micromol/mouse, i.c.v.). In the second method, the activity of N3 -phenacyluridine was continued until 120 min after the injection at a dose of 0.5 micromol/mouse. In last, N3-phenacyluridine (0.1 micromol/mouse, i.c.v.) significantly decreased in the numbers of acetic acid-induced abdominal constriction as compared to the control (1% Tween 80 saline). The ED50 value of the antinociceptive activity of N3-phenacyluridine was 0.02 imol/mouse, i.c.v. The present paper demonstrated for the first time that N3-phenacyluridine belonging to oxopyrimidine nucleoside analogue possesses not only the hypnotic and sedative activities previously reported, but also antinociceptive activity.
Kimura
Toshiyuki
T
Department of Hygienic Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University, Ho-3, Kanagawa-machi, Kanazawa 920-1181, Japan.
Shimizu
Tomomi
T
Funahashi
Tatsuya
T
Nagakura
Mayumi
M
Watanabe
Kazuhito
K
Tachibana
Kuniomi
K
Kondo
Shigemi
S
Ho
Ing Kang
IK
Yamamoto
Ikuo
I
D019342:Acetic Acid / Q000633:toxicity; D000698:Analgesia; D000818:Animals; D006993:Hypnotics and Sedatives / Q000627:therapeutic use*; D007276:Injections, Intraventricular; D008297:Male; D051379:Mice; D010146:Pain / Q000209:etiology / Q000517:prevention & control*; D014529:Uridine / Q000031:analogs & derivatives
D006993:Hypnotics and Sedatives; D019342:Acetic Acid; D014529:Uridine