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The antinociceptive activity of guanabenz, a new potent antihypertensive agent, and its interaction with alpha-adrenoceptors or opiate receptors, with particular reference to clonidine and morphine, were studied. Guanabenz, clonidine and morphine were found to possess a dose-dependent antinociceptive activity in mice and rats. In the tail flick assay, the antinociceptive activity of guanabenz and clonidine was antagonized by yohimbine but not by naloxone or phenoxybenzamine. Guanabenz, clonidine and morphine caused a concentration-dependent inhibition of the twitch response of transmurally stimulated guinea-pig ileum longitudinal muscle. Phentolamine and yohimbine reversed the twitch-inhibitory effects of guanabenz and clonidine, but naloxone failed to reverse this action. Guanabenz and low doses of clonidine caused locomotor hypoactivity. This action of both drugs was affected by yohimbine but not by phenoxybenzamine. In contrast, a high dose of clonidine caused locomotor hyperactivity which was affected by phenoxybenzamine but not by yohimbine. These results suggest that the antinociceptive activity of guanabenz, as in the case of clonidine, may be mediated by the activation of alpha 2-adrenoceptors and be independent from opiate receptors.
H Sakamoto, and
K Inoue, and
T Murata, and
S Kohno, and
K Ohata
January 1979,
Zahn-, Mund-, und Kieferheilkunde mit Zentralblatt,
H Sakamoto, and
K Inoue, and
T Murata, and
S Kohno, and
K Ohata
October 1974,
Immunitat und Infektion,
H Sakamoto, and
K Inoue, and
T Murata, and
S Kohno, and
K Ohata
September 1979,
European journal of pharmacology,
H Sakamoto, and
K Inoue, and
T Murata, and
S Kohno, and
K Ohata
October 1978,
Nihon yakurigaku zasshi. Folia pharmacologica Japonica,
H Sakamoto, and
K Inoue, and
T Murata, and
S Kohno, and
K Ohata
January 1979,
Seishin shinkeigaku zasshi = Psychiatria et neurologia Japonica,
H Sakamoto, and
K Inoue, and
T Murata, and
S Kohno, and
K Ohata
September 1977,
Blut,
H Sakamoto, and
K Inoue, and
T Murata, and
S Kohno, and
K Ohata
April 1987,
Experimental neurology,
H Sakamoto, and
K Inoue, and
T Murata, and
S Kohno, and
K Ohata
January 1981,
Polski przeglad radiologii i medycyny nuklearnej,
H Sakamoto, and
K Inoue, and
T Murata, and
S Kohno, and
K Ohata
January 1950,
American review of tuberculosis,
H Sakamoto, and
K Inoue, and
T Murata, and
S Kohno, and
K Ohata
November 1981,
Yao xue xue bao = Acta pharmaceutica Sinica,
