Comparison of α-adrenoceptor involvement in the antinociceptive action of tizanidine and clonidine in the mouse

Tsutomu Kameyama, Toshitaka Nabeshima, Kiyoshi Matsuno, Akira Sugimoto

Research output: Contribution to journalArticle

31 Citations (Scopus)

Abstract

The effect of drugs that influence the opioidergic and monoaminergic neuronal systems on the antinociceptive action of tizanidine [5-chloro-4-(2-imidazolin-2-yl-amino)-2,1,3-benzothiodiazole] was compared with their effect on the action of clonidine. The potency of the clonidine-induced antinoceptive action was 1.83 and 7.75 times greater than that of tizanidine in the tail-flick and acetic acid-induced writhing tests, respectively. The action of tizanidine and clonidine was completely antagonized by pretreatment with yohimbine, an α2-adrenoceptor blocker, but not by prazosin, an α1-adrenoceptor blocker. Other α1-adrenoceptor blockers, phenoxybenzamine and phentolamine, also attenuated the action of tizanidine and clonidine but the potency of these drugs was less than that of yohimbine. An opioid antagonist (naloxone), drugs influencing the serotonergic neuronal system (p-chlorophenylalanine, 5,6-dihydroxytryptamine, cyproheptadine), drugs influencing the catecholaminergic system (α-methyl-p-tyrosine, diethyl-dithiocarbamate, 6-hydroxydopamine, haloperidol) showed no effect on the action of tizanidine and clonidine. From these results, it appears that α2-adrenoceptors might be of importance in mediating the tizanidine and clonidine antinociceptive action in the tail-flick test.

Original languageEnglish
Pages (from-to)257-264
Number of pages8
JournalEuropean Journal of Pharmacology
Volume125
Issue number2
DOIs
Publication statusPublished - 17-06-1986
Externally publishedYes

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Clonidine
Adrenergic Receptors
Yohimbine
Tail
5,6-Dihydroxytryptamine
Pharmaceutical Preparations
Fenclonine
Serotonin Agents
Cyproheptadine
Phenoxybenzamine
Narcotic Antagonists
Prazosin
Phentolamine
Oxidopamine
Haloperidol
Naloxone
Acetic Acid
Tyrosine
tizanidine

All Science Journal Classification (ASJC) codes

  • Pharmacology

Cite this

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abstract = "The effect of drugs that influence the opioidergic and monoaminergic neuronal systems on the antinociceptive action of tizanidine [5-chloro-4-(2-imidazolin-2-yl-amino)-2,1,3-benzothiodiazole] was compared with their effect on the action of clonidine. The potency of the clonidine-induced antinoceptive action was 1.83 and 7.75 times greater than that of tizanidine in the tail-flick and acetic acid-induced writhing tests, respectively. The action of tizanidine and clonidine was completely antagonized by pretreatment with yohimbine, an α2-adrenoceptor blocker, but not by prazosin, an α1-adrenoceptor blocker. Other α1-adrenoceptor blockers, phenoxybenzamine and phentolamine, also attenuated the action of tizanidine and clonidine but the potency of these drugs was less than that of yohimbine. An opioid antagonist (naloxone), drugs influencing the serotonergic neuronal system (p-chlorophenylalanine, 5,6-dihydroxytryptamine, cyproheptadine), drugs influencing the catecholaminergic system (α-methyl-p-tyrosine, diethyl-dithiocarbamate, 6-hydroxydopamine, haloperidol) showed no effect on the action of tizanidine and clonidine. From these results, it appears that α2-adrenoceptors might be of importance in mediating the tizanidine and clonidine antinociceptive action in the tail-flick test.",
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Comparison of α-adrenoceptor involvement in the antinociceptive action of tizanidine and clonidine in the mouse. / Kameyama, Tsutomu; Nabeshima, Toshitaka; Matsuno, Kiyoshi; Sugimoto, Akira.

In: European Journal of Pharmacology, Vol. 125, No. 2, 17.06.1986, p. 257-264.

Research output: Contribution to journalArticle

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