Involvement of imidazoline receptors in the centrally acting muscle-relaxant effects of tizanidine.

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Eur J Pharmacol. 2002 Jun 12;445(3):187-93.
Involvement of imidazoline receptors in the centrally acting muscle-relaxant effects of tizanidine.

Honda M, Sekiguchi Y, Sato N, Ono H.

Laboratory of CNS Pharmacology, Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Japan.

The centrally acting muscle relaxant tizanidine has an imidazoline structure and binds not only to alpha(2)-adrenoceptors but also to imidazoline receptors. The role of imidazoline receptors in the muscle-relaxant effect of tizanidine was studied using the alpha(2)-adrenoceptor/imidazoline receptor antagonist idazoxan and the alpha(2)-adrenoceptor antagonist yohimbine. Tizanidine decreased the spinal mono- and polysynaptic reflexes in intact rats, and the inhibitory effects were antagonized by idazoxan but not by yohimbine. After pretreatment with prazosin, tizanidine decreased the mono- and polysynaptic reflexes in spinalized rats. While yohimbine partly inhibited tizanidine-induced depression of the polysynaptic reflex, idazoxan completely abolished tizanidine-induced depression of spinal reflexes. Furthermore, tizanidine-induced muscle relaxation in the traction test was significantly inhibited by idazoxan but not by yohimbine. From these results, it is suggested that imidazoline receptors, but not alpha(2)-adrenoceptors, are involved in the supraspinal inhibitory effects of tizanidine on spinal reflexes, and at the spinal level, alpha(2)-adrenoceptors and imidazoline receptors are involved in the inhibitory effects of tizanidine.

online pharmacy ref. source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12079683&dopt=Abstract

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