9485. Tizanidine
Nomenclature
CAS number: 51322-75-9
5-Chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-2,1,3-benzothiadiazol-4-amine; 5-chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole. C9H8ClN5S; mol wt 253.71.
C 42.61%, H 3.18%, Cl 13.97%, N 27.60%, S 12.64%.
Description and references
α2-Adrenergic agonist; centrally active myotonolytic. Prepn and antitremor activity: P. Neumann, NL 7306228; eidem, US 3843668 (1973, 1974 both to Wander-Sandoz). Pharmacology: A. C. Sayers et al., Arzneim.-Forsch. 30, 793 (1980); and mechanism of action studies: L. Turski et al., Brain Res. 379, 367 (1986); H. Ono et al., Gen. Pharmacol. 17, 137 (1986). Pharmacokinetics: V. Heazlewood et al., Eur. J. Clin. Pharmacol. 25, 65 (1983). Clinical evaluation in spasticity of multiple sclerosis: P. M. Newman et al., ibid. 23, 31 (1982); M. C. Hoogstraten et al., Acta Neurol. Scand. 77, 224 (1988).
Properties
Crystals from methanol, mp 221-223°. LD50 orally in mice: 235 mg/kg (Sayers).Derivative
Hydrochloride.Nomenclature
CAS number: 64461-82-1
AB-021; DS-103-282; Sirdalud (Novartis); Ternelin (Novartis); Zanaflex (Athena). C9H8ClN5S.HCl; mol wt 290.17.
C 37.25%, H 3.13%, Cl 24.44%, N 24.14%, S 11.05%.
Therapeutic Category
Muscle relaxant (skeletal).
Keywords
Muscle Relaxant (Skeletal)