2937. Detomidine

Nomenclature

CAS number: 76631-46-4
4-[(2,3-Dimethylphenyl)methyl]-1H-imidazole; 4-(2′,3′-dimethylbenzyl)imidazole.
C12H14N2; mol wt 186.25.
C 77.38%, H 7.58%, N 15.04%.

Description and references

α2-Adrenoceptor agonist with sedative and analgesic activity. Prepn: A. J. Karjalayne, K. O. A. Kurkela, EP 24829; eidem, US 4443466 (1981, 1984 both to Farmos). Physical studies: E. Laine et al., Acta Pharm. Suec. 20, 451 (1983). Crystal structure: L. H. J. Lajunen et al., ibid. 21, 163 (1984). Pharmacology: R. Virtanen, L. Nyman, Eur. J. Pharmacol. 108, 163 (1985); R. Virtanen, E. MacDonald, ibid. 115, 277 (1985). Mechanism of action: eidem, J. Vet. Pharmacol. Ther. 8, 30 (1985). Radioimmunoassay in biological samples: O. Vakkuri et al., Life Sci. 40, 1357 (1987). GC/MS determn in blood, plasma and urine: A. K. Singh et al., J. Chromatogr. 404, 223 (1987). Analgesic effects in horses: K. Sardari et al., J. Equine Vet. Sci. 25, 262 (2005).

Chemical structure

Properties

Crystals from acetone, mp 114-116°. LD50 i.v. in mice: 35 mg/kg (Karjalayne, Kurkela).

Derivative

Hydrochloride.

Nomenclature

CAS number: 90038-01-0
Dormosedan (Orion).
C12H14N2.HCl; mol wt 222.71.
C 64.72%, H 6.79%, N 12.58%, Cl 15.92%.

Properties

Crystals, mp 160°. Converts reversibly to monohydrate at room temp, 80% humidity. Sol in water.

Therapeutic Category (Veterinary)

Sedative and analgesic for horses and cattle.