Ipenoxazone

Ipenoxazone is a potent and centrally acting muscle relaxant.

Signaling Pathways >> Others >> Others

Research Areas >> Neurological Disease

Ipenoxazone is a potent and centrally acting muscle relaxant[1]. An intravenous injection of 2 mg/kg Ipenoxazone causes a reduction of electromyographic activity which reaches a maximum within 3 min after the injection. Within 1 min after the injection of Ipenoxazone at a dose of 4 mg/kg, the blood pressure changes from a control level of 138±9 mmHg to a minimum level of 98±9 mmHg (n=6) but it rapidly returns to the control level within 1 to 2 min, while the rigidity is still reduced significantly at that time. High doses (greater than 30 mg/kg i.p.) of Ipenoxazone produces a transient and dose-dependent sedation in almost all mice about 5 min after its administration[2].

Experiments are performed on 31 adult male rats (Wistar 310 to 430 g, 3 to 7 months of age) anesthetized with chloralose-urethane (50 and 500 mg/kg i.p., respectively). Ipenoxazone is administrated i.v. at 0.05 to 0.1 mL/100 g body weight (20 to 40 s per injection). These four different doses of Ipenoxazone (0.3, 1, 3 and 10 mg/kg) are administrated cumulatively, from small doses to larger doses. It is usually waited about 10 to 30 min between each trial or until all effects of the drug on the bladder have disappeared[1].

[1]. Kimura A, et al. Inhibitory effects of a new, potent, centrally acting muscle relaxant, (4S,5R)-4-(2-methylpropyl)-3-[3-(perhydroazepin-1-yl)propyl]-5- phenyl-1,3-oxazolidin-2-one (NC-1200) on micturition contractions of the bladder in rats. Eur J Pharmacol. 1988 Jul 26;152(1-2):55-62.

[2]. Masaki M, et al. A new class of potent centrally acting muscle relaxants: pharmacology of oxazolidinones in rat decerebrate rigidity. Br J Pharmacol. 1986 Sep;89(1):219-28.

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MOLECULAR FORMULA :

C22-H34-N2-O2

MOLECULAR WEIGHT :

358.58

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

38 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 13,455,1988