General pharmacological properties of muroctasin
Kojima, H.; Hirohashi, M.; Kasai, Y.; Takasuna, K.; Fukumoto, C.; Akashi, A.
Arzneimittel-Forschung 38(7a): 1002-1009
1988
ISSN/ISBN: 0004-4172 PMID: 3190791 Document Number: 306735
General pharmacological effects of N2-[(N-acetylmuramoyl)-L-alanyl-D-isoglutaminyl]-N6-stearoyl-L-lysine MDP-Lys(L18), muroctasin) were examined and the following results were obtained. Central nervous system: MDP-Lys(L18) had no effect on behavior, spontaneous motor activity, electroshock- and chemoshock-induced convulsions, hexobarbital sleeping time, pain threshold (mice), conditioned avoidance response (rats) at a dose of 0.4 mg/kg, s.c. and EEG as well as spinal reflex (cats) at a dose of 0.4 mg/kg, i.v. It produced a significant elevation in body temperature (rabbits) at doses of 13 .mu.g/kg, s.c. and greater. Respiratory and cardiovascular system (dogs): MDP-Lys(L18) did not show any significant effect on respiratory and cardiovascular functions at a dose of 0.4 mg/kg i.v. Autonomic nervous system: MDP-Lys(L18) induced a miosis (rabbits) at doses of 13 .mu.g/kg s.c. and greater. It did not affect norepinephrine-induced pressor and acetylcholine-induced depressor responses (dogs) and contraction of the nictitating membrane induced by electrical stimulation (cats) at a dose of 0.4 mg/kg i.v. Smooth muscles: in the experiments using the isolated ileum, vas deferens, trachea (guinea pigs) and uterus (rats), MDP-Lys(L18) showed neither spasmogenic nor spasmolytic activity at a concentration of 4 .times. 10-6 g/ml. Gastrointestinal propulsion (mice), gastric mucosa, gastric emptying rate and gastric secretion (rats) were not affected by this drug at a dose of 0.4 mg/kg s.c. MDP-Lys(L18) did not influence gastrointestinal motility (dogs) at a dose of 0.4 mg/kg, i.v. Miscellaneous: MDP(L18) suppressed carrageenan-induced edema (rats) at doses of 0.13 mg/kg s.c. and greater. MDP-Lys (L18) showed no influence on the contraction of the anterior tibial muscle induced by electrical stimulation (rabbits) at a dose of 0.4 mg/kg i.v. and the corneal reflex (guinea pigs) at a concentration of 4 .times. 10-6 g/ml. MDP-Lys(L18) exerted a significant diuretic effect in rats at a dose of 0.4 mg/kg s.c.