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  • Title: Sulfonyliminoimidazolidines, a new class of oral hypoglycemic agents. 4. Toxicity and general pharmacology of 1-[p-[2-(crotonylamino)-ethyl]-phenylsulfonyl]-3-cyclohexy l-2-imino- imidazolidine (CGP 11 112).
    Author: Märki F, Büch O, Delini-Stula A, Kraetz J, Petermann H, Radeke E, Schweizer A, Thomann P, Truog A.
    Journal: Arzneimittelforschung; 1984; 34(3):247-52. PubMed ID: 6539603.
    Abstract:
    Results of a first segment of toxicity tests and general pharmacological investigations with 1-[p-[2-(crotonylamino)-ethyl]-phenylsulfonyl]-3-cyclohexyl- 2- iminoimidazolidine (CGP 11 112), a potent new oral hypoglycemic agent, are reported. The acute LD50 in rats was 600 mg/kg p.o. and 25 mg/kg i.v. In a range finding study doses of 60 mg/kg p.o. and 10 mg/kg i.p., administered daily for 10 days, were tolerated without symptoms in rats, and 30 mg/kg p.o. produced no unequivocal toxic effects in dogs. Slight and transient increases of blood pressure were observed in anaesthetized cats at doses of 0.3 mg/kg i.v. and above. 3 mg/kg i.v. (1/10 LD) caused a transient blood pressure decrease. Heart rate, tidal volume and blood pressure effects of epinephrine (adrenaline), norepinephrine (noradrenaline) and acetylcholine were not significantly influenced in a dose range from 0.01 to 1.0 mg/kg i.v. In isolated organ segments, CGP 11 112 produced only unspecific effects at high concentrations. No intrinsic activity, but antagonism against BaCl2-induced contractions were observed in isolated guinea-pig ileum (one third papaverine hydrochloride). Rate and force of contraction of isolated guinea-pig atria were not affected up to 2.4 mumol/l; higher concentrations were cardiodepressant. In rats, CGP 11 112 increased the excretion of urine, sodium and chloride, but not potassium, dose-dependently (range 10-100 mg/kg). Similar effects observed in dogs suggest that the compound may affect fluid and electrolyte balance at high doses. Moderate antiphlogistic activity (ED40 10-40 mg/kg) was observed in the carrageenin-induced rat paw oedema.(ABSTRACT TRUNCATED AT 250 WORDS)
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