新規抗癌剤DL-1-(γ-Chloropropyl)-2-chloromethylpiperidine Hydrobromideの薬理作用

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The pharmacological properties of DL-1-(γ-chloropropyl)-2-chloromethylpiperidine hydrobromide (CAP-2), a new nitrogen mustard type antitumor agent, were investigated in various experimental animals. The LD_<50> value by intraperitoneal single injection of CAP-2 was 60.0 mg/kg for female mice and 65.0 mg/kg for male mice 7 days after injection. Female and male received a maximum tolerated dose of 30 mg/kg and 25 mg/kg, respectively, of CAP-2 intraperitoneally once a day for 7 days. Decrease of spontaneous motalities, mild prolongation of sleeping time, hypothermia, and analgesic action were observed by intraperitoneal injection in mice of a dose of 30 mg/kg of CAP-2,but not at smaller doses. In the isolated large intestine of the guinea pig, a low concentration of CAP-2 caused relaxation and a decrease of activity which was antagonistic for acetylcholine, but not for barium chloride. Intestinal relaxation disappeared and changed to intestinal contraction by the repeated application of CAP-2 (1×10^<-4>g/ml). CAP-2 (1×10^<-4>g/ml) caused intestines relaxed by atropine to contract and increased their activity. This contraction was inhibited by paraverine. In the isolated heart of the frog, CAP-2 showed a negative inotropic action and a concentration of 1×10^<-4>g/ml inhibited the diastric standstill by acetylcholine. CAP-2 did not affect femoral vessel flow in the frog even at a concentration of 3×10^<-2>g/ml. CAP-2 tended to contract the rectus abdominis muscle of the frog. In the rabbit, CAP-2 (1-5mg/kg, i.v.) exhibited a temporary hypotensive action and weak respiratory stimulation. From these results, it was confirmed that CAP-2 has a depressant effect on the central nervous system and an anticholinergic action on the peripheria.
社団法人日本薬学会の論文
1980-03-25

新規抗癌剤DL-1-(γ-Chloropropyl)-2-chloromethylpiperidine Hydrobromideの薬理作用

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