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首页> 外文期刊>Journal of pharmacology & toxicology. >Effects of Sedative Agent JM-1232(-) ((-)-3-(2-(4-methyl-l-piperazinyl)-2-oxoethyl)-2-phenyl-3,5,6,7-tetrahydrocyclopenta(flisoindole-l(2H)-one) on the Carotid Arteries of Rats
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Effects of Sedative Agent JM-1232(-) ((-)-3-(2-(4-methyl-l-piperazinyl)-2-oxoethyl)-2-phenyl-3,5,6,7-tetrahydrocyclopenta(flisoindole-l(2H)-one) on the Carotid Arteries of Rats

机译:镇静剂JM-1232( - )(( - ) - 3-(2-甲基 - 哌嗪基)-2-氧乙基)-2-苯基-3,5,6,7-四氢环戊基(Flisoindole -L(2H) - 大鼠颈动脉

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In the present study, we investigate whether JM-1232(-) ((-)-3-[2-(4-methyl-l-piperazinyl)-2-oxoethyl]-2-phenyl-3,5,6,7-tetrahydrocyclopenta[fJisoindole-1 (2H)-one) affects vessels directly or indirectly. We examined the effects of JM-1232(-) with several antagonists on rat carotid arteries using the Magnus method. JM-1232 (-) suppressed contraction non-specifically on norepinephrine, potassium chloride and calcium chloride at a high concentration (E_max: 10~-5-10~-4 M). There were no significant change in each pretreated group consisting of flumazenil, propranolol, atropine, cimetidine, imetit and N(omega)-nitro-L-arginine methyl ester, whereas a significant suppression was observed (p<0.05) in PK11195 (50% inhibition concentration (IC_50): 3.2+-0.9 (xl0~-5) M) and diphenhydramine (IC_50: 5.6+-1.7 (x10~-5) M).
机译:在本研究中,我们研究了JM-1232( - )(( - ) - 3- [2-(4-甲基-1-哌嗪基)-2-氧乙基] -2-苯基-3,5,6,7 -TeTrahydocyclopenta [Fjisoindole-1(2h)-one)直接或间接影响血管。 我们使用MAGNUS方法检查了JM-1232( - )在大鼠颈动脉上的几种拮抗剂的影响。 JM-1232( - )以高浓度(E_max:10〜5-10〜-4m)抑制了非特异性的脱碱基,氯化钾和氯化钙的收缩。 每种预处理组没有显着的变化,包括氟喹啉,普萘洛尔,阿托品,西咪替丁,IMetit和N(Omega) - Nitro-L-精氨酸甲酯,而PK11195中观察到显着抑制(P <0.05)(50% 抑制浓度(IC_50):3.2 + -0.9(XL0〜-5)m)和二苯络胺(IC_50:5.6 + -1.7(x10〜-5)m)。

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