Lakhe M, Furukawa Y, Yonezawa T, Nagashima Y, Hirose M, Chiba S
Department of Pharmacology, Shinshu University School of Medicine, Matsumoto, Japan.
Jpn J Pharmacol. 1996 Aug;71(4):333-5. doi: 10.1254/jjp.71.333.
We investigated the effects of U-92032 ((7-((bis-4-fluorophenyl) methyl)-1-piperazinyl)-2-2(2-hydroxyethylamino)-4-(1-methylethyl)- 2,4, 6-cycloheptatrien-1-one), a novel T-type Ca2+ channel blocker, on sinus rate and atrial contractile force in the isolated, blood-perfused atrium of the dog. U-92032 (1 to 300 nmol) induced negative chronotropic and inotropic responses in a dose-dependent manner, and the percentage decrease in sinus rate was less than that in atrial contractile force. Atropine did not affect the negative responses to U-92032. These results suggest that U-92032, a T-type Ca2+ channel blocker, simultaneously decreases the sinus rate and atrial force as do L-type Ca2+ channel blockers in the isolated dog atrium.
我们研究了新型T型钙通道阻滞剂U-92032（(7-((双-4-氟苯基)甲基)-1-哌嗪基)-2-(2-羟乙基氨基)-4-(1-甲基乙基)-2,4,6-环庚三烯-1-酮）对犬离体血液灌注心房的窦性心率和心房收缩力的影响。U-92032（1至300纳摩尔）以剂量依赖方式引起负性变时性和变力性反应，窦性心率的降低百分比小于心房收缩力的降低百分比。阿托品不影响对U-92032的负性反应。这些结果表明，T型钙通道阻滞剂U-92032在犬离体心房中与L型钙通道阻滞剂一样，同时降低窦性心率和心房力。
