Kobayashi H, Yuyama A, Shioya K, Sato K
Nihon Juigaku Zasshi. 1989 Aug;51(4):789-95. doi: 10.1292/jvms1939.51.789.
O-sec-butylphenyl methylcarbamate (BPMC), an anticholinesterase carbamate, was injected once (100 mg/kg, s.c.) or repeatedly (50 mg/kg/day for 10 days) into mice. Animals were examined for their behavior and for parameters of cholinergic activity in the forebrain. Mice that received only a single injection exhibited reduced ambulation, hypothermia, and impairment of rotarod performance for up to 3 hr after a single injection. BPMC increased levels of acetylcholine (ACh) in the forebrain for up to 6 hr, and decreased acetylcholinesterase (AChE) activity for up to 24 hr. Both high-affinity choline uptake (HACU) and binding of [3H]quinuclidinyl benzilate (QNB) were reduced 20 min after a single injection without any effect on choline acetyltransferase (ChAT) activity. In behavioral tests conducted 10 min prior to the daily injections, rotarod performance and ambulation were slightly impaired for a few days before and after cessation of injection. Repeated treatment decreased HACU and binding of [3H]QNB for 24 hr after the final injection without any changes in levels of ACh content, AChE activity and ChAT activity. BPMC may reversibly impair cholinergic functions through effects not only on AChE activity but also on HACU and binding of [3H]QNB.
O-仲丁基苯基甲基氨基甲酸酯(BPMC),一种抗胆碱酯酶氨基甲酸酯,以单次注射(100毫克/千克,皮下注射)或重复注射(50毫克/千克/天,共10天)的方式注入小鼠体内。对动物的行为以及前脑胆碱能活性参数进行检测。仅接受单次注射的小鼠在单次注射后长达3小时内表现出活动减少、体温过低以及转棒试验表现受损。BPMC在前脑使乙酰胆碱(ACh)水平升高长达6小时,并使乙酰胆碱酯酶(AChE)活性降低长达24小时。单次注射20分钟后,高亲和力胆碱摄取(HACU)以及[3H]喹核醇基苯甲酸酯(QNB)的结合均降低,而对胆碱乙酰转移酶(ChAT)活性无任何影响。在每日注射前10分钟进行的行为测试中,在注射停止前后的几天里,转棒试验表现和活动均略有受损。重复治疗在最后一次注射后24小时内降低了HACU以及[3H]QNB的结合,而ACh含量、AChE活性和ChAT活性水平无任何变化。BPMC可能不仅通过对AChE活性的影响,还通过对HACU以及[3H]QNB结合的影响来可逆地损害胆碱能功能。