Maĭsov N I, Baĭmanov T D, Burov Iu V
Biull Eksp Biol Med. 1991 Aug;112(8):164-6.
Comparative study of the uptake of 3H-epinephrine (3H-EN) and 3H-norepinephrine (3H-NE) into rat brain crude synaptosomes and effect of psychotropic drugs of different classes on this process showed that isolated nerve terminals had their own transport system for EN. The crude synaptosomal fraction had two transport system's for EN; high-specific active uptake with high affinity (KM = 3.7 + 0.21 microM) and low-affinity uptake (KM2 = 98.0 + 47.5 microM). En accumulation was saturable, stereo-specific and inhibited by ouabain (3 X 10(-3) M), protoveratrine A and B (10(-4) M), NaN3 (2 X 10(-3) M), 2,4-dinitrophenol (2 X 10(-3) M), p-chloromercuribenzoate (10(-4) M). Actinomycin D had no effect on the uptake of 3H-EN. 3H-HE was accumulated by two uptake system: 1-high affinity uptake system with KM values of 0.49 + 0.13 microM, 2-low affinity uptake system with KM values of 21.1 + 7.71 microM. Amphetamine, mesocarb, chlorpromazine, fluphenazine and haloperidol were equally effective inhibitors of 3H-EN and 2H-HE uptake. Imipramine, phenazepam, diazepam and carbamazepine (5 X 10(-5) M) had no effect on the uptake of 3H-NE. Imipramine, zimelidine, norzimelidine and viloxazine (5 X 10(-5) M) were more potent inhibitors of the 3H-EN uptake than that of 3H-NE.
对3H-肾上腺素(3H-EN)和3H-去甲肾上腺素(3H-NE)摄取到大鼠脑粗突触体中的情况以及不同类精神药物对该过程的影响进行的比较研究表明,分离的神经末梢具有自身的EN转运系统。粗突触体部分有两个EN转运系统;具有高亲和力(KM = 3.7 + 0.21 microM)的高特异性活性摄取和低亲和力摄取(KM2 = 98.0 + 47.5 microM)。EN的积累是可饱和的、立体特异性的,并受到哇巴因(3×10(-3) M)、原藜芦碱A和B(10(-4) M)、NaN3(2×10(-3) M)、2,4-二硝基苯酚(2×10(-3) M)、对氯汞苯甲酸(10(-4) M)的抑制。放线菌素D对3H-EN的摄取没有影响。3H-HE通过两个摄取系统积累:1- KM值为0.49 + 0.13 microM的高亲和力摄取系统,2- KM值为21.1 + 7.71 microM的低亲和力摄取系统。苯丙胺、美索卡、氯丙嗪、氟奋乃静和氟哌啶醇是3H-EN和2H-HE摄取的同等有效抑制剂。丙咪嗪、非那西泮、地西泮和卡马西平(5×10(-5) M)对3H-NE的摄取没有影响。丙咪嗪、齐美利定、去甲齐美利定和维洛沙嗪(5×10(-5) M)对3H-EN摄取的抑制作用比对3H-NE的更强。