Dolzhenko A T, Komissarov I V, Kharin N A
Biull Eksp Biol Med. 1989 Dec;108(12):684-6.
Experimenting on the slices of cortex and dorsal raphe nucleus of midbrain of rats which were incubated with 3H-hydroxytrypta-mine (3H-HT) studies showed the influence of series of serotonin agonists on the spontaneous and electrically stimulated release of 3H-HT from the slices. It was established that the serotonin in concentration of 10(-5) mol/l similarly inhibits the release of 3H-HT from the electrically stimulated slices of the brain cortex (78.6%) and on slices of the dorsal raphe nucleus of the midbrain (81.6%) had no effect on the spontaneous release of serotonin. The serotonin agonists in order of increasing ability to inhibit the electrically stimulated release of 3H-HT from the cortex slices is as follows: ipsapirone (0%), 8-OH-DPAT (23%), kampirone (26.5%), 1.2-PP (28.6%), kaplapirone (35.7%), buspirone (48%) and TFMPP (67%). On the ability to influence the release of 3H-HT from the electrically stimulated slices of the dorsal raphe nucleus of the midbrain of the rats serotonin agonists were in the following order: TEMPP (12.3%), kampirone (40%), 1.2-PP (42.9%), ipsapirone (52%), 8-OH-DPAT (54.1%), kampirone (57.2%) and buspirone (65.3%). It is suggested that the effect of both ipsapirone, kampirone and 8-OH-DPAT is greatly localized on the somato-dendritic synapses P1A-HT receptors, TEMPP is more on the terminal axons of HT-ergic neurones while kampirone, buspirone and active metabolite 1.2-PP act on the presynaptic and somatodendritic autoreceptors of serotonin.
在用3H - 羟色胺(3H - HT)孵育的大鼠大脑皮层和中脑背侧缝际核切片上进行的实验研究表明,一系列5 - 羟色胺激动剂对3H - HT从切片中的自发释放和电刺激释放有影响。已确定,浓度为10(-5) mol/l的5 - 羟色胺同样抑制大脑皮层电刺激切片中3H - HT的释放(78.6%),而对中脑背侧缝际核切片中3H - HT的释放(81.6%)没有影响,对5 - 羟色胺的自发释放也没有影响。按抑制大脑皮层切片中3H - HT电刺激释放能力增强的顺序,5 - 羟色胺激动剂如下:ipsapirone(0%)、8 - OH - DPAT(23%)、kampirone(26.5%)、1.2 - PP(28.6%)、kaplapirone(35.7%)、buspirone(48%)和TFMPP(67%)。就影响大鼠中脑背侧缝际核电刺激切片中3H - HT释放的能力而言,5 - 羟色胺激动剂的顺序如下:TEMPP(12.3%)、kampirone(40%)、1.2 - PP(42.9%)、ipsapirone(52%)、8 - OH - DPAT(54.1%)、kampirone(57.2%)和buspirone(65.3%)。有人提出,ipsapirone、kampirone和8 - OH - DPAT的作用主要定位于躯体 - 树突突触的P1A - HT受体,TEMPP更多作用于5 - 羟色胺能神经元的终末轴突,而kampirone、buspirone和活性代谢物1.2 - PP作用于5 - 羟色胺的突触前和躯体 - 树突自身受体。