Freedman R, Hoffer B J
J Neurobiol. 1975 May;6(3):277-88. doi: 10.1002/neu.480060304.
Phenothiazine derivatives were examined as potential antagonists of the inhibitory noradrenergic synapses from the nucleus locus coeruleus to rat cerebellar Purkinje cells. Fluphenazine, and its thioxanthine analogue, flupenthixol, antagonized the inhibitory action of norepinephrine, when iontrophoretically applied to single cells. Alpha-flupenthixol was generally more active than the beta isomer. Fluphenazine had no appreciable effect on inhibitions induced by iontophoresis of GABA or cyclic AMP. Parenteral fluphenazine also blocked the inhibition of Purkinje cells produced by the stimulation of the noradrenergic pathway from locus coeruleus, but basket and stellate cell inhibitory inputs to Purkinje cells were unaffected. These data suggest that fluphenazine can specifically block a known central adrenergic inhibitory pathway.
对吩噻嗪衍生物作为从蓝斑核到大鼠小脑浦肯野细胞的抑制性去甲肾上腺素能突触的潜在拮抗剂进行了研究。当离子电渗法应用于单细胞时，氟奋乃静及其硫杂蒽类似物三氟噻吨拮抗了去甲肾上腺素的抑制作用。α-三氟噻吨通常比β异构体更具活性。氟奋乃静对由γ-氨基丁酸（GABA）或环磷酸腺苷（cAMP）离子电渗诱导的抑制没有明显影响。胃肠外给予氟奋乃静也阻断了刺激蓝斑核的去甲肾上腺素能通路所产生的浦肯野细胞抑制，但浦肯野细胞的篮状细胞和星状细胞抑制性输入不受影响。这些数据表明，氟奋乃静可以特异性地阻断已知的中枢肾上腺素能抑制通路。
