Tempesta E, Janiri L, Pirrongelli C
Neuropharmacology. 1985 Jan;24(1):43-50. doi: 10.1016/0028-3908(85)90094-2.
Acetylcarnitine is an endogenous substance, active in the CNS, but its exact role in neurotransmission is still unknown. The present study was made to analyze by means of iontophoretic administration on single neurones of the medullary-pontine reticular formation in the rat the effects of the D- and L-acetylcarnitine on spontaneous and glutamate-evoked firing and on responses to applications of some other putative transmitters, such as acetylcholine, 5-hydroxytryptamine (5-HT), gamma-aminobutyric acid (GABA) and noradrenaline. L-Acetylcarnitine increased both spontaneous and evoked discharges, and potentiated cholinergic and serotonergic responses. The D-isomer was found to be almost ineffective. Neuronal responses to L-acetylcarnitine were reduced by dihydro-beta-erythroidine and enhanced by eserine, while atropine was ineffective. L-Acetylcarnitine increased both excitatory and inhibitory responses to 5-HT and its effect on the increase in firing rate induced by serotonergic drugs was reduced by dihydro-beta-erythroidine, but not by atropine. L- and D-Acetylcarnitine did not affect GABAergic or noradrenergic transmission. These results suggest a stereospecific facilitatory action of acetylcarnitine on neuronal responses to acetylcholine and 5-HT. It is hypothesized that this action could be exerted at a presynaptic level, at least with regard to serotonergic-induced responses, and that nicotinic receptors may be involved in the synaptic mechanism of release or reuptake of both acetylcholine and 5-HT.
乙酰肉碱是一种内源性物质,在中枢神经系统中具有活性,但其在神经传递中的确切作用尚不清楚。本研究旨在通过离子电渗法给药,分析D-和L-乙酰肉碱对大鼠延髓-脑桥网状结构单个神经元的自发放电和谷氨酸诱发放电的影响,以及对应用其他一些假定递质(如乙酰胆碱、5-羟色胺(5-HT)、γ-氨基丁酸(GABA)和去甲肾上腺素)的反应。L-乙酰肉碱增加了自发放电和诱发放电,并增强了胆碱能和5-羟色胺能反应。发现D-异构体几乎无效。二氢-β-刺桐啶可降低神经元对L-乙酰肉碱的反应,毒扁豆碱可增强该反应,而阿托品则无效。L-乙酰肉碱增加了对5-HT的兴奋性和抑制性反应,其对5-羟色胺能药物诱导的放电率增加的影响可被二氢-β-刺桐啶降低,但不能被阿托品降低。L-和D-乙酰肉碱不影响GABA能或去甲肾上腺素能传递。这些结果表明乙酰肉碱对神经元对乙酰胆碱和5-HT的反应具有立体特异性促进作用。据推测,至少就5-羟色胺能诱导的反应而言,这种作用可能在突触前水平发挥,并且烟碱样受体可能参与乙酰胆碱和5-HT释放或再摄取的突触机制。