Bernhard Michel, Takeda Kenneth, Keller Caroline, Haslebacher Mirko, Lambrou George N, Trendelenburg Anne-Ulrike
DA Ophthalmology, Novartis Institutes for BioMedical Research, PO Box WSJ-386.746, 4002 Basel, Switzerland.
Naunyn Schmiedebergs Arch Pharmacol. 2004 Oct;370(4):305-13. doi: 10.1007/s00210-004-0972-z. Epub 2004 Sep 16.
Sympathetic neurotransmitter release and its modulation by presynaptic muscarinic heteroreceptors were studied in mouse iris-ciliary bodies. Tissue preparations were preincubated with (3)H-noradrenaline and then superfused and stimulated electrically. Firstly, experimental conditions were defined, allowing study of presynaptic sympathetic inhibition in mouse iris-ciliary body. If tissue was stimulated four times with 36 pulses/3 Hz, tritium overflow peaks were reliably and reproducibly measured. As expected, these stimulation conditions led to marked alpha(2)-autoinhibition as indicated by the release-enhancing effect of the alpha(2)-antagonists phentolamine and rauwolscine. To ensure autoinhibition-free (3)H-noradrenaline release, which is optimal for studying presynaptic sympathetic inhibition, alpha(2)-receptors were blocked in all subsequent experiments. Under these conditions, evoked tritium overflow was almost completely abolished in the presence of the sodium channel blocker tetrodotoxin, indicating a neuronal origin of (3)H-noradrenaline release. Secondly, muscarinic inhibition of (3)H-noradrenaline release was characterized using the conditions described above (36 pulses/3 Hz; phentolamine 1 muM and rauwolscine 1 muM throughout). The muscarinic receptor agonist oxotremorine M decreased evoked tritium overflow in a concentration-dependent manner with an IC(50) of 0.33 muM and maximal inhibition of 51%. The concentration-response curve of oxotremorine M was shifted to the right by the muscarinic antagonists ipratropium and methoctramine, whereas pirenzepine was ineffective. The observed rank order of antagonist potencies, ipratropium > methoctramine > pirenzepine, which is typical for the M(2) subtype, indicates that presynaptic muscarinic receptors on sympathetic axons of mouse iris-ciliary bodies are predominantly M(2). Finally, inhibition of (3)H-noradrenaline release by endogenously secreted acetylcholine was investigated. Longer pulse trains, 120 pulses/3 Hz and 600 pulses/5 Hz, were used and the cholinesterase inhibitor physostigmine was added to the superfusion medium to increase synaptic levels of endogenous acetylcholine. Under these conditions, ipratropium approximately doubled the evoked overflow of tritium, indicating that endogenously released acetylcholine can activate presynaptic muscarinic heteroreceptors. In conclusion, the present experiments establish measurement of the electrically induced release of (3)H-noradrenaline from mouse iris-ciliary bodies. As in other species, noradrenaline release in this preparation was subject to presynaptic muscarinic inhibition. Our results also indicate that the presynaptic muscarinic receptors on sympathetic axons in mouse iris-ciliary body are predominantly M(2). Moreover, these receptors can be activated by both exogenous agonists and endogenously released acetylcholine and, hence, may operate physiologically in the interplay between the parasympathetic and sympathetic nervous system.
在小鼠虹膜睫状体中研究了交感神经递质释放及其受突触前毒蕈碱异受体的调节。将组织标本与(3)H-去甲肾上腺素预孵育,然后进行灌流并给予电刺激。首先,确定了实验条件,以便研究小鼠虹膜睫状体中的突触前交感抑制。如果用36个脉冲/3赫兹对组织进行4次刺激,可可靠且可重复地测量到氚溢出峰值。如预期的那样,这些刺激条件导致了明显的α(2)-自身抑制,这可通过α(2)-拮抗剂酚妥拉明和萝芙木碱的释放增强作用来表明。为确保无自身抑制的(3)H-去甲肾上腺素释放,这对于研究突触前交感抑制是最佳的,在所有后续实验中均阻断了α(2)-受体。在这些条件下,在存在钠通道阻滞剂河豚毒素的情况下,诱发的氚溢出几乎完全被消除,这表明(3)H-去甲肾上腺素释放源于神经元。其次,使用上述条件(36个脉冲/3赫兹;全程使用1μM酚妥拉明和1μM萝芙木碱)对(3)H-去甲肾上腺素释放的毒蕈碱抑制进行了表征。毒蕈碱受体激动剂氧化震颤素M以浓度依赖性方式降低诱发的氚溢出,IC(50)为0.33μM,最大抑制率为51%。氧化震颤素M的浓度-反应曲线被毒蕈碱拮抗剂异丙托溴铵和甲奥克明向右移动,而哌仑西平无效。观察到的拮抗剂效力顺序为异丙托溴铵>甲奥克明>哌仑西平,这是M(2)亚型的典型特征,表明小鼠虹膜睫状体交感神经轴突上的突触前毒蕈碱受体主要是M(2)。最后,研究了内源性分泌的乙酰胆碱对(3)H-去甲肾上腺素释放的抑制作用。使用了更长的脉冲序列,即120个脉冲/3赫兹和600个脉冲/5赫兹,并将胆碱酯酶抑制剂毒扁豆碱添加到灌流培养基中以增加内源性乙酰胆碱的突触水平。在这些条件下,异丙托溴铵使诱发的氚溢出增加了约一倍,表明内源性释放的乙酰胆碱可激活突触前毒蕈碱异受体。总之,本实验建立了从小鼠虹膜睫状体电诱导释放(3)H-去甲肾上腺素的测量方法。与其他物种一样,该制剂中的去甲肾上腺素释放受到突触前毒蕈碱抑制。我们的结果还表明,小鼠虹膜睫状体交感神经轴突上的突触前毒蕈碱受体主要是M(2)。此外,这些受体可被外源性激动剂和内源性释放的乙酰胆碱激活,因此可能在副交感神经系统和交感神经系统的相互作用中发挥生理作用。