The effects of the alpha2-adrenergic receptor agonists clonidine and rilmenidine, and antagonists yohimbine and efaroxan, on the spinal cholinergic receptor system in the rat.
The effects of the alpha2-adrenergic receptor agonists clonidine and rilmenidine, and antagonists yohimbine and efaroxan, on the spinal cholinergic receptor system in the rat.
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α2-肾上腺素能受体激动剂可乐定和利美尼定以及拮抗剂育亨宾和依法罗生对大鼠脊髓胆碱能受体系统的影响。
DOI：
10.1111/j.1742-7843.2004.pto940401.x
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发表时间：
2004
影响因子：
3.1
通讯作者：
A. Höglund
中科院分区：
文献类型：
--
作者：
K. Abelson;A. Höglund
胆碱能激动剂通过增加脊髓内乙酰胆碱释放的机制产生脊髓抗伤害感受。胆碱能受体系统与其他几种受体类型相互作用，如α 2-肾上腺素能受体。为了充分了解这些相互作用，必须详细研究各种受体配体对胆碱能系统的影响。本研究旨在研究α 2-肾上腺素能受体激动剂可乐定和利美尼定以及α 2-肾上腺素能受体拮抗剂育亨宾和依法克生对大鼠脊髓胆碱能受体的影响。脊髓微透析被用来测量在体内的乙酰胆碱的变化后，管理的配体，与或没有烟碱受体阻滞剂。此外，还研究了配体对毒蕈碱和尼古丁受体的体外结合特性。结果发现，可乐定和利美尼定增加脊髓乙酰胆碱释放，而育亨宾减少。依法罗生对乙酰胆碱释放的影响因浓度不同而不同。烟碱受体阻断剂减弱了所有配体的作用。所有配体对毒蕈碱受体的结合亲和力均较差。另一方面，所有配体具有亲和力的烟碱受体。可乐定和育亨宾结合最适合于一个位点结合曲线，而利美尼定和依法克生最适合于两个位点结合曲线。本研究表明，测试的α 2-肾上腺素能受体配体影响脊髓内乙酰胆碱释放在大鼠体内诱发的烟碱受体机制，并在体外具有结合亲和力的烟碱受体。α 2-肾上腺素能受体配体与烟碱受体的结合可能影响乙酰胆碱的椎管内释放。
Cholinergic agonists produce spinal antinociception via mechanisms involving an increased release of intraspinal acetylcholine. The cholinergic receptor system interacts with several other receptor types, such as alpha2-adrenergic receptors. To fully understand these interactions, the effects of various receptor ligands on the cholinergic system must be investigated in detail. This study was initiated to investigate the effects of the alpha2-adrenergic receptor agonists clonidine and rilmenidine and the alpha2-adrenergic receptor antagonists yohimbine and efaroxan on spinal cholinergic receptors in the rat. Spinal microdialysis was used to measure in vivo changes of acetylcholine after administration of the ligands, with or without nicotinic receptor blockade. In addition, in vitro binding properties of the ligands on muscarinic and nicotinic receptors were investigated. It was found that clonidine and rilmenidine increased, while yohimbine decreased spinal acetylcholine release. Efaroxan affected acetylcholine release differently depending on concentration. Nicotinic receptor blockade attenuated the effect of all ligands. All ligands showed poor binding affinity for muscarinic receptors. On the other hand, all ligands possessed affinity for nicotinic receptors. Clonidine and yohimbine binding was best fit to a one site binding curve and rilmenidine and efaroxan to a two site binding curve. The present study demonstrates that the tested alpha2-adrenergic receptor ligands affect intraspinal acetylcholine release in the rat evoked by nicotinic receptor mechanisms in vivo, and that they possess binding affinity to nicotinic receptors in vitro. The binding of alpha2-adrenergic receptor ligands to nicotinic receptors might affect the intraspinal release of acetylcholine.
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影响因子：
6.1
作者：
Eisenach, JC
通讯作者：
Eisenach, JC
大鼠烟碱镇痛的肾上腺素能、血清素能和胆碱能成分。
DOI：
--
发表时间：
1993
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Iwamoto,ET;Marion,L
通讯作者：
Marion,L
影响因子：
3.6
作者：
Duttaroy, A;Gomeza, J;Wess, J
通讯作者：
Wess, J
影响因子：
9.8
作者：
Buerkle, H;Yaksh, TL
通讯作者：
Yaksh, TL
微透析氧化震颤素、卡巴胆碱、地巴替丁和东莨菪碱对大鼠脊柱内乙酰胆碱释放的影响。
DOI：
--
发表时间：
2000
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Höglund,AU;Hamilton,C;Lindblom,L
通讯作者：
Lindblom,L