Evidence for prejunctional muscarinic autoreceptors in human and guinea pig trachea.
Evidence for prejunctional muscarinic autoreceptors in human and guinea pig trachea.
复制标题
人和豚鼠气管中交界前毒蕈碱自身受体的证据。
DOI：
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发表时间：
1995
影响因子：
24.7
通讯作者：
M. Belvisi
中科院分区：
文献类型：
--
作者：
H. Patel;P. Barnes;T. Takahashi;S. Tadjkarimi;M. Yacoub;M. Belvisi
功能研究表明，人体呼吸道胆碱能神经上存在前节突触前M受体。然而，这些研究是评估神经诱发的乙酰胆碱(ACh)释放变化的间接方法。通过比较M受体拮抗剂哌仑西平(M_1)、甲氧曲明(M_2)、4-DAMP(M_3)和利彭西平(M_1/M_3)对电场刺激(EFS)诱发的胆碱能神经收缩反应和[~H]ACh释放的影响，我们研究了人和豚鼠气管中M受体的存在。M1、M1/M3或M3拮抗剂以浓度依赖的方式抑制EFS引起的胆碱能收缩反应(4-DAMP>；rispenzepine>；pienzepine)，而美索曲明在低浓度(<；3微米)时促进这一反应。在ACh释放研究中，M3拮抗剂没有明显的作用，而哌仑西平、美索曲明和利培西平显著增加豚鼠气管ACh的释放。相反，M受体激动剂氧托莫林和非选择性拮抗剂异丙托溴铵显著抑制人气管ACh的释放，而M1、M1/M3或M3拮抗剂则不能显著增加人气管ACh的释放。这些数据表明，在人和豚鼠的气管中，胆碱能神经末梢上存在一种自身抑制受体。此外，异丙托溴铵在自身抑制受体上的作用可能会限制其在治疗阻塞性呼吸道疾病中的使用。
Functional studies suggest the presence of prejunctional muscarinic autoreceptors on cholinergic nerves in human airways. However, these studies are an indirect method of evaluating changes in neurally evoked acetylcholine (ACh) release. We have investigated the presence of muscarinic autoreceptors in human and guinea pig trachea by comparing the effects of the muscarinic receptor antagonists pirenzepine (M1), methoctramine (M2), 4-DAMP (M3), and rispenzepine (M1/M3) on cholinergic neural contractile responses evoked by electrical field stimulation (EFS) and [3H]ACh release. The M1, M1/M3, or M3 antagonists inhibited the EFS-evoked cholinergic contractile response in a concentration-dependent manner (4-DAMP > rispenzepine > pirenzepine), whereas methoctramine facilitated this response at low concentrations ( < 3 microM). In ACh release studies, the M3 antagonist had no significant effect, whereas pirenzepine, methoctramine, and rispenzepine significantly increased ACh release in guinea pig trachea. In contrast, ACh release was significantly inhibited by the muscarinic agonist oxotremorine M. Methoctramine and the nonselective antagonist ipratropium bromide, but not the M1, M1/M3, or M3 antagonists, significantly increased ACh release in human trachea. These data suggest the presence of an autoinhibitory receptor on cholinergic nerve terminals in human and guinea pig trachea. In addition, the action of ipratropium bromide at the autoinhibitory receptor may limit its use in the treatment of obstructive airways disease.
毒蕈碱受体亚型调节迷走神经刺激的支气管收缩。
DOI：
10.1152/jappl.1988.65.5.2144
发表时间：
1988
期刊：
Journal of applied physiology (Bethesda, Md. : 1985)
影响因子：
--
作者：
Bloom,JW;Baumgartener-Folkerts,C;Palmer,JD;Yamamura,HI;Halonen,M
通讯作者：
Halonen,M