Telenzepine-sensitive muscarinic receptors on rat pancreatic acinar cells.
Telenzepine-sensitive muscarinic receptors on rat pancreatic acinar cells.
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大鼠胰腺腺泡细胞上的替仑西平敏感毒蕈碱受体。
DOI：
10.1152/ajpgi.1998.274.4.g734
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发表时间：
1998
期刊：
影响因子：
--
通讯作者：
Gorelick,FS
中科院分区：
文献类型：
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作者：
Schmid,SW;Modlin,IM;Tang,LH;Stoch,A;Rhee,S;Nathanson,MH;Scheele,GA;Gorelick,FS
为了确定存在于大鼠胰腺腺泡细胞上的毒蕈碱亚型，我们研究了不同的毒蕈碱受体拮抗剂对离体大鼠胰腺腺泡中淀粉酶分泌和蛋白水解酶原加工的影响。最大酶原加工所需的卡巴胆碱浓度（10− 3 M）比最大淀粉酶分泌所需的浓度（10− 5 M）高10- 100倍。尽管M3拮抗剂4-二苯乙酰氧基-N-甲基-哌啶（4-DAMP）抑制分泌和转化（50%抑制分别为6 × 10− 7 M和1 × 10− 8 M），但最有效的抑制剂是M1拮抗剂替仑西平（50%抑制分别为5 × 10− 10 M和1 × 10− 11 M）。另一种M1拮抗剂哌仑西平和M2拮抗剂甲基辛四明在浓度高达1 × 10− 5 M时，并不减少淀粉酶分泌或酶原加工。通过PCR分析腺泡细胞毒蕈碱受体显示M1和M3亚型的表达。胰腺腺泡细胞在淀粉酶分泌和酶原转化方面具有不同的毒蕈碱拮抗剂敏感性模式（替仑西平β 4-DAMP >哌仑西平）。
To identify the muscarinic subtype present on the rat pancreatic acinar cell, we examined the effects of different muscarinic receptor antagonists on amylase secretion and proteolytic zymogen processing in isolated rat pancreatic acini. Maximal zymogen processing required a concentration of carbachol 10- to 100-fold greater (10−3M) than that required for maximal amylase secretion (10−5M). Although both secretion and conversion were inhibited by the M3 antagonist 4-diphenylacetoxy-N-methyl-piperidine (4-DAMP) (50% inhibition ∼6 × 10−7M and 1 × 10−8M, respectively), the most potent inhibitor was the M1 antagonist telenzepine (50% inhibition ∼5 × 10−10M and 1 × 10−11M, respectively). Pirenzepine, another M1 antagonist, and the M2 antagonist methoctramine did not reduce amylase secretion or zymogen processing in concentrations up to 1 × 10−5M. Analysis of acinar cell muscarinic receptor by PCR revealed expression of both m1 and m3 subtypes. The pancreatic acinar cell has a distinct pattern of muscarinic antagonist sensitivity (telenzepine ≫ 4-DAMP > pirenzepine) with respect to both amylase secretion and zymogen conversion.