The muscarinic receptor subtype in mouse pancreatic B‐cells

FEBS Letters

Henquin, J.C.¹  Nenquin, M.¹ 

[1] Unité de Diabétologie et Nutrition, UCL 54.74, University of Louvain, Faculty of Medicine, B-1200 Brussels, Belgium

关键词: Acetylcholine;    Muscarinic receptor;    Pirenzepine;    Insulin release;    Ion flux;    (Pancreatic islet);   

DOI  :  10.1016/0014-5793(88)80290-4

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Isolated mouse islets were used to identify the muscarinic receptor subtype present in pancreatic B-cells. We thus compared the inhibitory potencies of atropine (non-specific), of pirenzepine (specific for M₁ receptors) and of compound AF-DX 116 (specific for cardiac M₂ receptors) on acetylcholine-induced insulin release, ⁸⁶Rb⁺ efflux and ⁴⁵Ca²⁺ efflux. The three antagonists inhibited all effects of acetylcholine, but EC₅₀ values were markedly different: atropine = 1.5–5 nM, pirenzepine = 0.6–1.7 μM and AF-DX 116 = 1.7–11 μM. The results did not suggest that the various effects of ACh could result from the activation of different subtypes of receptors. It is concluded that muscarinic receptors of pancreatic B-cells belong to an M₂ subtype distinct from the cardiac M₂ receptors.

【 授权许可】

Unknown