Binding of specific ligands to muscarinic receptors alters the fluidity of membrane fragments from rat brain A fluorescence polarization study with lipid‐specific probes

FEBS Letters

Bergelson, L.D.¹  Molotkovsky, J.G.¹  Köiv, A.²  Manevich, E.M.³  Järv, J.² 

[1] Shemyakin Institute of Bioorganic Chemistry, USSR Academy of Sciences, Moscow, USSR;Tartu State University, Tartu, Estonian SSR, USSR;Semashko Medical Stomatological Institute, Moscow, USSR

关键词: Muscarinic receptor;    Atropine;    Carbachol;    Fluorescence;    Membrane fluidity;   

DOI  :  10.1016/0014-5793(88)80282-5

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

The previously suggested method of following ligand-receptor interactions by measuring ligand-induced changes in membrane fluidity [(1986) FEBS Lett. 194, 313–316] was employed to study the binding of specific ligands of the muscarinic receptor to rat brain membrane fragments containing a fluorescent analogue of phosphatidylcholine (APC) as a membrane probe. Upon addition of carbachol and atropine in low concentrations the fluorescence polarization of the APC-labeled membranes decreased significantly demonstrating that binding of these ligands to the muscarinic receptor increases the fluidity of its lipid environment. The fluidity changes were specific, concentration-dependent and saturable. In comparison with radioligand assays the fluorescent lipid probe method proved to be much more sensitive but the K _d values obtained by the two methods differed considerably.

【 授权许可】

Unknown