Methyllycaconitine: a selective probe for neuronal α‐bungarotoxin binding sites

FEBS Letters

Lunt, G.G.¹  Wonnacott, S.¹  Ward, J.M.¹  Cockcroft, V.B.¹  Smillie, F.S.¹ 

[1] Department of Biochemistry, University of Bath, Bath BA2 7AY, UK

关键词: Methyllycaconitine;    Nicotinic receptor;    Brain α-bungarotoxin binding site;    Nicotinic pharmacophore;   

DOI  :  10.1016/0014-5793(90)81231-C

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

The ability of methyllycaconitine (MLA) to inhibit the binding of [¹²⁵I]α-bungarotoxin to rat brain membranes, frog and human muscle extracts and the human muscle cell line TE671 has been measured. MLA showed a markedly higher affinity for the rat brain site (K _i 1.4 × 10⁻⁹ M) than for the muscle receptors (K _i; 10⁻⁵-10⁻⁶ M). Structure modelling techniques were used to fit the structure of MLA to a nicotinic pharmacophore model. MLA is the first low molecular weight ligand to be shown to discriminate between muscle nicotinic receptors and their α-bungarotoxinbinding counterpart in the brain, and as such may be a useful structural probe for pursuing the structural and functional properties of the neuronal protein.

【 授权许可】

Unknown