Isolation and characterization of a fraction from brain that inhibits 1,4‐[3H]dihydropyridine binding and L‐type calcium channel current

FEBS Letters

Howard, A.D.¹  Janis, R.A.¹  Scriabine, A.¹  Shrikhande, A.V.¹  McCarthy, R.T.¹  Johnson, D.E.¹  Greguski, R.¹ 

[1] Institute for Preclinical Pharmacology, Miles Inc., 400 Morgan Lane, West Haven, CT 06516, USA

关键词: Endogenous ligand;    Modulator;    1;    4-Dihydropyridine;    Nitrendipine;    Ca2+ antagonist;    Receptor binding;    (Brain);    DHP;    1;    4-dihydropyridine-type Ca2+-channel antagonist;    FBI;    < 1 kDa inhibitory fraction from brain;    HPLC high-performance liquid chromatography;    MBP;    myelin basic protein;    SEC;    size exclusion chromatography;    TFA;    trifluoroacetic acid;   

DOI  :  10.1016/0014-5793(88)80923-2

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Bovine brain was subjected to acid extraction and several purification steps. A fraction from brain that eluted from C18 reverse-phase columns at 30–35% acetonitrile inhibited [³H]nitrendipine binding to cardiac membranes. Further purification of this fraction on a sizing column in the presence of 40% acetonitrile yielded a low molecular mass fraction (< 1 kDa) that produced a time- and voltage-dependent inhibition of L-type (but not T-type) Ca²⁺-channel current in GH₃ cells. The results suggest that this fraction contains an endogenous substance that binds directly to slowly-inactivating Ca²⁺ channels and thereby inhibits current flow.

【 授权许可】

Unknown