Labeling of neuropeptide Y receptors in SK-N-MC cells using the novel, nonpeptide Y sub(1) receptor-selective antagonist [ super(3)H]BIBP3226

The binding of tritium-labelled BIBP3226, N super(2)-(diphenylacetyl)-N-[(4-hydroxy-phenyl) methyl]-D-arginine amide, to human neuroblastoma SK-N-MC cells was investigated. [ super(3)H]BIBP3226 reversibly binds to neuropeptide Y receptors of the Y sub(1) subtype expressed in SK-N-MC cells with a K s...

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Bibliographic Details
Published in:European journal of pharmacology 1995-01, Vol.278 (3), p.239-242
Main Authors: Entzeroth, M, Braunger, H, Eberlein, W, Engel, W, Rudolf, K, Wienen, W, Wieland, HA, Willim, K D, Doods, H N
Format: Article
Language:English
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Summary:The binding of tritium-labelled BIBP3226, N super(2)-(diphenylacetyl)-N-[(4-hydroxy-phenyl) methyl]-D-arginine amide, to human neuroblastoma SK-N-MC cells was investigated. [ super(3)H]BIBP3226 reversibly binds to neuropeptide Y receptors of the Y sub(1) subtype expressed in SK-N-MC cells with a K sub(D) of 2.1 plus or minus 0.3 nM (mean plus or minus S.E.M., n = 3) and a B sub(max) of 58400 plus or minus 1100 sites/cell. Non-specific binding did not exceed 30% of the total radioactivity bound at K sub(D). In competition experiments [ super(3)H]BIBP3226 is concentration-dependently displaced by neuropeptide Y and its peptide analogues with an affinity pattern neuropeptide Y-() [Leu super(31),Pro super(34)] neuropeptide Y-(), neuropeptide Y-(18-36). This rank order of potencies is consistent with the interaction of [ super(3)H]BIBP3226 with neuropeptide Y receptors of the Y sub(1) subtype. Therefore, [ super(3)H]BIBP3226 can be used as selective ligand to study neuropeptide Y Y sub(1) receptors.
ISSN:0014-2999