Document Detail

Human neuropeptide YY1 receptors exert unequal control of the extracellular acidification rate in different cell lines.
MedLine Citation:
PMID:  9617757     Owner:  NLM     Status:  MEDLINE    
The ability of the human neuropeptide YY1 receptor subtype to increase the extracellular acidification rate in different cell lines was investigated by using the Cytosensor Microphysiometer. In CHO-Y1 cells (Chinese Hamster Ovary cells expressing the cloned human neuropeptide YY1 receptor), neuropeptide Y increased the acidification rate by up to 15% of the basal level with a -Log(EC50) of 7.42. As expected for neuropeptide YY1 receptors, this response was potently inhibited by the neuropeptide YY1-selective non-peptide antagonist BIBP3226 ((R)-N2-(diphenylacetyl)-N-[(4-hydroxy-phenyl)methyl]-D-arginine amide). Its enantiomer BIBP3435 ((S)-N2-(diphenylacetyl)-N-[(4-hydroxy-phenyl)methyl]-D-arginin amide) was less potent. The antagonists themselves did not affect the extracellular acidification rate at concentrations up to 10 microM. In SK-N-MC cells (a neuroblastoma cell line of human origin that expresses the neuropeptide YY1 receptor) no change of the acidification rate could be observed in the presence of neuropeptide Y at concentrations up to 1 microM. For control, the neuropeptide YY1 receptors were also investigated by assessing whole cell radioligand binding and, at the functional level, by assessing their ability to decrease the forskolin-induced accumulation of cAMP. The specific (i.e., neuropeptide Y-displaceable) binding of [3H]neuropeptide Y was to a homogeneous class of high-affinity sites in both SK-N-MC and CHO-Y1 cells. The equilibrium dissociation constants for [3H]neuropeptide Y, the total number of binding sites and the kinetic constants for association and for dissociation were similar. Neuropeptide Y produced a dose-dependent inhibition of forskolin-induced cAMP accumulation in SK-N-MC cells (-log(EC50) = 9.40) but it did not affect cAMP accumulation in CHO-Y1 cells. Non-transfected CHO-K1 cells were used as negative control throughout the study. No binding or response could be observed in these cells. Our data suggest that the signalling mechanisms of neuropeptide YY1 receptors are closely related to the cell type in which they are expressed.
I Van Liefde; P M Vanderheyden; N Fraeyman; J P De Backer; G Vauquelin
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  European journal of pharmacology     Volume:  346     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1998 Apr 
Date Detail:
Created Date:  1998-08-04     Completed Date:  1998-08-04     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  87-95     Citation Subset:  IM    
Department of Protein Chemistry, Free University of Brussels (VUB), Sint-Genesius Rode, Belgium.
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MeSH Terms
Arginine / analogs & derivatives,  pharmacology
CHO Cells
Cell Line
Cyclic AMP / metabolism
Forskolin / pharmacology
Hydrogen-Ion Concentration
Neuropeptide Y / metabolism*
Radioligand Assay
Receptors, Neuropeptide Y / antagonists & inhibitors,  physiology*
Tumor Cells, Cultured
Reg. No./Substance:
0/BIBP 3226; 0/Neuropeptide Y; 0/Receptors, Neuropeptide Y; 0/neuropeptide Y-Y1 receptor; 60-92-4/Cyclic AMP; 66428-89-5/Forskolin; 74-79-3/Arginine

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