Secretin receptors in the neuroglioma hybrid cell line NG108-15. Characterization and regulation of their expression.

Abstract

Secretin receptors in membranes from the neuroblastoma-glioma hybrid cell line NG108-15 were investigated by 125I-secretin binding and adenylate cyclase activation. On both parameters the corresponding relative potencies of parent peptides were, respectively: secretin greater than helodermin greater than peptide histidine isoleucinamide = vasoactive intestinal peptide. With secretin analogs and secretin fragments, the order of potency for binding was: secretin = [Val5]secretin greater than [Ala2]secretin = [Ala11]secretin greater than [Ala4, Val5] secretin greater than [Ala4]secretin greater than [D-Phe4] secretin greater than [D-Phe2]secretin = secretin (2-27) greater than secretin (3-27) greater than secretin (7-27). Also, on adenylate cyclase, [D-Phe4]secretin, [D-Phe2]secretin, secretin (2-27) and secretin (3-27) were partial agonists while secretin (7-27) was ineffective. The differentiating agent N6,2'-O-dibutyryladenosine 3',5'-monophosphate (1 mM) increased the density of secretin receptors and secretin-stimulated adenylate cyclase activity after a lag period of 4 h. After incubation for 24 h, receptor number and enzyme activity were increased 4- and 3-fold, respectively. These effects were inhibited totally by 1 microgram/ml cycloheximide and halved by 5 micrograms/ml actinomycin D. They were mimicked by 1 mM sodium butyrate but were not reproduced by either 8-bromoadenosine 3',5'-monophosphate or the phosphodiesterase inhibitor rac-4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone.

• Authors: D Gossen, M Tastenoy, P Robberecht, J Christophe
• Journal: European journal of biochemistry (Eur J Biochem) Vol. 193 Issue 1 Pg. 149-54 (Oct 05 1990) ISSN: 0014-2956 [Print] England
• PMID: 2171930 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Butyrates
• Receptors, G-Protein-Coupled
• Receptors, Gastrointestinal Hormone
• secretin receptor
• Butyric Acid
• Secretin
• Bucladesine
• Adenylyl Cyclases

Topics

• Adenylyl Cyclases (metabolism)
• Animals
• Bucladesine (pharmacology)
• Butyrates (pharmacology)
• Butyric Acid
• Cell Line
• Cell Membrane (metabolism)
• Enzyme Activation
• Hybrid Cells
• Kinetics
• Mice
• Neuroglia (metabolism)
• Neurons (metabolism)
• Rats
• Receptors, G-Protein-Coupled
• Receptors, Gastrointestinal Hormone (metabolism)
• Secretin (metabolism)