Homologous regulation of voltage-dependent calcium channels by 1,4-dihydropyridines

• Published in: Biochemical and biophysical research communications Vol. 160; no. 2; pp. 929 - 936
• Main Authors: Skattebøl, A., Brown, A.M., Triggle, D.J.
• Format: Journal Article
• Language: English
• Published: San Diego, CA Elsevier Inc 28.04.1989; Elsevier
• Subjects: 1,4-dihydropyridine; 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester - pharmacology; Animals; Barium - metabolism; Biological and medical sciences; calcium; Calcium - metabolism; Calcium Channels - drug effects; Calcium Channels - metabolism; Calcium Channels - physiology; Cell Line; Cell physiology; Dihydropyridines - metabolism; Dihydropyridines - pharmacology; Fundamental and applied biological sciences. Psychology; Kinetics; Membrane and intracellular transports; Membrane Potentials - drug effects; Molecular and cellular biology; Pheochromocytoma - metabolism; Radioligand Assay; Rats; Receptors, Nicotinic - drug effects; Cell culture; Calcium; Radiolabelling; Ionic channel; Biomembrane; Binding site; In vitro; Pyridine derivatives; Regulation(control); Spectrometry; Cell line; Activator; Antagonist; Biological receptor
• ISSN: 0006-291X; 1090-2104
• DOI: 10.1016/0006-291X(89)92524-2

Chronic treatment of PC 12 cells with the 1,4-dihydropyridine Ca2+ channel antagonist nifedipine [ 5 × 10-8M/5 days ] and the activator S Bay K 8644 [ 5 × 10-7M/5 days ] resulted in up- and down-regulation of 1,4-dihydropyridine binding site density by 29 and 24%, respectively, without change in affinity. These changes in binding site density represent functional changes as indicated by the corresponding changes in K+ depolarization-induced 45Ca2+ uptake and in whole cell currents carried by Ba2+ ions. This homologous regulation of voltage-dependent Ca2+ channels [ VDCC ] by potent and specific ligands parallels that observed for other classes of membrane receptors.