Abstract:
:The 1,4-dihydropyridine-sensitive voltage-gated Ca2+ channel is widely distributed in excitable cells. The channel and its several associated drug binding sites are known to be up- and downregulated by a variety of homologous and heterologous influences including membrane depolarization. The neurosecretory GH4C1 cell line possesses L-type channels. Depolarization of these cells by elevated K+ increases the binding affinity of 1,4-dihydropyridines and decreases the number of 1,4-dihydropyridine binding sites and functional channels. There is a coordinate upregulation of the number of muscarinic receptors. This membrane potential- and Ca(2+)-calmodulin-dependent process of channel downregulation may involve internalization of the channel heteromeric complex or, more plausibly, a dissociation of the complex and a concomitant loss of both binding and permeation functions.
journal_name
Ann N Y Acad Scijournal_title
Annals of the New York Academy of Sciencesauthors
Liu J,Rutledge A,Triggle DJdoi
10.1111/j.1749-6632.1995.tb16568.xsubject
Has Abstractpub_date
1995-09-15 00:00:00pages
119-33; discussion 160-2eissn
0077-8923issn
1749-6632journal_volume
765pub_type
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