Evidence for multiple receptor sites within the putative calcium channel View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

1982-10

AUTHORS

David R. Ferry, Hartmut Glossmann

ABSTRACT

Summary[3H]-Nimodipine, a potent calcium channel blocker, binds to an apparently homogeneous population of receptors in guinea-pig brain membranes (KD=0.62 nM, Hill coefficient}1.0). Diltiazem (10−5 M) lowers the KD for [3H]-nimodipine by a factor of 3 without changing the maximum number of binding sites. Diltiazem decreased the dissociation rate constant of the nimodipine-receptor complex from 0.18 min−1 to 0.049 min−1 and altered the pharmacological profile as revealed by displacement studies with (−) and (+) verapamil, (−) and (+) prenylamine and 1,4 dihydropyridines. In conclusion [3H]-nimodipine binding can be utilized as a tool to evaluate complex molecular interactions between calcium channel blockers. More... »

PAGES

80-83

References to SciGraph publications

  • 1975-03. Inotropic and electrophysiological actions of verapamil and D 600 in mammalian myocardium in NAUNYN-SCHMIEDEBERG'S ARCHIVES OF PHARMACOLOGY
  • 1975-03. Inotropic and electrophysiological actions of verapamil and D 600 in mammalian myocardium in NAUNYN-SCHMIEDEBERG'S ARCHIVES OF PHARMACOLOGY
  • Identifiers

    URI

    http://scigraph.springernature.com/pub.10.1007/bf00586355

    DOI

    http://dx.doi.org/10.1007/bf00586355

    DIMENSIONS

    https://app.dimensions.ai/details/publication/pub.1042113252

    PUBMED

    https://www.ncbi.nlm.nih.gov/pubmed/6292744


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