These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Characterization of calcium antagonist receptors in highly purified porcine cardiac sarcolemma.
    Author: Haase H, Wallukat G, Vetter R, Will H.
    Journal: Biomed Biochim Acta; 1987; 46(8-9):S363-9. PubMed ID: 2829862.
    Abstract:
    Drug receptors for the Ca-antagonists nitrendipine and (-)desmethoxyverapamil (D-888) were studied in porcine cardiac sarcolemma. The dihydropyridine (DHP) derivative [3H]nitrendipine binds to a single population of high affinity sites (KD = 0.44 +/- 0.10 nM, Bmax = 2.43 +/- 0.19 pmol/mg; (n = 8), whereas the phenylalkylamine derivative [3H](-)D-888 interacts with high and low affinity sites of KD = 5.1 +/- 1.4 nM and KD = 438 +/- 86 nM (n = 6) in the same membrane preparations. The antagonists tested differ also with respect to their pharmacological efficacy on cultured intact heart myocytes. The EC50 value of the negative chronotropic effect exerted by D-888 corresponds to its high affinity binding component. Nitrendipine exhibit a 200-fold lower pharmacological efficacy, as would be expected from binding data.
    [Abstract] [Full Text] [Related] [New Search]