The inhibition of the sarcoplasmic calcium pump by prenylamine, reserpine, chlorpromazine and imipramine

@article{Balzer2004TheIO,
  title={The inhibition of the sarcoplasmic calcium pump by prenylamine, reserpine, chlorpromazine and imipramine},
  author={H. Balzer and Madoka Makinose and Wilhelm Hasselbach},
  journal={Naunyn-Schmiedebergs Archiv f{\"u}r Pharmakologie und experimentelle Pathologie},
  year={2004},
  volume={260},
  pages={444-455}
}
Zusammenfassung1. Reserpin, Prenylamin, Chlorpromazin und Imipramin hemmen sowohl die Geschwindigkeit der Calcium-Aufnahme als auch die der Calcium-induzierten Extra-ATP-Spaltung an isolierten Vesikelmembranen des sarkoplasmatischen Reticulums von quergestreifter Muskulatur des Kaninchens. Die für eine 50%ige Hemmung erforderlichen Konzentrationen betragen beim Reserpin, Prenylamin und Chlorpromazin 3×10−5M, beim Impiramin ∼3×10−4M.2. Calcium-Efflux und -Influx werden durch die Pharmaka in… 
Beeinflussung des Calcium-Austauschs und der Muskelfunktion des M. rectus und sartorius des Frosches durch Chlorpromazin, Prenylamin, Imipramin und Reserpin
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The pattern of fatty acids of phosphatides in the skeletal muscles of rats with druginduced (20.25-diazacholesterol) myotonia is examined and an increase in the C18:2, C20:4 and C22:6 fatty acids is found.
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TLDR
Arguments have been presented in favour of the assumption that a high internal concentration of soluble calcium present inside the vesicles during the initial phase of net calcium uptake is an essential condition for the drug effect.
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The inhibitory potency of these compounds upon the calcium pump appears to be correlated with their membrane activity or potency as local anaesthetic agents, rather than with their β-adrenoceptor blocking potency.
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The activity of the calcium pump is not affected appreciably when the vesicles are treated with hydrazine under optimal conditions for phosphorylation, and the stability of the isolated phosphoprotein has its optimum at pH 2.5.
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It is hypothesized that conformational membrane changes might contribute to the leakage of macromolecules such as enzymes from the cell interior and be consistent with an imipramine-induced interference at these enzyme sites and a disruption of lipid-protein interrelations.
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To study the release of granular products from individual cells, formaldehyde-chloral induced fluorescence and α-MSH- and β-endorphin immunoreactivies were demonstrated in consecutive sections from pituitaries of rats given 8 mg/kg body weight of reserpine 24 h before sacrifice, and results indicate coordinated release of thesegranular products at the cellular level after Reserpine treatment.
The sarcoplasmic calcium pump — A most efficient ion translocating system
  • W. Hasselbach
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    Biophysics of structure and mechanism
  • 2004
TLDR
In contrast to the sodium-potassium transporting plasma membranes, the sarcoplasmic membranes (SR) are highly specialized structures into which only two major intrinsic proteins, a calcium transporting protein and a calcium binding protein are embedded and can transform reversibly chemical into osmotical energy.
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