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  • Title: Solubilization of the calcium antagonist receptor from rat brain.
    Author: Curtis BM, Catterall WA.
    Journal: J Biol Chem; 1983 Jun 25; 258(12):7280-3. PubMed ID: 6305932.
    Abstract:
    [3H]Nitrendipine binds with high affinity to a calcium antagonist receptor in rat brain membranes. At 4 degrees C, treatment with digitonin solubilized the calcium antagonist receptor as a stable complex with [3H]nitrendipine. The nitrendipine concentration that gave a half-maximal amount of the solubilized [3H]nitrendipine-receptor complex was identical to the Kd for specific nitrendipine binding to brain membranes. Nitrendipine dissociated from digitonin-solubilized and membrane-bound receptors with a half-time of 24 to 30 min at 20 degrees C. Verapamil increased and diltiazem decreased the dissociation rate to a similar extent in both preparations indicating that the solubilized receptor contains both the dihydropyridine and diltiazem/verapamil binding sites. Sucrose gradient sedimentation experiments gave a value of S20, omega = 19.2 for the receptor-digitonin complex. The solubilized calcium antagonist receptor binds specifically to wheat germ agglutinin-Sepharose columns consistent with an identification as a glycoprotein.
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