Abstract：
:[3H]-d-cis-Diltiazem binds to canine cardiac sarcolemma in a specific, saturable, and reversible manner with a KD = 58.0 +/- 9.5 nM and a receptor site density (maximum binding) of 2.19 +/- 0.24 pmol/mg of protein. Bepridil and verapamil, Ca2+ channel inhibitors, can completely inhibit this binding at nM concentrations. This inhibition was determined from saturation binding data to be due to a change in affinity of the radioligand, suggesting a competitive interaction between the three drugs. However, in dissociation experiments, both bepridil and verapamil increased the dissociation rate of the radioligand. This effect is uncharacteristic of competitive inhibitors and suggests that bepridil and verapamil regulate [3H]-d-cis-diltiazem binding in a negative allosteric fashion through their own distinct binding sites.
journal_name
Mol Pharmacoljournal_title
Molecular pharmacologyauthors
Balwierczak JL,Johnson CL,Schwartz Asubject
Has Abstractpub_date
1987-02-01 00:00:00pages
175-9issue
2eissn
0026-895Xissn
1521-0111journal_volume
31pub_type
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更新日期：1986-10-01 00:00:00
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