High affinity binding sites for [3H]-nitrendipine in rabbit uterine smooth muscle |
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Authors: | William C Miller John B Moore |
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Institution: | Research Labs, Ortho Pharmaceutical Corporation, Raritan, New Jersey, 08869, USA |
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Abstract: | The binding properties of the high affinity binding site for 3H]-nitrendipine on rabbit uteri membranes were investigated. The specific component had a dissociation constant of 0.46±.07nM and a maximal binding of 175±11 pmol/mg. A variety of other calcium channel blockers inhibited the binding of 3H]nitrendipine with varying potencies. Flunarizine demonstrated a high potency (IC50 = 0.30 uM) in inhibiting binding while verapamil and bepridil were less potent with IC50's of approximately 0.6–1.5 uM. Diltiazem did not displace nitrendipine even at very high concentrations. Verapamil displayed negative cooperative inhibition suggesting that a second site exists on uterine membranes for the binding of other calcium channel blockers. |
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