Abstract
The nonpeptide substance P receptor antagonist CP-96,345 was found to displace binding to Ca2+ channel binding sites labelled with either [3H]desmethoxyverapamil or [3H]diltiazem and to enhance [3H]nitrendipine binding. Unlike the substance P receptor antagonist activity of CP-96,345, these effects on Ca2+ channel binding sites were neither stereoselective nor species-dependent. It is concluded that CP-96,345 may act as an antagonist of L-type Ca2+ channels in addition to being a potent NK1 receptor (substance P) antagonist.
Publication types
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Comparative Study
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Corrected and Republished Article
MeSH terms
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Animals
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Binding, Competitive
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Biphenyl Compounds / pharmacology*
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Brain / drug effects
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Calcium Channels / drug effects*
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Diltiazem / pharmacology
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Drug Interactions
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Guinea Pigs
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Heart / drug effects
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Nitrendipine / pharmacology
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Radioligand Assay
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Rats
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Receptors, Neurokinin-1
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Receptors, Neurotransmitter / antagonists & inhibitors*
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Substance P / metabolism*
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Tritium
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Verapamil / analogs & derivatives
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Verapamil / pharmacology
Substances
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Biphenyl Compounds
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Calcium Channels
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Receptors, Neurokinin-1
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Receptors, Neurotransmitter
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Tritium
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Substance P
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4-desmethoxyverapamil
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Nitrendipine
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Verapamil
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Diltiazem
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CP 96345