The substance P receptor antagonist CP-96,345 interacts with Ca2+ channels.
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.
Schmidt
A W
AW
Department of Neuroscience, Pfizer Inc., Groton, CT 06340-1596.
McLean
S
S
Heym
J
J
D000818:Animals; D001667:Binding, Competitive; D001713:Biphenyl Compounds / Q000494:pharmacology*; D001921:Brain / Q000187:drug effects; D015220:Calcium Channels / Q000187:drug effects*; D004110:Diltiazem / Q000494:pharmacology; D004347:Drug Interactions; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D009568:Nitrendipine / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D018040:Receptors, Neurokinin-1; D017981:Receptors, Neurotransmitter / Q000037:antagonists & inhibitors*; D013373:Substance P / Q000378:metabolism*; D014316:Tritium; D014700:Verapamil / Q000031:analogs & derivatives / Q000494:pharmacology
D001713:Biphenyl Compounds; D015220:Calcium Channels; D018040:Receptors, Neurokinin-1; D017981:Receptors, Neurotransmitter; D014316:Tritium; D013373:Substance P; C043184:4-desmethoxyverapamil; D009568:Nitrendipine; D014700:Verapamil; D004110:Diltiazem; C066892:CP 96345