Haloperidol competitively inhibits the binding of (+)-[3H]SKF-10,047 to sigma sites.
Scatchard plots of equilibrium saturation binding data revealed that haloperidol inhibits the binding of (+)-[3H]SKF-10,047 to sigma sites in a competitive manner. In experiments using membranes from both guinea pig and rat brain the apparent Kd of (+)-[3H]SKF-10,047 for sigma sites was significantly increased, whereas the apparent Bmax was not altered by the addition of 10 nM haloperidol.
McCann
D J
DJ
Neurochemistry Unit, National Institute on Drug Abuse, Baltimore, MD 21224.
Su
T P
TP
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D006168:Guinea Pigs; D006220:Haloperidol / Q000494:pharmacology*; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D010620:Phenazocine / Q000031:analogs & derivatives* / Q000494:pharmacology; D051381:Rats; D011957:Receptors, Opioid / Q000378:metabolism*; D017480:Receptors, sigma
D011957:Receptors, Opioid; D017480:Receptors, sigma; C012134:SK&F 10047; D010620:Phenazocine; D006220:Haloperidol