Neurotransmitter receptor binding studies predict antiemetic efficacy and side effects.
Radioligand binding studies were used to analyze the interaction of antiemetics with central dopamine D2 and alpha-adrenergic1 receptors. The affinity of antiemetics for dopamine D2 receptors labeled by 3H-spiperone significantly correlated with clinically effective drug doses (r = 0.92; P less than 0.01). Furthermore, the relative inhibition of alpha-adrenergic1 receptors as measured by 3H-WB 4101 binding predicts the clinical side effects of sedation and orthostatic hypotension. Neurotransmitter receptor binding analysis provides a rapid and sensitive technique for measuring antiemetic potency as well as associated side effects.
D000818:Animals; D000932:Antiemetics / Q000378:metabolism* / Q000494:pharmacology; D001711:Biotransformation; D001923:Brain Chemistry; D002421:Caudate Nucleus / Q000378:metabolism; D002540:Cerebral Cortex / Q000378:metabolism; D002746:Chlorpromazine / Q000378:metabolism; D066298:In Vitro Techniques; D011346:Prochlorperazine / Q000378:metabolism; D011869:Radioligand Assay; D051381:Rats; D011942:Receptors, Adrenergic, alpha / Q000378:metabolism; D011954:Receptors, Dopamine / Q000378:metabolism; D017448:Receptors, Dopamine D2; D017981:Receptors, Neurotransmitter / Q000037:antagonists & inhibitors / Q000378:metabolism*
D000932:Antiemetics; D011942:Receptors, Adrenergic, alpha; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D017981:Receptors, Neurotransmitter; D002746:Chlorpromazine; D011346:Prochlorperazine