Haloperidol increases prolactin release and cyclic AMP formation in vitro: inverse agonism at dopamine D2 receptors?
Haloperidol (30 nM, 3 microM) was found to increase prolactin release from GH4C 1 cells transfected with the D2 receptor cDNA (GH4ZR 7) and from wild-type (untransfected) GH 3 cells, but not from wild-type GH4C 1 cells. In addition, haloperidol (3 microM) stimulated cAMP formation in GH 3 cells. It is suggested that haloperidol may act as an inverse agonist rather than as a neutral antagonist at dopaminergic D2 receptors.
Nilsson
C L
CL
Department of Pharmacology, University of Göteborg, Sweden.
Eriksson
E
E
D015056:1-Methyl-3-isobutylxanthine / Q000494:pharmacology; D000818:Animals; D002460:Cell Line; D000242:Cyclic AMP / Q000096:biosynthesis*; D015259:Dopamine Agents / Q000494:pharmacology*; D006220:Haloperidol / Q000494:pharmacology*; D011388:Prolactin / Q000378:metabolism*; D011863:Radioimmunoassay; D051381:Rats; D017448:Receptors, Dopamine D2 / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism; D014660:Vasoactive Intestinal Peptide / Q000494:pharmacology
D015259:Dopamine Agents; D017448:Receptors, Dopamine D2; D014660:Vasoactive Intestinal Peptide; D011388:Prolactin; D000242:Cyclic AMP; D006220:Haloperidol; D015056:1-Methyl-3-isobutylxanthine