Clinical melperone treatment blocks D2-dopamine receptors in the human brain as determined by PET.
Positron emission tomography and 11-C-labelled raclopride was used to determine central D2-dopamine receptor occupancy in three melperone treated patients. Treatment with melperone in daily doses of 250 and 300 mg for 3 to 6 weeks, resulted in a receptor occupancy above 70%. Thus, clinical doses of melperone as we previously demonstrated for several classical neuroleptics cause a substantial D2-dopamine receptor blockade in the human brain in vivo.
Wiesel
F A
FA
Department of Psychiatry and Psychology, Karolinska Institute.
Farde
L
L
Halldin
C
C
D000328:Adult; D014150:Antipsychotic Agents / Q000493:pharmacokinetics / Q000627:therapeutic use*; D002090:Butyrophenones / Q000493:pharmacokinetics / Q000627:therapeutic use*; D005260:Female; D006801:Humans; D008297:Male; D011388:Prolactin / Q000097:blood; D011618:Psychotic Disorders / Q000097:blood / Q000188:drug therapy*; D020891:Raclopride; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D012457:Salicylamides; D012559:Schizophrenia / Q000097:blood / Q000188:drug therapy*; D014055:Tomography, Emission-Computed
D014150:Antipsychotic Agents; D002090:Butyrophenones; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D012457:Salicylamides; D020891:Raclopride; D011388:Prolactin; C008522:metylperon