Effects of chronic chlorpromazine treatment on peripheral benzodiazepine binding sites in heart, kidney, and cerebral cortex of rats.
Daily intraperitoneal administration to rats of 5 mg/kg of chlorpromazine (CPZ) for 21 days induced a significant up-regulation (51%) of peripheral benzodiazepine binding sites (PBSs) in cerebral cortex and a down-regulation of PBSs in the heart (25%) and kidney (14%), whereas no alteration in [3H]flunitrazepam binding in cerebral cortex was observed. [3H]PK 11195 binding to cerebral cortex returned to normal following 5 days of CPZ withdrawal, whereas the density of PBSs in the heart and kidney remained reduced. The affinity of PBSs for the ligand [3H]PK 11195 in the cerebral cortex and heart was not affected by the drug treatment or withdrawal. The CPZ-induced alterations in PBSs may be relevant to the effects of the drug on CNS and/or peripheral organs.
Gavish
M
M
Rappaport Family Institute for Research in the Medical Sciences, Haifa, Israel.
Weizman
R
R
D000818:Animals; D002540:Cerebral Cortex / Q000378:metabolism*; D002746:Chlorpromazine / Q000494:pharmacology*; D005445:Flunitrazepam / Q000378:metabolism; D007546:Isoquinolines / Q000378:metabolism; D007668:Kidney / Q000378:metabolism*; D008297:Male; D009206:Myocardium / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D011963:Receptors, GABA-A / Q000187:drug effects / Q000378:metabolism*
D007546:Isoquinolines; D011963:Receptors, GABA-A; D005445:Flunitrazepam; D002746:Chlorpromazine; C037850:PK 11195