Irreversible interaction of beta-haloalkylamine derivatives with dopamine D1 and D2 receptors.
The interaction of beta-haloalkylamine derivatives of dopamine agonists and antagonists with 3H-spiperone binding (D2 sites) and 3H-flupenthixol binding (D1 sites) was studied. N-chloroethyl derivatives of phenothiazines and thioxanthenes were potent inhibitors of the binding of both ligands. The in vitro inhibition of binding produced by these compounds was irreversible. The drugs were however only weakly active in vivo. The results suggest that beta-haloalkylamine derivatives of neuroleptics may be useful compounds for studying dopamine receptors in vitro.
D000818:Animals; D002090:Butyrophenones / Q000378:metabolism*; D002417:Cattle; D003342:Corpus Striatum / Q000378:metabolism; D005475:Flupenthixol / Q000378:metabolism*; D009588:Nitrogen Mustard Compounds / Q000502:physiology*; D010640:Phenothiazines / Q000494:pharmacology*; D011954:Receptors, Dopamine / Q000187:drug effects / Q000378:metabolism*; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; D013134:Spiperone / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013892:Thioxanthenes / Q000378:metabolism* / Q000494:pharmacology*
D002090:Butyrophenones; D009588:Nitrogen Mustard Compounds; D010640:Phenothiazines; D011954:Receptors, Dopamine; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; D013892:Thioxanthenes; D013134:Spiperone; D005475:Flupenthixol