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  • Title: Turnover of specific [3H]spiperone and [3H]N,n-propylnorapomorphine binding sites in rat striatum following phenoxybenzamine administration.
    Author: Hall MD, Jenner P, Marsden CD.
    Journal: Biochem Pharmacol; 1983 Oct 01; 32(19):2973-7. PubMed ID: 6626267.
    Abstract:
    Inclusion of phenoxybenzamine into incubates containing rat striatal preparations equipotently displaced specific striatal [3H]spiperone and [3H]NPA binding. Pre-incubation of striatal membranes with phenoxybenzamine followed by extensive washing equipotently inhibited the subsequent specific [3H]spiperone or [3H]NPA binding. In both displacement and pre-incubation experiments phenoxybenzamine caused complete inhibition of specific [3H]spiperone binding to rat striatal membranes, but only partially inhibited specific [3H]NPA binding. Following parenteral administration to rats, phenoxybenzamine caused a marked inhibition of ex vivo specific [3H]spiperone binding in striatal tissue preparations from these animals which lasted approximately 24 hr following in vivo drug administration. In contrast, administration of phenoxybenzamine caused only a transient change in ex vivo specific [3H]NPA binding. Phenoxybenzamine causes irreversible inhibition of [3H]spiperone and [3H]NPA binding in vitro. In vivo administration of phenoxybenzamine discriminates between [3H]spiperone and [3H]NPA in ex vivo studies suggesting that these binding sites have different turnover rates.
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