| Literature DB >> 1971105 |
X Zhang1, Y Nakata, T Kikuchi, T Segawa.
Abstract
7-[3-(4-[2,3-Dimethylphenyl]piperazinyl)propoxy]-2(1H)-quinolinone (OPC-4392), a presynaptic dopamine autoreceptor agonist and postsynaptic D-2 receptor antagonist (Yasuda et al., Life Sci. 42: 1941-1954, 1988), was studied for its binding characteristics at 3H-SCH 23390-labeled dopamine D-1 receptors and 3H-spiperone-labeled dopamine D-2 receptors in rat striatum. The binding affinity of OPC-4392 for 3H-spiperone-labeled D-2 receptors was 500 times higher than for 3H-SCH 23390-labeled D-1 receptors. 6-Hydroxydopamine lesions of striatum and high-frequency current lesions of medial forebrain bundle did not affect the competition of OPC-4392 for 3H-spiperone binding. Kainic acid lesions of striatum significantly changed the one-site model fit to a two-site model fit of the competition curve of OPC-4392 for 3H-spiperone binding, suggesting that OPC-4392 competed with 3H-spiperone binding differently for postsynaptic dopamine D-2 receptors and for presynaptic dopamine autoreceptors.Entities:
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Year: 1990 PMID: 1971105 DOI: 10.1023/a:1015882314302
Source DB: PubMed Journal: Pharm Res ISSN: 0724-8741 Impact factor: 4.200