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Interactions of 7-[3-(4-[2,3-Dimethylphenyl]piperazinyl)-propoxy]-2(lH)-quinolinone (OPC-4392) with 3H-Spiperone and 3H-SCH 23390 Binding in Rat Striatum: Effects of Lesions

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Abstract

7-[3-(4-[2,3-Dimethylphenyl]piperazinyl)propoxy]-2(lH)-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-l 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-l 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.

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Authors and Affiliations

  1. Department of Pharmacology, Institute of Pharamceutical Sciences, Hiroshima University School of Medicine, Kasumi 1-2-3, Minami-ku, Hiroshima, 734, Japan

    Xiao Zhang, Yoshihiro Nakata & Tomio Segawa

  2. Laboratories of New Drug Research, Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd., Japan

    Tetsuro Kikuchi

Authors
  1. Xiao Zhang
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  2. Yoshihiro Nakata
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  3. Tetsuro Kikuchi
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  4. Tomio Segawa
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Zhang, X., Nakata, Y., Kikuchi, T. et al. Interactions of 7-[3-(4-[2,3-Dimethylphenyl]piperazinyl)-propoxy]-2(lH)-quinolinone (OPC-4392) with 3H-Spiperone and 3H-SCH 23390 Binding in Rat Striatum: Effects of Lesions. Pharm Res 7, 280–282 (1990). https://doi.org/10.1023/A:1015882314302

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  • DOI: https://doi.org/10.1023/A:1015882314302

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