MPTP lesions of the nigrostriatal dopaminergic projection decrease [3H]1-[1-(2-thienyl)cyclohexyl]-piperidine binding to PCP site 2: Further evidence that PCP site 2 is associated with the biogenic amine reuptake complex |
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| Authors: | Hyacinth C Akunne Jan N Johannessen Brian R de Costa Kenner C Rice Richard B Rothman |
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| Institution: | (1) Laboratory of Medicinal Chemistry, NIDDK, Bldg. 10-3D41, 20892 Bethesda, MD;(2) Laboratory of Clinical Science, NIMH, 20892 Bethesda, MD;(3) Division of Toxicology, Center for Food Safety and Applied Nutrition, FDA, 20204 Washington, D.C.;(4) Laboratory of Clinical Psychopharmacology, NIDA Addiction Research Center, PO BOX 5180, 21224 Baltimore, MD |
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| Abstract: | Our previous studies have demonstrated that, using membranes of guinea pig brain, 3H]1-1-(2-thienyl)cyclohexyl]piperidine (3H]TCP) labels not only the phencyclidine binding site associated with the NMDA receptor (PCP site 1), but also a second high affinity binding site which is associated with the biogenic amine reuptake carrier (termed PCP site 2). To test this hypothesis, the binding of 3H]GBR12935 to the dopamine transporter, and 3H]TCP binding to PCP sites 1 and 2 were measured in caudates harvested from control MPTP-treated and reserpine-treated dogs. MPTP treatment decreased dopamine levels by over 99%, decreased 3H]GBR12935 binding by over 90%, decreased 3H]TCP binding to PCP site 2 by about 50%, and had no significant effect on 3H]TCP binding to PCP site 1. These data are consistent with hypothesis that a portion of PCP site 2 is associated with dopaminergic nerve, terminals in dog caudate. |
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| Keywords: | Phencyclidine dopamine MPTP receptors PCP receptor |
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