{"doi":"10.1002/syn.890090107","title":"Severe depletion of cocaine recognition sites associated with the dopamine transporter in Parkinson's‐diseased striatum","abstract":"<jats:title>Abstract</jats:title><jats:p>The cocaine congener [<jats:sup>3</jats:sup>H]CFT, also designated [<jats:sup>3</jats:sup>H]WIN 35,428 (2β;‐carbomethoxy‐3β;‐(4‐fluorophenyltropane)), labels cocaine receptors associated with the dopamine transporter in primate striatum. Autoradiogrpahic distribution of [<jats:sup>3</jats:sup>H]CFT binding (5 nM) in human postmortem control and Parkinson's‐diseased striatal tissue sections was compared. In control tissue, high and comparable levels of [<jats:sup>3</jats:sup>H]CFT binding were observed in the putamen and caudate nucleus. At least 90–99% of total [<jats:sup>3</jats:sup>H]CFT bound was inhibited by (—)‐cocaine (30 μM), suggesting that a high proportion of [<jats:sup>3</jats:sup>H]CFT is specifically bound. In Parkinson's‐diseased tissue, binding sites for [<jats:sup>3</jats:sup>H]CFT were reduced by 80% in the caudate nucleus and 96% in the putamen. This pattern of depletion parallels the previously reported loss of dopamine in these brain regions (Kish, Shannak, and Hornykiewicz, <jats:italic>New Engl. J. Med.</jats:italic>, 318:876–880, 1988). In the dorsal caudate nucleus of Parkinson's‐diseased tissue, a lateral‐to‐medial gradient of [<jats:sup>3</jats:sup>H]CFT binding was observed, with the lateral caudate more severely depleted than the medial caudate. The marked decrease of [<jats:sup>3</jats:sup>H]CFT binding sites in Parkinson's diseased striatum supports the following conclusions: (1) the dopamine transporter is localized primarily on presynaptic nigrostriatal terminals; (2) in the caudate and putamen, cocaine recognition sites are associated primarily with the dopamine transporter; (3) the low level of nonspecific binding of [<jats:sup>3</jats:sup>H]CFT and the marked depletion of [<jats:sup>3</jats:sup>H]CFT‐labeled sites suggest that radiolabeled derivatives of CFT or its congeners may be suitable imaging probes for presynaptic dopamine nerve terminals.</jats:p>","journal":"Synapse","year":1991,"id":37286,"datarank":15.533409296318288,"base_score":5.4680601411351315,"endowment":5.4680601411351315,"self_citation_contribution":0.8202090211702698,"citation_network_contribution":14.713200275148019,"self_endowment_contribution":0.8202090211702698,"citer_contribution":14.713200275148019,"corpus_percentile":null,"corpus_rank":null,"citation_count":236,"citer_count":200,"citers_with_citation_signal":197,"citers_with_endowment":197,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":69446,"name":"Bertha K. 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