Specific binding of 3H-SCH 23390 to dopamine D1 receptors in vivo |
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| Authors: | P H Andersen F C Gr?nvald |
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| Affiliation: | 1. Department of Pharmacology, NOVO Pharmaceuticals R&D, Novo Alle, DK-2880 Bagsvaerd, Denmark;2. Department of Med. Chemistry I, NOVO Pharmaceuticals R&D, Novo Alle, DK-2880 Bagsvaerd, Denmark;1. Department of Pharmacy, China Pharmaceutical University, Nanjing 210009, China;2. China National Narcotics Control Commission - China Pharmaceutical University Joint Laboratory on Key Technologies of Narcotics Control, Nanjing 210009, China;3. Key Laboratory of Drug Monitoring and Control, Drug Intelligence and Forensic Center, Ministry of Public Security, Beijing 100193, China |
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| Abstract: | The binding of 3H-SCH 23390 was studied in vivo in the mouse brain. The binding was saturable, reversible and stereospecific. The level of nonspecific binding was 5-15% of total binding. Pharmacological characterization revealed binding of 3H-SCH 23390 to D1 receptors. Thus, dopaminergic antagonists known to possess D1 affinity, e.g., SCH 23390 itself, cis-flupentixol and (+)-butaclamol, were potent inhibitors of the 3H-SCH 23390 binding. On the other hand, high doses of D2 selective compounds were required to inhibit the 3H-SCH 23390 binding. These results indicate that 3H-SCH 23390 is a ligand of choice for in vivo studies of D1 receptors. |
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