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• W2038215153 abstract "3H-SCH-23390, a selective antagonist of D-1 dopamine (DA) receptors, was used in a radioreceptor assay with rat brain striatal tissue, optimized biochemically, and extensively characterized pharmacologically with striatal membranes. Nonspecific binding, denned with excess cis(Z)-flupenthixol (300 nM), averaged 20–25% of total counts bound. Specific binding was linearly dependent on the amount of original striatal tissue (0–4 mg) or protein (0–250μg), temperature dependent, saturable and reversible, and appeared to involve a single site at ligand concentrations limited to <10 nM. Binding in rat brain regions ranked as: striatum > accumbens > prefrontal cortex > posterior cerebral cortex > cerebellum. Association was virtually complete within 30 min at 30°, and the rate of dissociation at 30° was 0.0377 min−1 (half-time = 18.4 min). Affinity (Ka or Kd) determined from association and dissociation rate constants and from concentration isotherms averaged 0.349 and 0.340 nM respectively. Including Na+ at 150 mM increased apparent maximum specific binding (Bmax) by 19%, with a 29% increase in affinity; other monovalent cations alone had small effects on specific binding; Ca2+ and Mg2+ reduced binding by 30–40% at 5–10 mM, and a physiologic mixture of cations reduced binding by 42%. Agents (N = 85) were tested for potency (Ki or IC50) in competition with the ligand (at 0.30 nM). Those known to have selective effects at D-1 receptors, generally, were most potent and stereoselective. Na+ (150 mM) had little effect on the affinity of cis-thioxanthenes but decreased that of most other agents tested with high D-1 affinity. For antipsychotic agents, the correlation of typlcal clinical daily doses versus Ki at D-1 sites (r = 0.06) was much lower than at D-2 sites (r = 0.94) . (−)Thioridazine was discovered to be D-1 selective, whereas the (+) enantiomer was selective for D-2 sites labeled with 3H-spiperone. Relatively sedating antidepressants had greater D-1 affinity than their less-sedating, secondary amine congeners." @default.
• W2038215153 created "2016-06-24" @default.
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• W2038215153 date "1989-02-01" @default.
• W2038215153 modified "2023-09-24" @default.
• W2038215153 title "Pharmacology of binding of 3H-SCH-23390 to D-1 dopaminergic receptor sites in rat striatal tissue" @default.
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• W2038215153 doi "https://doi.org/10.1016/0006-2952(89)90387-0" @default.
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