Binding of [3H]SKF 38393 to Dopamine D-l Receptors in Rat Striatum In Vitro; Estimation of Receptor Molecular Size by Radiation Inactivation
- 1 February 1987
- journal article
- research article
- Published by Wiley in Journal of Neurochemistry
- Vol. 48 (2), 370-375
- https://doi.org/10.1111/j.1471-4159.1987.tb04103.x
Abstract
[3H]SKF 38393 (2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine) binds with high affinity to 3,4-dihdyroxyphenylethylamine (dopamine) D-1, receptors in rat striatum in vitro (Kd = 7 and 14 nM in nonfrozen and frozen striatum, respectively). The number of binding sites (Bmax) was .apprx. 80.0 pmol/g of original tissue, a value similar to the Bmax for the dopamine D-1 antagonist SCH 23390. Nondisplaceable [3H]SKF 38393 binding was .apprx. 45% of total binding. Irradiation (0-4 Mrad) of frozen whole striata decreased the number of [3H]SKF 38393 binding sites monoexponentially without changing the binding affinity. The functional molecular mass for the agonist dopamine D-1 binding site was 132,800 daltons, which is higher than the functional molecular mass of the antagonist dopamine D-1 binding site (.apprx. 80,000 daltons).Keywords
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