Binding of [3H]SKF 38393 to dopamine D-1 receptors in rat striatum in vitro; estimation of receptor molecular size by radiation inactivation

[3H]SKF 38393 (2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine) binds with high affinity to 3,4-dihydroxyphenylethylamine (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 approximate...

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Bibliographic Details
Published inJournal of neurochemistry Vol. 48; no. 2; p. 370
Main Authors Gredal, O, Nielsen, M
Format Journal Article
LanguageEnglish
Published England 01.02.1987
Subjects
2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine
Animals
Benzazepines - metabolism
Binding, Competitive
Corpus Striatum - metabolism
Male
Molecular Weight
Rats
Rats, Inbred Strains
Receptors, Dopamine - metabolism
Receptors, Dopamine - radiation effects
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Summary:[3H]SKF 38393 (2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine) binds with high affinity to 3,4-dihydroxyphenylethylamine (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 approximately 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 approximately 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 (approximately 80,000 daltons).
ISSN:0022-3042