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Characterization of Dopamine and β‐Adrenergic Receptors Linked to Cyclic AMP Formation in Intact Cells of the Clone D384 Derived from a Human Astrocytoma
Author(s) -
Balmforth Anthony J.,
Yasunari Kenichi,
Vaughan Peter F. T.,
Ball Stephen G.
Publication year - 1988
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1988.tb01119.x
Subject(s) - sch 23390 , endocrinology , medicine , chemistry , dopamine , antagonist , receptor , agonist , dopamine receptor , biology , biochemistry
3,4‐Dihydroxyphenylethylamine (dopamine) and β‐adrenergic receptor agonists and antagonists were assessed for their effects on cyclic AMP accumulation in human astrocytoma derived clone D384 cells. Dopamine, SKP 38393, and 2‐amino‐6,7‐dihydroxy‐l,2,3,4‐tetrahydronaphthalene increased cyclic AMP content with K a values of 2.0, 0.2, and 1.6 μ M . The D 1‐ selective antagonists SCH 23390 ( K i , 1.2 n M ) and SKF 83566 ( K i , 0.8 n M ) were over 5,000‐fold more potent than the D 2‐ selective antagonist domperidone ( K i , 6.7 μ M ) at inhibiting dopamine stimulation of cyclic AMP formation. SCH 23388 ( K i , 560 n M; the S ‐enantiomer of SCH 23390) was 400‐fold less potent than SCH 23390. Isopren‐aline, adrenaline, salbutamol, and noradrenaline increased cyclic AMP content with K a values of 0.13, 0.12, 0.22, and 7.60 μ M . The β 2‐ selective antagonist ICI 118,551 ( K i , 0.8 n M ) was almost 8,000‐fold more potent than the β,‐selective antagonist practolol ( K i , 5.9 μ M ) at inhibiting isoprenaline stimulated cyclic AMP accumulation. These results demonstrate that D384 cells express D 1 ‐dopamine and β 2‐ adren‐ergic receptors linked to adenylate cyclase. Furthermore, the dopamine receptor expressed by D384 cells exhibits a pharmacological profile typical of a mammalian striatal D 1 ‐re‐ceptor and therefore the use of this clone represents another approach to studying central D 1 ‐receptors.