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[ 3 H]S33084: a novel, selective and potent radioligand at cloned, human dopamine D 3 receptors
- Source :
- Naunyn-Schmiedeberg's Archives of Pharmacology. 361:569-572
- Publication Year :
- 2000
- Publisher :
- Springer Science and Business Media LLC, 2000.
-
Abstract
- The novel, selective dopamine D3 receptor antagonist, S33084 [(3aR,9bS)-N[4-(8-cyano-1,3a,4,9b-tetrahydro-3H-benzopyrano[3,4-c]pyrrole-2-yl)-butyl] (4-phenyl)benzamide], was tritium-labelled to 59 Ci/mmol specific activity. Determination of association and dissociation rate constants at recombinant, human (h) D3 receptors stably expressed in Chinese hamster ovary (CHO) cells yielded a K d value (0.16 nM) comparable to that observed in saturation binding experiments (0.17 nM). The competition binding profile of [3H]S33084 with diverse D3 receptor agonists and antagonists correlated highly (0.99) with that of [3H]spiperone. In conclusion, [3H]S33084 is a highly potent and selective radioligand at dopamine D3 receptors, which should be of considerable use for their characterisation.
- Subjects :
- Spiperone
CHO Cells
Biology
Transfection
Tritium
Binding, Competitive
Radioligand Assay
chemistry.chemical_compound
Dopamine receptor D3
Cricetinae
Radioligand
medicine
Animals
Humans
Benzopyrans
Pyrroles
Benzamide
Receptor
Cells, Cultured
Pharmacology
Receptors, Dopamine D2
Chinese hamster ovary cell
Receptors, Dopamine D3
Antagonist
General Medicine
Recombinant Proteins
chemistry
Biochemistry
Dopamine Antagonists
medicine.drug
Subjects
Details
- ISSN :
- 14321912 and 00281298
- Volume :
- 361
- Database :
- OpenAIRE
- Journal :
- Naunyn-Schmiedeberg's Archives of Pharmacology
- Accession number :
- edsair.doi.dedup.....217390b75e88591904fe89c8247b4ac4