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Receptor-receptor link in membranes revealed by ligand competition: Example for dopamine D1 and D2 receptors

✍ Scribed by Philip Seeman; Roger K. Sunahara; Hyman B. Niznik

Publisher
John Wiley and Sons
Year
1994
Tongue
English
Weight
345 KB
Volume
17
Category
Article
ISSN
0887-4476

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✦ Synopsis

An interaction or link between dopamine D1 receptors and dopamine D2 receptors was found by a ligand competition method, using [3Hlraclopride to label dopamine D2 receptors and SCH 23390 to block dopamine D1 receptors. In the presence of endogenous or exogenous dopamine, SCH 23390 increased the binding of [3H]raclopride in post-mortem human striata homogenates or in tissue culture cells containing human dopamine D1 and D2 receptors. In order to reveal such intramembrane receptor-receptor interactions in general, therefore, it appears essential to add two agonists, one for each receptor, and then to block one of the receptors when measuring the binding of a ligand to the second receptor.

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✍ Anton N. M. Schoffelmeer; Francois Hogenboom; Arie H. Mulder; Eric Ronken; Johan 📂 Article 📅 1994 🏛 John Wiley and Sons 🌐 English ⚖ 703 KB

## Abstract In this study we examined the selectivity of dopamine (DA) for rat striatal DA D~1~ and D~2~ receptors. In a Krebs‐HEPES buffer, the K~i~ values of DA for D~1~ binding sites (labelled with [^3^H]SCH23390) and D~2~ binding sites (labelled with [^3^H]spiroperidol) in striatal membranes am