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. 1978 Jun;75(6):2641–2643. doi: 10.1073/pnas.75.6.2641

Conformation of dopamine at the dopamine receptor.

H L Komiskey, J F Bossart, D D Miller, P N Patil
PMCID: PMC392618  PMID: 275833

Abstract

Tritiated dopamine was used to label the dopamine receptor in membranes isolated from the rat corpus striatum. Scatchard analysis of displacement of [3H]dopamine by nonradioactive dopamine indicated the presence of two binding sites. The similarities in affinity, capacity, and drug specificity of the high-affinity site in the striatal membranes from rat and the binding site in the membranes from the calf caudate nucleus suggest that [3H]dopamine labels the same site in both species. In order to determine what conformation of dopamine is preferred at the dopamine receptor site, conformationally restricted analogs of dopamine--namely, the cis and trans 2-amino-1(3,4-dihydroxyphenyl)cyclobutane hydrochlorides--were tested for their affinity to the receptor. Compared to the cis conformation, the trans-restricted analogs had more affinity for the receptor site, indicating that dopamine probably interacts with the receptor in the trans conformation.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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