Conformation of dopamine at the dopamine receptor

H. L. Komiskey, J. F. Bossart, Duane Miller, P. N. Patil

Research output: Contribution to journalArticle

18 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)2641-2643
Number of pages3
JournalProceedings of the National Academy of Sciences of the United States of America
Volume75
Issue number6
DOIs
StatePublished - Jan 1 1978

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Dopamine Receptors
Dopamine
Corpus Striatum
Membranes
Binding Sites
Cyclobutanes
Caudate Nucleus
Pharmaceutical Preparations

All Science Journal Classification (ASJC) codes

  • General

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Conformation of dopamine at the dopamine receptor. / Komiskey, H. L.; Bossart, J. F.; Miller, Duane; Patil, P. N.

In: Proceedings of the National Academy of Sciences of the United States of America, Vol. 75, No. 6, 01.01.1978, p. 2641-2643.

Research output: Contribution to journalArticle

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