Dopamine D1 receptor agonists display a different intrinsic activity in rat, monkey and human astrocytes

R J Vermeulen, C A Jongenelen, C H Langeveld, E C Wolters, J C Stoof, B Drukarch

Research output: Contribution to journalArticleAcademicpeer-review

Abstract

Measuring dopamine D1 receptor stimulated cyclic AMP production in cultured astrocytes from rat, monkey and human brain, we demonstrate that the 'classical' drug SKF 38393 (7,8-dihydroxy-1- phenyl-2,3,4,5-tetrahydro-1 H-3-benzazepine) is a partial agonist with particularly low intrinsic activity in primates. Furthermore, its analogue SKF 81297 (6-chloro-7,8-dihydroxy-1-phenyl-2,3,4,5- tetrahydro-1 H-3-benzazepine) is shown to be a full agonist in rats but a partial, albeit more efficacious, agonist in primates, whereas the benzopyran A 68930 ((1R,3S)-1-aminomethyl-5,6- dihydroxy-3-phenyl-isochroman HCl) displays full efficacy in both species. The data suggest that cultured astrocytes provide a good model to study species differences in the pharmacological characteristics of dopamine D1 receptor agonists and indicate that SKF 38393 is not suited to study dopamine D1 receptor function in primates.

Original languageEnglish
Pages (from-to)121-5
Number of pages5
JournalEuropean Journal of Pharmacology
Volume269
Issue number1
Publication statusPublished - 15 Sep 1994

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