Dopamine agonistic potency of two novel prolactin release-inhibiting ergolines.

Abstract:

:Two novel 8 alpha-amino ergolines (CH 29-717 and CU 32-085) have been shown to inhibit secretion of prolactin in rats in vivo. However, when tested for dopaminomimetic potency on pituitary cell culture preparations in vitro, CH 29-717 inhibited prolactin release with an IC50 = 4 X 10(-9) M. In the same model the 1-methyl-derivative CU 32-085 was only weakly active even at high concentrations. When both compounds were incubated together, CU 32-085 displayed an inhibitory effect on the prolactin release restriction caused by CH 29-717. The activities were not time-dependent since similar results were obtained with incubation for 3 or 24 h. These results support the hypothesis that the 1-methyl ergoline derivative CU 32-085 is a partial agonist and becomes fully active in vivo only after metabolic conversion.

journal_name

Eur J Pharmacol

authors

Markó M

doi

10.1016/0014-2999(84)90167-5

subject

Has Abstract

pub_date

1984-06-01 00:00:00

pages

263-6

issue

3-4

eissn

0014-2999

issn

1879-0712

pii

0014-2999(84)90167-5

journal_volume

101

pub_type

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