Dopamine receptor profile of co-dergocrine (Hydergine) and its components.

Abstract:

:Co-dergocrine (Hydergine), an ergot preparation composed of four dihydrogenated peptide ergot alkaloids (dihydroergocornine, dihydroergocristine, dihydro-alpha-ergokryptine, dihydro-beta-ergokryptine, 3:3:2:1), has been reported to exert in vivo effects suggesting an interaction with dopaminergic systems. The present investigation provides evidence that, in the striatum of the rat, co-dergocrine and its components interact directly with D1- and D2-subtypes of dopamine receptors. In homogenates of rat striatum, co-dergocrine and three of its components (dihydroergocornine, dihydro-alpha-ergokryptine, dihydro-beta-ergokryptine) stimulate cyclic AMP formation (D1-receptor response) having similar EC50 values but different efficacies. The same compounds inhibit electrically evoked tritium overflow from rat striatal slices preincubated with [3H]choline (D2-receptor response) at about 50 times lower concentrations. Here again the compounds exhibit differential maximal effects. One component, dihydroergocristine, antagonises both receptor types. The effect of co-dergocrine in functional responses mediated by both D1- and D2-receptors seems to reflect the summation of the contribution of its components.

journal_name

Eur J Pharmacol

authors

Markstein R

doi

10.1016/0014-2999(82)90312-0

subject

Has Abstract

pub_date

1982-12-24 00:00:00

pages

145-55

issue

2

eissn

0014-2999

issn

1879-0712

pii

0014-2999(82)90312-0

journal_volume

86

pub_type

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