Mesulergine and its 1,20-N,N-bidemethylated metabolite interact directly with D1- and D2-receptors.


Mesulergine (CU 32-085), an 8 alpha-aminoergoline, has been reported to influence striatal dopamine turnover in a time-dependent biphasic manner, suggesting initial dopamine antagonistic and late dopamine agonistic effects. To clarify whether these opposing in vivo effects are due to a metabolic conversion in vivo or reflect mixed antagonist/agonist effects… (More)