mesulergine

Mesulergine is a synthetic ergoline derivative that acts as a serotonin receptor antagonist and dopamine receptor agonist. It was developed primarily as a treatment candidate for Parkinson's disease and hyperprolactinemia, but was never marketed due to adverse effects observed in preclinical animal studies[1][10]. Pharmacologically, mesulergine displays high affinity for serotonin 5-HT2 family receptors, acting as an antagonist at 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7 receptors, while exhibiting partial agonist properties at dopamine D2-like receptors and at the serotonin 5-HT6 receptor[1][4][3]. Clinical development was discontinued after histological abnormalities were observed in rats[1]. Mesulergine is notable for its use as a research tool in mapping and investigating serotonin receptor distribution in the brain[3][7].

Brand names

Mesulergine

Other names

mesulergineMesulergine hydrochlSulfamide, N'-[(8α)-1,6-dimethylergolin-8-yl]-N,N-dimethyl-N'-[(8-α1,6-dimethylergolin-8-yl]-N,N-dimethylsulfamidehydrochloride