Delergotrile
chemical compound
Delergotrile (INNTooltip International Nonproprietary Name; developmental code name CM 29-712), also known as 6-methylergoline-8α-acetonitrile, is a dopamine receptor agonist of the ergoline family described as an antiparkinsonian agent which was never marketed. It is an analogue of lergotrile (LY-79907).
The drug shows high affinity for the dopamine D2 receptor (Ki = 34 nM). In addition to dopamine receptors, delergotrile shows affinity for the serotonin 5-HT1 receptor (K0.5 = 2.0 nM) and for the serotonin 5-HT2 receptor (Ki = 57 nM), as well as for the α1- and α2-adrenergic receptors. The drug appears to be an agonist of both dopamine D1 and to a lesser extent D2 receptors. Due to its dopamine receptor agonism, delergotrile produces antiparkinsonian-like effects, induces changes in locomotor activity and stereotypy, and reverses reserpine-induced akinesia in rodents. It also produces effects consistent with weak blockade of α-adrenergic receptors in rodents.
Delergotrile was first described in the literature by 1976. It was developed by Sandoz.
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This entry incorporates text from “Delergotrile” on English Wikipedia. Contributors are listed in the page history. Text is available under the Creative Commons Attribution-ShareAlike 4.0 License. Selected authority identifiers and statements are retrieved from Wikidata under CC0; their references and qualifiers remain part of the verification path.