LY-86057 is a serotonin receptor modulator of the ergoline family. It is the N1-desisopropyl analogue of the much better-known ergoline and serotonin receptor antagonist LY-53857. The drug shows high affinity for the serotonin 5-HT2 receptors, including for the serotonin 5-HT2A receptor (Ki = 1.79–55.9 nM) and for the serotonin 5-HT2B receptor (Ki = 12.2–12.3 nM), whereas its affinity for the serotonin 5-HT2C receptor was not determined. It shows more than 10-fold greater affinity for the human, monkey, and pig serotonin 5-HT2A receptors than for the rat serotonin 5-HT2A receptor. LY-86057 is said to act as an antagonist of the serotonin 5-HT2A receptor. It also shows high affinity for the serotonin 5-HT1F receptor (Ki = 12.2 nM). Other analogues of LY-86057 besides LY-53857 (the N1-isopropyl derivative) have also been described, for instance LY-108742 (the N1-methyl derivative) and LY-197541 (the N1-isobutyl derivative). LY-86057 was first described in the scientific literature by 1993.
See also Substituted ergoline LY-53857 LY-215840 Ergometrine LA-3Cl-SB
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