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LY-86057

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LY-86057
BERJAYA
Clinical data
Other namesLY86057; 6-Methylergoline-8β-carboxylic acid 2-hydroxy-1-methylpropyl ester
Drug classSerotonin receptor modulator; Serotonin 5-HT2A receptor antagonist
ATC code
  • None
Identifiers
  • 3-hydroxybutan-2-yl (6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinoline-9-carboxylate
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC20H26N2O3
Molar mass342.439 g·mol−1
3D model (JSmol)
  • CC(C(C)OC(=O)[C@@H]1C[C@H]2[C@@H](CC3=CNC4=CC=CC2=C34)N(C1)C)O
  • InChI=1S/C20H26N2O3/c1-11(23)12(2)25-20(24)14-7-16-15-5-4-6-17-19(15)13(9-21-17)8-18(16)22(3)10-14/h4-6,9,11-12,14,16,18,21,23H,7-8,10H2,1-3H3/t11?,12?,14-,16-,18-/m1/s1
  • Key:GOHDSZGHAHFEHG-JZLGIKSISA-N

LY-86057 is a serotonin receptor modulator of the ergoline family.[1] It is the N1-desisopropyl analogue of the much better-known ergoline and serotonin receptor antagonist LY-53857.[1]

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.[1][2][3] 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.[2][4][5] LY-86057 is said to act as an antagonist of the serotonin 5-HT2A receptor.[6] It also shows high affinity for the serotonin 5-HT1F receptor (Ki = 12.2 nM).[7]

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).[4][2][5]

LY-86057 was first described in the scientific literature by 1993.[2][4][7]

See also

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References

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  1. 1 2 3 van Wijngaarden I, Soudijn W (1997). "5-HT2A, 5-HT2B and 5-HT2C receptor ligands". Pharmacochemistry Library. Vol. 27. Elsevier. pp. 161–197. doi:10.1016/s0165-7208(97)80013-x. ISBN 978-0-444-82041-9.
  2. 1 2 3 4 Nelson DL, Lucaites VL, Audia JE, Nissen JS, Wainscott DB (June 1993). "Species differences in the pharmacology of the 5-hydroxytryptamine2 receptor: structurally specific differentiation by ergolines and tryptamines". The Journal of Pharmacology and Experimental Therapeutics. 265 (3): 1272–1279. doi:10.1016/S0022-3565(25)38269-8. PMID 8510008.
  3. ↑ Wainscott DB, Lucaites VL, Kursar JD, Baez M, Nelson DL (February 1996). "Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences". The Journal of Pharmacology and Experimental Therapeutics. 276 (2): 720–727. doi:10.1016/S0022-3565(25)12346-X. PMID 8632342.
  4. 1 2 3 Johnson MP, Audia JE, Nissen JS, Nelson DL (August 1993). "N(1)-substituted ergolines and tryptamines show species differences for the agonist-labeled 5-HT2 receptor". European Journal of Pharmacology. 239 (1–3): 111–118. doi:10.1016/0014-2999(93)90983-o. PMID 8223886.
  5. 1 2 Johnson MP, Loncharich RJ, Baez M, Nelson DL (February 1994). "Species variations in transmembrane region V of the 5-hydroxytryptamine type 2A receptor alter the structure-activity relationship of certain ergolines and tryptamines". Molecular Pharmacology. 45 (2): 277–286. doi:10.1016/S0026-895X(25)09924-9. PMID 8114677.
  6. ↑ Johnson MP, Wainscott DB, Lucaites VL, Baez M, Nelson DL (October 1997). "Mutations of transmembrane IV and V serines indicate that all tryptamines do not bind to the rat 5-HT2A receptor in the same manner". Brain Research. Molecular Brain Research. 49 (1–2): 1–6. doi:10.1016/s0169-328x(97)00115-0. PMID 9387857.
  7. 1 2 Wainscott DB, Cohen ML, Schenck KW, Audia JE, Nissen JS, Baez M, et al. (March 1993). "Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor". Molecular Pharmacology. 43 (3): 419–426. doi:10.1016/S0026-895X(25)13628-6. PMID 8450835.
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