Sergolexole
Sergolexole structure.png
Identifiers
  • (4-methoxycyclohexyl) (6aR,9R,10aR)-7-methyl-4-propan-2-yl-6,6a,8,9,10,10a-hexahydroindolo[4,3-fg]quinoline-9-carboxylate
CAS Number
PubChem CID
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC26H36N2O3
Molar mass424.585 g·mol−1
3D model (JSmol)
  • CC(C)N1C=C2C[C@@H]3[C@H](C[C@H](CN3C)C(=O)OC4CCC(CC4)OC)C5=C2C1=CC=C5
  • InChI=1S/C26H36N2O3/c1-16(2)28-15-17-13-24-22(21-6-5-7-23(28)25(17)21)12-18(14-27(24)3)26(29)31-20-10-8-19(30-4)9-11-20/h5-7,15-16,18-20,22,24H,8-14H2,1-4H3/t18-,19?,20?,22-,24-/m1/s1
  • Key:RJBJIKXTJIZONR-FTNAIZGWSA-N

Sergolexole (developmental code name LY-281,067) is an ergoline derivative which acts as a selective antagonist of the serotonin 5-HT2 receptors. It has been used for various research applications, but was never developed for medical use.[1][2][3]

References

  1. ^ Cohen ML, Fuller RW, Kurz KD, Parli CJ, Mason NR, Meyers DB, et al. (January 1988). "Preclinical pharmacology of a new serotonergic receptor antagonist, LY281067". The Journal of Pharmacology and Experimental Therapeutics. 244 (1): 106–12. PMID 3335993.
  2. ^ Cohen ML, Parli CJ, Fuller RW (December 1989). "5-Hydroxytryptamine2 receptor antagonist activity of the acid metabolite (1-isopropyl dihydrolysergic acid) of the ergoline ester, sergolexole (LY281067)". The Journal of Pharmacology and Experimental Therapeutics. 251 (3): 1006–11. PMID 2600800.
  3. ^ Koba S, Pakala R, Watanabe T, Katagiri T, Benedict CR (November 1999). "Vascular smooth muscle proliferation: synergistic interaction between serotonin and low density lipoproteins". Journal of the American College of Cardiology. 34 (5): 1644–51. doi:10.1016/s0735-1097(99)00349-6. PMID 10551718.