LY-215,840

LY-215,840
Identifiers
	IUPAC name (6aR,9R,10aR)-N-((1S,2R)-2-hydroxycyclopentyl)-4-isopropyl-7-methyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline-9-carboxamide;
CAS Number	137328-52-0;
PubChem CID	9822062;
IUPHAR/BPS	180;
ChemSpider	7997811;
CompTox Dashboard (EPA)	DTXSID20929769 ;
Chemical and physical data
Formula	C24H33N3O2
Molar mass	395.547 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN1[C@]([C@]2([H])C[C@@H](C(N[C@@H]3[C@H](O)CCC3)=O)C1)([H])CC4=CN(C(C)C)C5=CC=CC2=C54;
	InChI InChI=1S/C24H33N3O2/c1-14(2)27-13-15-11-21-18(17-6-4-8-20(27)23(15)17)10-16(12-26(21)3)24(29)25-19-7-5-9-22(19)28/h4,6,8,13-14,16,18-19,21-22,28H,5,7,9-12H2,1-3H3,(H,25,29)/t16-,18-,19+,21-,22-/m1/s1; Key:IMSDOBUYDTVEHN-ILMFXRJHSA-N;

LY-215,840 is an ergoline derivative drug developed by Eli Lilly, which acts as a potent and selective antagonist at the serotonin 5-HT₂ and 5-HT₇ receptors. It has anti-hypertensive and muscle relaxant effects in animal studies.[1][2][3][4][5][6][7][8]

References

Cohen ML, Robertson DW, Bloomquist WE, Wilson HC (April 1992). "LY215840, a potent 5-hydroxytryptamine (5-HT)2 receptor antagonist, blocks vascular and platelet 5-HT2 receptors and delays occlusion in a rabbit model of thrombosis". The Journal of Pharmacology and Experimental Therapeutics. 261 (1): 202–8. PMID 1560366.
Cushing DJ, Zgombick JM, Nelson DL, Cohen ML (June 1996). "LY215840, a high-affinity 5-HT7 receptor ligand, blocks serotonin-induced relaxation in canine coronary artery". The Journal of Pharmacology and Experimental Therapeutics. 277 (3): 1560–6. PMID 8667223.
Terrón JA, Falcón-Neri A (June 1999). "Pharmacological evidence for the 5-HT7 receptor mediating smooth muscle relaxation in canine cerebral arteries". British Journal of Pharmacology. 127 (3): 609–16. doi:10.1038/sj.bjp.0702580. PMC 1566051. PMID 10401550.
Meneses A, Terrón JA (June 2001). "Role of 5-HT(1A) and 5-HT(7) receptors in the facilitatory response induced by 8-OH-DPAT on learning consolidation". Behavioural Brain Research. 121 (1–2): 21–8. doi:10.1016/S0166-4328(00)00378-8. PMID 11275281.
Watts SW, Yang P, Banes AK, Baez M (October 2001). "Activation of Erk mitogen-activated protein kinase proteins by vascular serotonin receptors". Journal of Cardiovascular Pharmacology. 38 (4): 539–51. doi:10.1097/00005344-200110000-00006. PMID 11588524.
Lenglet S, Louiset E, Delarue C, Vaudry H, Contesse V (May 2002). "Activation of 5-HT(7) receptor in rat glomerulosa cells is associated with an increase in adenylyl cyclase activity and calcium influx through T-type calcium channels". Endocrinology. 143 (5): 1748–60. doi:10.1210/endo.143.5.8817. PMID 11956157.
Meneses A (December 2002). "Involvement of 5-HT(2A/2B/2C) receptors on memory formation: simple agonism, antagonism, or inverse agonism?". Cellular and Molecular Neurobiology. 22 (5–6): 675–88. doi:10.1023/A:1021800822997. PMID 12585687.
Sánchez-Lopez A, Centurión D, Vázquez E, Arulmani U, Saxena PR, Villalón CM (October 2003). "Pharmacological profile of the 5-HT-induced inhibition of cardioaccelerator sympathetic outflow in pithed rats: correlation with 5-HT1 and putative 5-ht5A/5B receptors". British Journal of Pharmacology. 140 (4): 725–35. doi:10.1038/sj.bjp.0705489. PMC 1574076. PMID 14504136.

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[1] Cohen ML, Robertson DW, Bloomquist WE, Wilson HC (April 1992). "LY215840, a potent 5-hydroxytryptamine (5-HT)2 receptor antagonist, blocks vascular and platelet 5-HT2 receptors and delays occlusion in a rabbit model of thrombosis". The Journal of Pharmacology and Experimental Therapeutics. 261 (1): 202–8. PMID 1560366.

[2] Cushing DJ, Zgombick JM, Nelson DL, Cohen ML (June 1996). "LY215840, a high-affinity 5-HT7 receptor ligand, blocks serotonin-induced relaxation in canine coronary artery". The Journal of Pharmacology and Experimental Therapeutics. 277 (3): 1560–6. PMID 8667223.

[3] Terrón JA, Falcón-Neri A (June 1999). "Pharmacological evidence for the 5-HT7 receptor mediating smooth muscle relaxation in canine cerebral arteries". British Journal of Pharmacology. 127 (3): 609–16. doi:10.1038/sj.bjp.0702580. PMC 1566051. PMID 10401550.

[4] Meneses A, Terrón JA (June 2001). "Role of 5-HT(1A) and 5-HT(7) receptors in the facilitatory response induced by 8-OH-DPAT on learning consolidation". Behavioural Brain Research. 121 (1–2): 21–8. doi:10.1016/S0166-4328(00)00378-8. PMID 11275281.

[5] Watts SW, Yang P, Banes AK, Baez M (October 2001). "Activation of Erk mitogen-activated protein kinase proteins by vascular serotonin receptors". Journal of Cardiovascular Pharmacology. 38 (4): 539–51. doi:10.1097/00005344-200110000-00006. PMID 11588524.

[6] Lenglet S, Louiset E, Delarue C, Vaudry H, Contesse V (May 2002). "Activation of 5-HT(7) receptor in rat glomerulosa cells is associated with an increase in adenylyl cyclase activity and calcium influx through T-type calcium channels". Endocrinology. 143 (5): 1748–60. doi:10.1210/endo.143.5.8817. PMID 11956157.

[7] Meneses A (December 2002). "Involvement of 5-HT(2A/2B/2C) receptors on memory formation: simple agonism, antagonism, or inverse agonism?". Cellular and Molecular Neurobiology. 22 (5–6): 675–88. doi:10.1023/A:1021800822997. PMID 12585687.

[8] Sánchez-Lopez A, Centurión D, Vázquez E, Arulmani U, Saxena PR, Villalón CM (October 2003). "Pharmacological profile of the 5-HT-induced inhibition of cardioaccelerator sympathetic outflow in pithed rats: correlation with 5-HT1 and putative 5-ht5A/5B receptors". British Journal of Pharmacology. 140 (4): 725–35. doi:10.1038/sj.bjp.0705489. PMC 1574076. PMID 14504136.