LY-215,840 explained

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]}

Notes and References

1. Cohen ML, Robertson DW, Bloomquist WE, Wilson HC . 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 . April 1992 . 1560366 .
2. Cushing DJ, Zgombick JM, Nelson DL, Cohen ML . 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 . June 1996 . 8667223 .
3. Terrón JA, Falcón-Neri A . Pharmacological evidence for the 5-HT7 receptor mediating smooth muscle relaxation in canine cerebral arteries . British Journal of Pharmacology . 127 . 3 . 609–16 . June 1999 . 10401550 . 1566051 . 10.1038/sj.bjp.0702580 .
4. Meneses A, Terrón JA . 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 . June 2001 . 11275281 . 10.1016/S0166-4328(00)00378-8 . 26090343 .
5. Watts SW, Yang P, Banes AK, Baez M . Activation of Erk mitogen-activated protein kinase proteins by vascular serotonin receptors . Journal of Cardiovascular Pharmacology . 38 . 4 . 539–51 . October 2001 . 11588524 . 10.1097/00005344-200110000-00006 . 43167169 . free .
6. Lenglet S, Louiset E, Delarue C, Vaudry H, Contesse V . 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 . May 2002 . 11956157 . 10.1210/endo.143.5.8817 . free .
7. Meneses A . 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 . December 2002 . 12585687 . 10.1023/A:1021800822997 . 25703079 .
8. Sánchez-Lopez A, Centurión D, Vázquez E, Arulmani U, Saxena PR, Villalón CM . 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 . October 2003 . 14504136 . 1574076 . 10.1038/sj.bjp.0705489 .