LY-215,840

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LY-215,840
LY-215840 structure.png
Systematic (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
Clinical data
Legal status ?
Identifiers
CAS number 137328-52-0
ATC code ?
PubChem CID 132049
Chemical data
Formula C24H33N3O2 
Mol. mass 395.54 g/mol

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[edit]

  1. ^ Cohen, M. L.; Robertson, D. W.; Bloomquist, W. E.; Wilson, H. C. (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): 202–208. PMID 1560366.  edit
  2. ^ Cushing, D. J.; Zgombick, J. M.; Nelson, D. L.; Cohen, M. L. (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): 1560–1566. PMID 8667223.  edit
  3. ^ Terrón, J. A.; Falcón-Neri, A. (1999). "Pharmacological evidence for the 5-HT7receptor mediating smooth muscle relaxation in canine cerebral arteries". British Journal of Pharmacology 127 (3): 609–616. doi:10.1038/sj.bjp.0702580. PMC 1566051. PMID 10401550.  edit
  4. ^ Meneses, A.; Terrón, J. A. (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): 21–28. doi:10.1016/S0166-4328(00)00378-8. PMID 11275281.  edit
  5. ^ Watts, S. W.; Yang, P.; Banes, A. K.; Baez, M. (2001). "Activation of Erk mitogen-activated protein kinase proteins by vascular serotonin receptors". Journal of cardiovascular pharmacology 38 (4): 539–551. doi:10.1097/00005344-200110000-00006. PMID 11588524.  edit
  6. ^ Lenglet, S.; Louiset, E.; Delarue, C.; Vaudry, H.; Contesse, V. (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): 1748–1760. doi:10.1210/en.143.5.1748. PMID 11956157.  edit
  7. ^ Meneses, A. (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): 675–688. doi:10.1023/A:1021800822997. PMID 12585687.  edit
  8. ^ Sánchez-López, A.; Centurión, D.; Vázquez, E.; Arulmani, U.; Saxena, P. R.; Villalón, C. M. (2003). "Pharmacological profile of the 5-HT-induced inhibition of cardioaccelerator sympathetic outflow in pithed rats: Correlation with 5-HT1and putative 5-ht5A/5Breceptors". British Journal of Pharmacology 140 (4): 725–735. doi:10.1038/sj.bjp.0705489. PMC 1574076. PMID 14504136.  edit