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'''LY-215,840''' is an [[ergoline]] derivative drug developed by [[Eli Lilly and Company|Eli Lilly]], which acts as a potent and selective [[Antagonist (pharmacology)|antagonist]] at the [[serotonin]] [[5-HT2 receptor|5-HT<sub>2</sub>]] and [[5-HT7 receptor|5-HT<sub>7</sub>]] [[Receptor (biochemistry)|receptor]]s. It has anti-[[hypertension|hypertensive]] and [[muscle relaxant]] effects in animal studies.<ref>{{Cite pmid|1560366}}</ref><ref>{{Cite pmid|8667223}}</ref><ref>{{Cite pmid|10401550}}</ref><ref>{{Cite pmid|11275281}}</ref><ref>{{Cite pmid|11588524}}</ref><ref>{{Cite pmid|11956157}}</ref><ref>{{Cite pmid|12585687}}</ref><ref>{{Cite pmid|14504136}}</ref>
'''LY-215,840''' is an [[ergoline]] derivative drug developed by [[Eli Lilly and Company|Eli Lilly]], which acts as a potent and selective [[Antagonist (pharmacology)|antagonist]] at the [[serotonin]] [[5-HT2 receptor|5-HT<sub>2</sub>]] and [[5-HT7 receptor|5-HT<sub>7</sub>]] [[Receptor (biochemistry)|receptor]]s. It has anti-[[hypertension|hypertensive]] and [[muscle relaxant]] effects in animal studies.<ref>{{Cite journal
| last1 = Cohen | first1 = M. L.
| last2 = Robertson | first2 = D. W.
| last3 = Bloomquist | first3 = W. E.
| last4 = Wilson | first4 = H. C.
| title = 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
| journal = The Journal of pharmacology and experimental therapeutics
| volume = 261
| issue = 1
| pages = 202–208
| year = 1992
| pmid = 1560366
}}</ref><ref>{{Cite journal
| last1 = Cushing | first1 = D. J.
| last2 = Zgombick | first2 = J. M.
| last3 = Nelson | first3 = D. L.
| last4 = Cohen | first4 = M. L.
| title = LY215840, a high-affinity 5-HT7 receptor ligand, blocks serotonin-induced relaxation in canine coronary artery
| journal = The Journal of pharmacology and experimental therapeutics
| volume = 277
| issue = 3
| pages = 1560–1566
| year = 1996
| pmid = 8667223
}}</ref><ref>{{Cite journal
| last1 = Terrón | first1 = J. A.
| last2 = Falcón-Neri | first2 = A.
| doi = 10.1038/sj.bjp.0702580
| title = Pharmacological evidence for the 5-HT7receptor mediating smooth muscle relaxation in canine cerebral arteries
| journal = British Journal of Pharmacology
| volume = 127
| issue = 3
| pages = 609–616
| year = 1999
| pmid = 10401550
| pmc =1566051
}}</ref><ref>{{Cite journal
| doi = 10.1016/S0166-4328(00)00378-8
| last1 = Meneses | first1 = A.
| last2 = Terrón | first2 = J. A.
| title = Role of 5-HT(1A) and 5-HT(7) receptors in the facilitatory response induced by 8-OH-DPAT on learning consolidation
| journal = Behavioural brain research
| volume = 121
| issue = 1–2
| pages = 21–28
| year = 2001
| pmid = 11275281
}}</ref><ref>{{Cite journal
| doi = 10.1097/00005344-200110000-00006
| last1 = Watts | first1 = S. W.
| last2 = Yang | first2 = P.
| last3 = Banes | first3 = A. K.
| last4 = Baez | first4 = M.
| title = Activation of Erk mitogen-activated protein kinase proteins by vascular serotonin receptors
| journal = Journal of cardiovascular pharmacology
| volume = 38
| issue = 4
| pages = 539–551
| year = 2001
| pmid = 11588524
}}</ref><ref>{{Cite journal
| doi = 10.1210/en.143.5.1748
| last1 = Lenglet | first1 = S.
| last2 = Louiset | first2 = E.
| last3 = Delarue | first3 = C.
| last4 = Vaudry | first4 = H.
| last5 = Contesse | first5 = V.
| title = 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
| journal = Endocrinology
| volume = 143
| issue = 5
| pages = 1748–1760
| year = 2002
| pmid = 11956157
}}</ref><ref>{{Cite journal
| doi = 10.1023/A:1021800822997
| last1 = Meneses | first1 = A.
| title = Involvement of 5-HT(2A/2B/2C) receptors on memory formation: Simple agonism, antagonism, or inverse agonism?
| journal = Cellular and molecular neurobiology
| volume = 22
| issue = 5–6
| pages = 675–688
| year = 2002
| pmid = 12585687
}}</ref><ref>{{Cite journal
| last1 = Sánchez-López | first1 = A.
| last2 = Centurión | first2 = D.
| last3 = Vázquez | first3 = E.
| last4 = Arulmani | first4 = U.
| last5 = Saxena | first5 = P. R.
| last6 = Villalón | first6 = C. M.
| doi = 10.1038/sj.bjp.0705489
| title = Pharmacological profile of the 5-HT-induced inhibition of cardioaccelerator sympathetic outflow in pithed rats: Correlation with 5-HT1and putative 5-ht5A/5Breceptors
| journal = British Journal of Pharmacology
| volume = 140
| issue = 4
| pages = 725–735
| year = 2003
| pmid = 14504136
| pmc =1574076
}}</ref>




Revision as of 04:59, 28 August 2015

LY-215,840
Identifiers
  • (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
PubChem CID
IUPHAR/BPS
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC24H33N3O2
Molar mass395.54 g/mol g·mol−1
3D model (JSmol)
  • 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

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

  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.
  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.
  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.
  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.
  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.
  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.
  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.
  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.


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