Chemistry: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;
UNII	D2G5U4P5B3;
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;

Short description: Chemical compound

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

↑ "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. PMID 1560366.
↑ "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. PMID 8667223.
↑ "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. doi:10.1038/sj.bjp.0702580. PMID 10401550.
↑ "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. doi:10.1016/S0166-4328(00)00378-8. PMID 11275281.
↑ "Activation of Erk mitogen-activated protein kinase proteins by vascular serotonin receptors". Journal of Cardiovascular Pharmacology 38 (4): 539–51. October 2001. doi:10.1097/00005344-200110000-00006. PMID 11588524.
↑ "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. doi:10.1210/endo.143.5.8817. PMID 11956157.
↑ "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. doi:10.1023/A:1021800822997. PMID 12585687.
↑ "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. doi:10.1038/sj.bjp.0705489. PMID 14504136.

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Original source: https://en.wikipedia.org/wiki/LY-215,840. Read more

[1] "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. PMID 1560366.

[2] "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. PMID 8667223.

[3] "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. doi:10.1038/sj.bjp.0702580. PMID 10401550.

[4] "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. doi:10.1016/S0166-4328(00)00378-8. PMID 11275281.

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

[6] "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. doi:10.1210/endo.143.5.8817. PMID 11956157.

[7] "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. doi:10.1023/A:1021800822997. PMID 12585687.

[8] "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. doi:10.1038/sj.bjp.0705489. PMID 14504136.

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v t e Ergolines
Lysergic acid derivatives	2-Bromo-LSD (BOL-148) Bromocriptine Cabergoline Dihydroergocornine Dihydroergocristine Dihydroergocryptine Dihydroergometrine (Dihydroergonovine, Dihydroergobasine) Dihydroergosine Dihydroergotamine Epicriptine Ergine (LSA; LA-111; Lysergamide) Ergocornine Ergocristine Ergocryptine Ergoloid (Dihydroergotoxine) Ergometrine (Ergonovine, Ergobasine) Ergometrinine Ergotamine Ergotoxine Ergovaline Lisuride LSD LSH Lysergic Acid Lysergic acid cyclobutylamide Lysergic acid cyclopentylamide Lysergic Acid Methyl Ester Lysergol Mesulergine Metergoline Methergine (Methylergometrine, Methylergonovine, Methylergobasine) Methysergide Pergolide Syntometrine
Psychedelic lysergamides	1B-LSD 1P-ETH-LAD 1P-LSD AL-LAD ALD-52 BU-LAD CYP-LAD DAL DAM-57 ECPLA Ergonovine ETFELA ETH-LAD IP-LAD LAMPA LAE-32 LSD LPD-824 LSM-775 LSH LSD-Pip Lysergic Acid 2-Butylamide Lysergic Acid 2,4-Dimethylazetidide Lysergic Acid 3-Pentylamide Methylergonovine MIPLA MLD-41 PARGY-LAD PRO-LAD
clavines	agroclavine elymoclavine lysergol festuclavine fumigaclavine A fumigaclavine B fumigaclavine C
Other ergolines	Ergoline
Natural sources	Achnatherum robustum (Sleepy Grass) Claviceps spp. (Ergot) Morning glory: Argyreia nervosa (Hawaiian Baby Woodrose), Ipomoea spp.(Morning Glory, Tlitliltzin, Badoh Negro), Rivea corymbosa (Coaxihuitl, Ololiúqui)

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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^Y
PubChem CID	9822062
IUPHAR/BPS	180
ChemSpider	7997811
UNII	D2G5U4P5B3
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

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