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LY 215840

Names

[ CAS No. ]:
137328-52-0

[ Name ]:
LY 215840

[Synonym ]:
[Orn8]-Urotensin II
Ergoline-8-carboxamide,N-(2-hydroxycyclopentyl)-6-methyl-1-(1-methylethyl)-,(8beta(1S,2R))
Ergoline-8-carboximide,N-(2-hydroxycyclopentyl)-6-methyl-1-(1-methylethyl)-,(8beta(1S,2R))
(4R,7R)-N-[(1S,2R)-2-hydroxycyclopentyl]-6-methyl-11-(propan-2-yl)-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(16),9,12,14-tetraene-4-carboxamide

Biological Activity

[Description]:

LY215840, a 5-HT7 receptor ligand and a 5-HT2 receptor antagonist, blocks serotonin-induced relaxation in canine coronary artery[1][2].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT2 Receptor

5-HT7 Receptor


[In Vitro]

LY215840 (1 μM) markedly potentiated contraction to 5-carboxamidotryptamine, the most potent coronary relaxant agonist and the agonist with the highest 5-HT7 receptor affinity[1]. LY215840 (3 x 10-10 to 10-8 M) blocks 5-HT2 receptors mediating contraction to 5-HT in vitro[2].

[References]

[1]. D J Cushing, et al. LY215840, a high-affinity 5-HT7 receptor ligand, blocks serotonin-induced relaxation in canine coronary artery. J Pharmacol Exp Ther. 1996 Jun;277(3):1560-6.  

[2]. M L Cohen , et al. 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. J Pharmacol Exp Ther. 1992 Apr;261(1):202-8.  

Chemical & Physical Properties

[ Density]:
1.34g/cm3

[ Boiling Point ]:
642.1ºC at 760mmHg

[ Molecular Formula ]:
C24H33N3O2

[ Molecular Weight ]:
395.54

[ Flash Point ]:
342.1ºC

[ Exact Mass ]:
395.25700

[ PSA ]:
60.99000

[ LogP ]:
3.99000

[ Vapour Pressure ]:
2.3E-17mmHg at 25°C

[ Index of Refraction ]:
1.689

Related Compounds