LY 215840

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Cat.No. 1523 - LY 215840 | C24H33N3O2 | CAS No. 137328-52-0
Description: 5-HT2/5-HT7 antagonist
Chemical Name: [8β(1S,2R)]-N-(2-Hydroxycyclopentyl)-6-methyl-1-(1-methylethyl)-ergoline-8-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations (4)
Reviews
Literature

Biological Activity

5-HT2/5-HT7 receptor antagonist. Reduces stimulatory effect of serotonin on aldosterone secretion; also reduces 5-HT-induced cAMP formation (pKB = 8.26).

Technical Data

M. Wt 395.54
Formula C24H33N3O2
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 137328-52-0
PubChem ID 9822062
InChI Key IMSDOBUYDTVEHN-ILMFXRJHSA-N
Smiles CC(C)N2C1=C(C(C[C@]4([H])[C@@]([H])3C[C@@H]([C@@](N[C@@H]5[C@H](O)CCC5)=O)CN4C)=C2)C3=CC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.55 100
ethanol 9.89 25

Preparing Stock Solutions

The following data is based on the product molecular weight 395.54. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.53 mL 12.64 mL 25.28 mL
5 mM 0.51 mL 2.53 mL 5.06 mL
10 mM 0.25 mL 1.26 mL 2.53 mL
50 mM 0.05 mL 0.25 mL 0.51 mL

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References

References are publications that support the biological activity of the product.

Cushing et al (1996) LY215840, a high-affinity 5-HT7 receptor ligand, blocks serotonin-induced relaxation in canine coronary artery. J.Pharmacol.Exp.Ther. 277 1560 PMID: 8667223

Lenglet et al (2002) Activation of 5-HT7 receptor in rat glomerulosa cells is associated with an increase in adenylyl cyclase activity and calcium influx through T-type calcium channels. Endocrinology 143 1748 PMID: 11956157

Louiset et al (2006) Expression of serotonin7 receptor and coupling of ectopic receptors to protein kinase A and ionic currents in adrenocorticotropin-independent macronodular adrenal hyperplasia causing Cushing's syndrome. J.Clin.Endocrinol.Metab. 91 4578 PMID: 16954157


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Keywords: LY 215840, LY 215840 supplier, LY215840, 5-ht, serotonin, receptors, antagonists, 5ht2, 5ht7, 5-hydroxytryptamine, Non-selective, 5-HT, 5-HT2, 5-HT7, Receptors, 1523, Tocris Bioscience

4 Citations for LY 215840

Citations are publications that use Tocris products. Selected citations for LY 215840 include:

Watts et al (2015) 5-HT is a potent relaxant in rat superior mesenteric veins. PLoS Negl Trop Dis 3 e00103 PMID: 25692021

Chan et al (2015) Ergot Alkaloids (Re)generate New Leads as Antiparasitics. BMC Neurosci 9 e0004063 PMID: 26367744

Chan et al (2016) A Miniaturized Screen of a Schistosoma mansoni Serotonergic G Protein-Coupled Receptor Identifies Novel Classes of Parasite-Selective Inhibitors. PLoS Pathog 12 e1005651 PMID: 27187180

Du et al (2015) Adrenergic and serotonin receptors affect retinal superoxide generation in diabetic mice: relationship to capillary degeneration and permeability. FASEB J 29 2194 PMID: 25667222


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Literature in this Area

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5-HT Receptors Scientific Review

Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.

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