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Submit ReviewLY 215840
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)
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 the degree 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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Product Datasheets
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:
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
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
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Reviews for LY 215840
Average Rating: 3 (Based on 1 Review.)
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5-HT has a potential for relaxant.
By
Anonymous on 02/18/2020
Assay Type: In Vivo
Species: Rat
1nM 5-HT7 receptor antagonists LY215840
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