LY 215840
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
Do you know of a great paper that uses LY 215840 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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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.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
