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.
All Tocris products are intended for laboratory research use only.
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 products' biological activity.
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
Keywords: LY 215840, supplier, LY215840, 5-ht, serotonin, receptors, antagonists, 5ht2, 5ht7, 5-hydroxytryptamine, Non-selective, 5-HT, Non-selective, 5-HT2, 5-HT7, Receptors, Non-selective, 5-HT, Tocris Bioscience
