Biological Activity
Potent and selective dopamine D1 receptor antagonist (Ki values are 0.08 - 1.9 nM and 6 - 45 nM for D1 and D2 receptors respectively). Also displays moderate affinity for the 5-HT2A receptor (Ki = 20 nM). Active in vivo.
Technical Data
| M. Wt | 290.41 |
| Formula | C20H22N2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 274694-98-3 |
| PubChem ID | 4350931 |
| InChI Key | YEWGIGCYIAMFMA-UHFFFAOYSA-N |
| Smiles | CN1CCC2=C(CC3=CC=CC=C3CC1)NC1=CC=CC=C21 |
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 | |||
| 1eq. HCl | 14.52 | 50 | |
| DMSO | 29.04 | 100 | |
| ethanol | 2.9 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 290.41. 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 | 3.44 mL | 17.22 mL | 34.43 mL |
| 5 mM | 0.69 mL | 3.44 mL | 6.89 mL |
| 10 mM | 0.34 mL | 1.72 mL | 3.44 mL |
| 50 mM | 0.07 mL | 0.34 mL | 0.69 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
El-Subbagh et al (2002) Dopamine/serotonin receptor ligands: Part IV [1]: Synthesis and pharmacology of novel 3-benzazecines and 3-benzazonines as potential 5-HT2A and dopamine receptor ligands. Arch.Pharm. (Weinheim). 9 443 PMID: 12447918
Kassack et al (2002) Pharmacological characterization of the benz[d]indolo[2,3-g]azecine LE300, a novel type of a nanomolar dopamine receptor antagonist. Naunyn Schmiedebergs Arch.Pharmacol. 366 543 PMID: 12444495
Witt et al (2000) 7-Methyl-6,7,8,9,14,15-hexahydro-5H-benz[d]indolo[2,3-g]azecine: a new heterocyclic system and a new lead compound for dopamine receptor antagonists. J.Med.Chem. 43 2079 PMID: 10821720
Keywords: LE 300, supplier, Potent, selective, dopamine, D1, antagonists, Dopamine, Receptors, dopaminergic, LE300, D1, and, D5, Receptors, D1, and, D5, Receptors, Tocris Bioscience
