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Description: Potent and selective D1 antagonist
Chemical Name: 6,7,8,9,14,15-Hexahydro-7-methyl-5H-indolo[3,2-f][3]benzazecine
Purity: ≥98% (HPLC)
Biological Activity for LE 300
LE 300 is a 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.
Compound Libraries for LE 300
LE 300 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for LE 300
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for LE 300
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 14.52 | 50 | |
| DMSO | 29.04 | 100 |
Preparing Stock Solutions for LE 300
The following data is based on the product molecular weight 290.41. 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 | 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 for LE 300
References for LE 300
References are publications that support the biological activity of the product.
El-Subbagh et al (2002) DA/serotonin receptor ligands: Part IV [1]: Synthesis and pharmacology of novel 3-benzazecines and 3-benzazonines as potential 5-HT2A and DA 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 DA 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 DA receptor antagonists. J.Med.Chem. 43 2079 PMID: 10821720
If you know of a relevant reference for LE 300, please let us know.
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Keywords: LE 300, LE 300 supplier, Potent, selective, dopamine, D1, antagonists, Dopamine, Receptors, dopaminergic, LE300, and, D5, 1674, Tocris Bioscience
2 Citations for LE 300
Citations are publications that use Tocris products. Selected citations for LE 300 include:
Cilz et al (2014) DArgic modulation of GABAergic transmission in the entorhinal cortex: concerted roles of α1 adrenoreceptors, inward rectifier K+, and T-type Ca2+ channels. Cereb Cortex 24 3195 PMID: 23843440
Gildea et al (2012) DA and angiotensin type 2 receptors cooperatively inhibit sodium transport in human renal proximal tubule cells. Hypertension 60 396 PMID: 22710646
Do you know of a great paper that uses LE 300 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* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Dopamine Receptors Scientific Review
Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.
Addiction Poster
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
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.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.