LE 300

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Cat.No. 1674 - LE 300 | C20H22N2 | CAS No. 274694-98-3
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)
Datasheet
Citations (2)
Reviews
Literature

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
1eq. HCl 14.52 50
DMSO 29.04 100

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

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References

References are publications that support the biological activity of the product.

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


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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:

Gildea et al (2012) Dopamine and angiotensin type 2 receptors cooperatively inhibit sodium transport in human renal proximal tubule cells. Hypertension 60 396 PMID: 22710646

Cilz et al (2014) Dopaminergic 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


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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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