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LE 300

Catalog No. T22921   CAS 274694-98-3

LE 300 represents a structurally novel type of antagonists acting preferentially at the dopamine D(1)/D(5)receptors and the serotonin 5-HT(2A)receptor.

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LE 300 Chemical Structure
LE 300, CAS 274694-98-3
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Biological Description
Chemical Properties
Storage & Solubility Information
Description LE 300 represents a structurally novel type of antagonists acting preferentially at the dopamine D(1)/D(5)receptors and the serotonin 5-HT(2A)receptor.
Targets&IC50 dopamine D1 receptor:1.9 nM (Ki,Human), 5-HT2A:8.32 (pA2,rat), dopamine D5 receptor:7.5 nM (Ki,Human)
In vitro The Kis of LE 300 are 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. In a rat tail artery experiment, the pA2 value of LE 300 at the 5-HT2A receptor was 8.32[2].
Molecular Weight 290.4
Formula C20H22N2
CAS No. 274694-98-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

1eq. HCl: <15 mg/ml(51.65 mM)

DMSO: <30 mg/ml(103.30 mM)

TargetMolReferences and Literature

1. Rostom SA. Novel fused pyrrole heterocyclic ring systems as structure analogs of LE 300: Synthesis and pharmacological evaluation as serotonin 5-HT(2A), dopamine and histamine H(1) receptor ligands. Arch Pharm (Weinheim). 2010 Feb;343(2):73-80. 2. Kassack MU, et al. 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. 2002 Dec;366(6):543-50. 3. Hefnawy M, et al. Spectrofluorimetric determination of dopamine receptor antagonist LE 300 in mice plasma. Luminescence. 2016 Feb;31(1):63-6.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Parkinson's Disease Compound Library Anti-Neurodegenerative Disease Compound Library

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Keywords

LE 300 274694-98-3 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor inhibit Inhibitor LE300 LE-300 Serotonin Receptor 5-hydroxytryptamine Receptor inhibitor

 

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