274694-98-3
Chemical Structure
LE 300
- CAS No.: 274694-98-3
- Formula:C20H22N2
- Molecular Weight:290.40
IUPAC Name: 7-methyl-6,7,8,9,14,15-hexahydro-5H-benzo[7,8]azecino[5,4-b]indole
InChIKey: YEWGIGCYIAMFMA-UHFFFAOYSA-N
SMILES: CN1CCC2=C(NC3=C2C=CC=C3)CC4=CC=CC=C4CC1
Biological Activity: LE 300 is a potent and selective dopamine D1-like receptor antagonist with Kis of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT2A receptor with a pA2 of 8.32 in a rat tail artery assay[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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LE 300 | 98.5% | LE 300 is a potent and selective dopamine D1-like receptor antagonist with Kis of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT2A receptor with a pA2 of 8.32 in a rat tail artery assay. | ||||||||||||||||||||
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References
- [1]. 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. [Content Brief]
- [2]. 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. [Content Brief]