274694-98-3

274694-98-3 structure

Name: LE 300
Chemical Name: le 300
CAS Number: 274694-98-3
Molecular Formula: C₂₀H₂₂N₂
Molecular Weight: 290.40200
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2016-02-12 08:35:10
Modify Date: 2024-01-03 09:32:08
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].

Name	le 300
Synonyms	Tocris-1674 Lopac-L-8401

Description	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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	Human D1 Receptor:1.9 nM (Ki) Human D5 Receptor:7.5 nM (Ki) Rat 5-HT2A:8.32 (pA2)
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. [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.