LE 300

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].

Product Specifications

CAS Number

[274694-98-3]

UNSPSC

12352005

Target

5-HT Receptor; Dopamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/le-300.html

Purity

98.5

Solubility

DMSO : 29.04 mg/mL (ultrasonic; warming)

Smiles

CN1CCC2=C(NC3=C2C=CC=C3)CC4=CC=CC=C4CC1

Molecular Formula

C20H22N2

Molecular Weight

290.40

References & Citations

[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.