LE 300

Modify Date: 2024-01-03 09:32:08

LE 300 Structure
LE 300 structure
Common Name LE 300
CAS Number 274694-98-3 Molecular Weight 290.40200
Density 1.114g/cm3 Boiling Point 464ºC at 760 mmHg
Molecular Formula C20H22N2 Melting Point N/A
MSDS Chinese USA Flash Point 234.4ºC

 Use of 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].

 Names

Name le 300
Synonym More Synonyms

 LE 300 Biological Activity

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
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.

 Chemical & Physical Properties

Density 1.114g/cm3
Boiling Point 464ºC at 760 mmHg
Molecular Formula C20H22N2
Molecular Weight 290.40200
Flash Point 234.4ºC
Exact Mass 290.17800
PSA 19.03000
LogP 3.72700
Vapour Pressure 8.69E-09mmHg at 25°C
Index of Refraction 1.63

 Synonyms

Tocris-1674
Lopac-L-8401