LE 300
Chemical Name: 6,7,8,9,14,15-Hexahydro-7-methyl-5H-indolo[3,2-f][3]benzazecine
Purity: ≥98%
Biological Activity
LE 300 is a potent and selective dopamine D1 receptor antagonist (Ki values are 0.08 - 1.9 nM and 6 - 45 nM for D1 and D2 receptors respectively). Also displays moderate affinity for the 5-HT2A receptor (Ki = 20 nM). Active in vivo.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Treatment with the antipsychotic agent, risperidone, reduces disease severity in experimental autoimmune encephalomyelitis.
O'Sullivan D, Green L, Stone S, Zareie P, Kharkrang M, Fong D, Connor B, La Flamme A
PLoS ONE, 2014;9(8):e104430. -
DA/serotonin receptor ligands: Part IV [1]: Synthesis and pharmacology of novel 3-benzazecines and 3-benzazonines as potential 5-HT2A and DA receptor ligands.
El-Subbagh et al.
Arch.Pharm. (Weinheim)., 2002;9:443 -
Pharmacological characterization of the benz[d]indolo[2,3-g]azecine LE300, a novel type of a nanomolar DA receptor antagonist.
Kassack et al.
Naunyn Schmiedebergs Arch.Pharmacol., 2002;366:543 -
7-Methyl-6,7,8,9,14,15-hexahydro-5H-benz[d]indolo[2,3-g]azecine: a new heterocyclic system and a new lead compound for DA receptor antagonists.
Witt et al.
J.Med.Chem., 2000;43:2079
Product Datasheets
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Citations for LE 300
The citations listed below are publications that use Tocris products. Selected citations for LE 300 include:
2 Citations: Showing 1 - 2
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DArgic modulation of GABAergic transmission in the entorhinal cortex: concerted roles of α1 adrenoreceptors, inward rectifier K+, and T-type Ca2+ channels.
Authors: Cilz Et al.
Cereb Cortex 2014;24:3195
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DA and angiotensin type 2 receptors cooperatively inhibit sodium transport in human renal proximal tubule cells.
Authors: Gildea Et al.
Hypertension 2012;60:396
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