L-745870 (trihydrochloride)

L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors[1][2][3].

Product Specifications

CAS Number

[866021-03-6]

UNSPSC

12352005

Hazard Statement

H302-H315-H319

Target

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/l-745870-trihydrochloride.html

Solubility

10 mM in DMSO

Smiles

ClC(C=C1)=CC=C1N(CC2)CCN2CC3=CNC4=NC=CC=C43.Cl.Cl.Cl

Molecular Formula

C18H22Cl4N4

Molecular Weight

436.21

Precautions

P264-P270-P280-P302+P352-P305+P351+P338-P330-P362+P364-P501

References & Citations

[1]Bristow LJ, et al. Schizophrenia and L-745,870, a novel dopamine D4 receptor antagonist. Trends Pharmacol Sci. 1997 Jun;18 (6) :186-8.|[2]Patel S, et al. Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor. J Pharmacol Exp Ther. 1997 Nov;283 (2) :636-47.|[3]Kulagowski JJ, et al. 3- ((4- (4-Chlorophenyl) piperazin-1-yl) -methyl) -1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. J Med Chem. 1996 May 10;39 (10) :1941-2.