L-745,870 trihydrochloride

Cat. No. 1002

L-745,870 trihydrochloride C18H19N4Cl.3HCl [866021-03-6]

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Chemical Name: 3-(4-[4-Chlorophenyl]piperazin-1-yl)-methyl-1H-pyrrolo[2,3-b]pyridine trihydrochloride

Biological Activity

A highly potent and selective D4 dopamine receptor antagonist; L-745,870 has Ki values of 0.51, 2300 and 960 nM for D4, D3 and D2 subtypes respectively and > 1000-fold selectivity over 5-HT2, D1 and D5 receptors.

Licensing Information

Sold with the permission of Merck Sharp and Dohme Ltd.

Technical Data

Soluble to 100 mM in water
>99 %
Desiccate at +4°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Pillai et al (1998) Human D2 and D4 dopamine receptors couple through βγ G-protein subunits to inwardly rectifying K+ channels (GIRK1) in a Xenopus oocyte expression system: selective antagonism by L-741,626 and L-745,870 respectively. Neuropharmacology 37 983. PMID: 9833627.

Bristow et al (1997) Schizophrenia and L-745, 870 a novel dopamine D4 receptor antagonist. TiPS 18 186. PMID: 9226994.

Patel et al (1997) Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor. J.Pharmacol.Exp.Ther. 283 636. PMID: 9353380.

Kulagowski et al (1996) 3-[[4-(4-Chlorophenyl)piperazin-1-yl]methyl-1H-pyrrolo[2,3-b]pyridine: an antagonist with high affinity and selectivity for the human D4 receptor. J.Med.Chem. 39 1941. PMID: 8642550.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for L-745,870 trihydrochloride include:

Chen et al (2015) Activation of D4 dopamine receptor decreases angiotensin II type 1 receptor expression in rat renal proximal tubule cells. Autophagy 65 153. PMID: 25368031.

Jensen (2015) Effects of Dopamine D2-Like Receptor Antagonists on Light Responses of Ganglion Cells in Wild-Type and P23H Rat Retinas. PLoS One 10 e0146154. PMID: 26717015.

Steullet et al (2014) Fast oscillatory activity in the anterior cingulate cortex: dopaminergic modulation and effect of perineuronal net loss. Front Cell Neurosci 8 244. PMID: 25191228.

Suárez-Boomgaard et al (2014) Dopamine D4 receptor counteracts morphine-induced changes in opioid receptor signaling in the striosomes of the rat caudate putamen. Int J Mol Sci 15 1481. PMID: 24451133.

Okada et al (2005) A dopamine D4 receptor antagonist attenuates ischemia-induced neuronal cell damage via upregulation of neuronal apoptosis inhibitory protein. Hypertension 25 794. PMID: 15729293.

Do you know of a great paper that uses L-745,870 trihydrochloride from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: L-745,870 trihydrochloride, supplier, selective, D4, antagonists, Dopamine, Receptors, dopaminergic, L745870, Tocris Bioscience, D4 Receptor Antagonist products

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