L-745,870 trihydrochloride

Name: L-745,870 trihydrochloride
Brand: Tocris Bioscience
SKU: 1002
Rating: 5 (1 reviews)

Catalog # 1002

Citations (13)

(1)

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Key Product Details

Description:	Highly selective D₄ antagonist
Chemical Name:	3-(4-[4-Chlorophenyl]piperazin-1-yl)-methyl-1H-pyrrolo[2,3-b]pyridine trihydrochloride
Purity:	≥99% (HPLC)
Molecular Weight:	436.21

View Full Technical Details for L-745,870 trihydrochloride

Biological Activity

L-745,870 trihydrochloride is a highly potent and selective D₄ dopamine receptor antagonist; L-745,870 has K_i 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

M. Wt	436.21
Formula	C₁₈H₁₉N₄Cl.3HCl
Storage	Desiccate at +4°C
Purity	≥99% (HPLC)
CAS Number	866021-03-6
PubChem ID	49759035
InChi Key	KJSOYZLYCFYXFC-UHFFFAOYSA-N
Smiles	Cl.Cl.Cl.ClC1=CC=C(C=C1)N1CCN(CC2=CNC3=NC=CC=C23)CC1

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.

Solubility

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	water	43.62	100

Preparing Stock Solutions

The following data is based on the product molecular weight 436.21.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.29 mL	11.46 mL	22.92 mL
5 mM	0.46 mL	2.29 mL	4.58 mL
10 mM	0.23 mL	1.15 mL	2.29 mL
50 mM	0.05 mL	0.23 mL	0.46 mL

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References

References are publications that support the biological activity of the product.

Pillai Human D2 and D4 DA 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 respect Neuropharmacology 1998 PMID: 9833627
Bristow Schizophrenia and L-745, 870 a novel DA D₄ receptor antagonist. TiPS 1997 PMID: 9226994
Patel Biological profile of L-745,870, a selective antagonist with high affinity for the DA D₄ receptor. J.Pharmacol.Exp.Ther. 1997 PMID: 9353380
Kulagowski 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. 1996 PMID: 8642550

Citations for L-745,870 trihydrochloride (13)

Showing 1 - 10 of 13 citations Showing All

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

Sharma et al. (2021) Epithelial phenotype restoring drugs suppress macular degeneration phenotypes in an iPSC model. Nat Commun. 12:7293
PMID: 34911940
Matsui and Alvarez (2018) Cocaine Inhibition of Synaptic Transmission in the Ventral Pallidum Is Pathway-Specific and Mediated by Serotonin. Cell Rep. 23(13):3852
PMID: 29949769
Huang (2017) Neurochemical arguments for the use of DA D4 receptor stimulation to improve cognitive impairment associated with schizophrenia. Pharmacol Biochem Behav. 157:16
PMID: 28455127
Guo (2017) DA D4 receptor activation restores CA1 LTP in hippocampal slices from aged mice. Aging Cell. 16(6):1323
PMID: 28975698
Dai et al. (2017) Is DA transporter-mediated DArgic signaling in the retina a noninvasive biomarker for attention-deficit/ hyperactivity disorder? A study in a novel DA transporter variant Val559 transgenic mouse model. J Neurodev Disord. 9:38
PMID: 29281965
Picton et al. (2016) Mechanisms underlying the endogenous DArgic inhibition of spinal locomotor circuit function in Xenopus tadpoles. Scientific Reports. 6:35749
PMID: 27760989
Jensen (2015) Effects of DA D2-Like Receptor Antagonists on Light Responses of Ganglion Cells in Wild-Type and P23H Rat Retinas. PLoS One. 10:e0146154
PMID: 26717015
Chen et al. (2015) Activation of D4 DA receptor decreases angiotensin II type 1 receptor expression in rat renal proximal tubule cells. Autophagy. 65:153
PMID: 25368031
Suárez-Boomgaard et al. (2014) DA 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
Steullet et al. (2014) Fast oscillatory activity in the anterior cingulate cortex: DArgic modulation and effect of perineuronal net loss. Front Cell Neurosci. 8:244
PMID: 25191228
Herwerth et al. (2012) D4 DA receptors modulate NR2B NMDA receptors and LTP in stratum oriens of hippocampal CA1. Cereb Cortex. 22:1786
PMID: 21955919
Okada et al. (2005) A DA D4 receptor antagonist attenuates ischemia-induced neuronal cell damage via upregulation of neuronal apoptosis inhibitory protein. Hypertension. 25:794
PMID: 15729293
Basso et al. (2005) Antidepressant-like effect of D(2/3) receptor-, but not D(4) receptor-activation in the rat forced swim test. Neuropsychopharmacology. 30:1257
PMID: 15688083

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Inhibition of Synaptic Transmission in the VP

Name: Anonymous

Species: Mouse

Assay Type: In Vivo

L-745870 (100 nM)

PMID: 29949769

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