L-745,870 trihydrochloride

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Cat.No. 1002 - L-745,870 trihydrochloride | C18H19N4Cl.3HCl | CAS No. 866021-03-6
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)
Datasheet
Citations (12)
Reviews (1)
Literature (4)

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

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 Data

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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

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

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

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

Pillai et al (1998) 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 37 983 PMID: 9833627


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Keywords: L-745,870 trihydrochloride, L-745,870 trihydrochloride supplier, selective, D4, antagonists, Dopamine, Receptors, dopaminergic, L745870, 1002, Tocris Bioscience

12 Citations for L-745,870 trihydrochloride

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

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

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

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

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


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Reviews for L-745,870 trihydrochloride

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Inhibition of Synaptic Transmission in the VP.
By Anonymous on 02/02/2020
Assay Type: In Vivo
Species: Mouse

L-745870 (100 nM)

PMID: 29949769
review image

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