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 (7)
Literature

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
physiological saline 21.81 50mM with gentle warming
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 solvent 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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Safety Datasheet

References

References are publications that support the products' biological activity.

Bristow et al (1997) Schizophrenia and L-745, 870 a novel dopamine 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 dopamine D4 receptor. J.Pharmacol.Exp.Ther. 283 636 PMID: 9353380

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 r Neuropharmacology 37 983 PMID: 9833627


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

7 Citations for L-745,870 trihydrochloride

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

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

Huang (2017) Neurochemical arguments for the use of dopamine D4 receptor stimulation to improve cognitive impairment associated with schizophrenia. Pharmacol Biochem Behav 157 16 PMID: 28455127

Picton et al (2016) Mechanisms underlying the endogenous dopaminergic inhibition of spinal locomotor circuit function in Xenopus tadpoles. Scientific Reports 6 35749 PMID: 27760989

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

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

Suárez-Boomgaard et al (2014) Dopamine D4 receptor counteracts morphine-induced changes in µ 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: dopaminergic modulation and effect of perineuronal net loss. Front Cell Neurosci 8 244 PMID: 25191228


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

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