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Submit ReviewL-745,870 trihydrochloride
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)
Biological Activity for L-745,870 trihydrochloride
L-745,870 trihydrochloride is 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 for L-745,870 trihydrochloride
| 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 for L-745,870 trihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 43.62 | 100 |
Preparing Stock Solutions for L-745,870 trihydrochloride
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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Product Datasheets for L-745,870 trihydrochloride
References for L-745,870 trihydrochloride
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
If you know of a relevant reference for L-745,870 trihydrochloride, please let us know.
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Keywords: L-745,870 trihydrochloride, L-745,870 trihydrochloride supplier, selective, D4, antagonists, Dopamine, Receptors, dopaminergic, L745870, 1002, Tocris Bioscience
13 Citations for L-745,870 trihydrochloride
Citations are publications that use Tocris 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
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 1323 PMID: 28975698
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
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
Matsui and Alvarez (2018) Cocaine Inhibition of Synaptic Transmission in the Ventral Pallidum Is Pathway-Specific and Mediated by Serotonin. Cell Rep 23 3852 PMID: 29949769
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
Suárez-Boomgaard et al (2014) DA 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: DArgic modulation and effect of perineuronal net loss. Front Cell Neurosci 8 244 PMID: 25191228
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
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
Do you know of a great paper that uses L-745,870 trihydrochloride from Tocris? Please let us know.
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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)
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