L-745,870 trihydrochloride
Chemical Name: 3-(4-[4-Chlorophenyl]piperazin-1-yl)-methyl-1H-pyrrolo[2,3-b]pyridine trihydrochloride
Purity: ≥99%
Biological Activity
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.Technical Data
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.
Additional Information
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Schizophrenia and L-745, 870 a novel DA D4 receptor antagonist.
Bristow et al.
TiPS, 1997;18:186 -
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.
Kulagowski et al.
J.Med.Chem., 1996;39:1941 -
Biological profile of L-745,870, a selective antagonist with high affinity for the DA D4 receptor.
Patel et al.
J.Pharmacol.Exp.Ther., 1997;283:636 -
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
Pillai et al.
Neuropharmacology, 1998;37:983
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Citations for L-745,870 trihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for L-745,870 trihydrochloride include:
13 Citations: Showing 1 - 10
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Epithelial phenotype restoring drugs suppress macular degeneration phenotypes in an iPSC model.
Authors: Sharma Et al.
Nat Commun 2021;12:7293
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Cocaine Inhibition of Synaptic Transmission in the Ventral Pallidum Is Pathway-Specific and Mediated by Serotonin.
Authors: Matsui and Alvarez
Cell Rep 2018;23(13):3852
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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.
Authors: Dai Et al.
J Neurodev Disord 2017;9:38
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DA D4 receptor activation restores CA1 LTP in hippocampal slices from aged mice.
Authors: Guo
Aging Cell 2017;16(6):1323
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Neurochemical arguments for the use of DA D4 receptor stimulation to improve cognitive impairment associated with schizophrenia.
Authors: Huang
Pharmacol Biochem Behav 2017;157:16
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Mechanisms underlying the endogenous DArgic inhibition of spinal locomotor circuit function in Xenopus tadpoles.
Authors: Picton Et al.
Scientific Reports 2016;6:35749
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Activation of D4 DA receptor decreases angiotensin II type 1 receptor expression in rat renal proximal tubule cells.
Authors: Chen Et al.
Autophagy 2015;65:153
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Effects of DA D2-Like Receptor Antagonists on Light Responses of Ganglion Cells in Wild-Type and P23H Rat Retinas.
Authors: Jensen
PLoS One 2015;10:e0146154
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Fast oscillatory activity in the anterior cingulate cortex: DArgic modulation and effect of perineuronal net loss.
Authors: Steullet Et al.
Front Cell Neurosci 2014;8:244
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DA D4 receptor counteracts morphine-induced changes in � opioid receptor signaling in the striosomes of the rat caudate putamen.
Authors: Suárez-Boomgaard Et al.
Int J Mol Sci 2014;15:1481
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D4 DA receptors modulate NR2B NMDA receptors and LTP in stratum oriens of hippocampal CA1.
Authors: Herwerth Et al.
Cereb Cortex 2012;22:1786
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Antidepressant-like effect of D(2/3) receptor-, but not D(4) receptor-activation in the rat forced swim test.
Authors: Basso Et al.
Neuropsychopharmacology 2005;30:1257
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A DA D4 receptor antagonist attenuates ischemia-induced neuronal cell damage via upregulation of neuronal apoptosis inhibitory protein.
Authors: Okada Et al.
Hypertension 2005;25:794
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