Catalog Number: 1002
Chemical Name: 3-(4-[4-Chlorophenyl]piperazin-1-yl)-methyl-1H-pyrrolo[2,3-b]pyridine trihydrochloride
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.
Technical Data
  • M.Wt:
    436.21
  • Formula:
    C18H19N4Cl.3HCl
  • Solubility:
    Soluble to 100 mM in water
  • Purity:
    >99%
  • Storage:
    Desiccate at +4°C
  • CAS No:
    866021-03-6
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.
Additional Information
Licensing Caveats:
Sold with the permission of Merck Sharp and Dohme Ltd.
Background References
  1. Schizophrenia and L-745, 870 a novel dopamine D4 receptor antagonist.
    Bristow et al.
    TiPS, 1997;18:186
  2. 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
  3. Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor.
    Patel et al.
    J.Pharmacol.Exp.Ther., 1997;283:636
  4. 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
    Pillai et al.
    Neuropharmacology, 1998;37:983
Citations:

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

8 Citations: Showing 1 - 8
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  1. Dopamine D4 receptor activation restores CA1 LTP in hippocampal slices from aged mice.
    Authors: Guo
    Aging Cell 2017;16(6):1323
  2. Neurochemical arguments for the use of dopamine D4 receptor stimulation to improve cognitive impairment associated with schizophrenia.
    Authors: Huang
    Pharmacol Biochem Behav 2017;157:16
  3. Mechanisms underlying the endogenous dopaminergic inhibition of spinal locomotor circuit function in Xenopus tadpoles.
    Authors: Picton Et al.
    Scientific Reports 2016;6:35749
  4. Activation of D4 dopamine receptor decreases angiotensin II type 1 receptor expression in rat renal proximal tubule cells.
    Authors: Chen Et al.
    Autophagy 2015;65:153
  5. Effects of Dopamine D2-Like Receptor Antagonists on Light Responses of Ganglion Cells in Wild-Type and P23H Rat Retinas.
    Authors: Jensen
    PLoS One 2015;10:e0146154
  6. Fast oscillatory activity in the anterior cingulate cortex: dopaminergic modulation and effect of perineuronal net loss.
    Authors: Steullet Et al.
    Front Cell Neurosci 2014;8:244
  7. Dopamine 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
  8. A dopamine 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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