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.
Sold with the permission of Merck Sharp and Dohme Ltd.
|Storage||Desiccate at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|physiological saline||21.81||50mM with gentle warming|
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.
|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|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
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
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, 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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