L-745870 hydrochloride
Based on 3 publication(s) in Google Scholar
L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 1173023-36-3
- Formula: C18H20Cl2N4
- Molecular Weight:363.28
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) L-745870 hydrochloride
MoreAll Dopamine Receptor Isoforms
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Biological Activity
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Human D4 Receptor 4.3 nM (Ki) |
D2 Receptor 960 nM (Ki) |
D3 Receptor 2300 mM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
80 nM
Compound: L-745870
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Binding affinity to cloned human Dopamine receptor D3 expressed in CHO cells by [3H]spiperone displacement.
Binding affinity to cloned human Dopamine receptor D3 expressed in CHO cells by [3H]spiperone displacement.
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[PMID: 9873481] |
L-745870 is capable of antagonizing the ability of D4 receptors to inhibit agonist-induced stimulation of [35S]-GTPgS binding; blocking the inhibition of forskolin-stimulated adenylate cyclase activity in transfected human embryonic kidney (HEK293) and Chinese hamster ovary (CHO) cells; blocking dopamine-induced inhibition of Ca2+ currents in transfected GH4C1 pituitary cells; inhibiting D4 activation of cloned G protein-coupled inwardly rectifying K+ channels; and antagonizing dopamine-induced stimulation of extracellular acidification in transfected cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Following oral administration to squirrel monkeys, L745870 (10 mg/kg p.o.) induces mild sedation and extrapyramidal motor symptoms, notably bradykinesia, became apparent at 30 mg/kg. Lower doses of L-745870 has no observable behavioural effects in monkeys[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1173023-36-3
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Appearance Solid
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Molecular Weight 363.28
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Formula C18H20Cl2N4
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Color Light yellow to yellow
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SMILES
[H]Cl.ClC(C=C1)=CC=C1N(CC2)CCN2CC3=CNC4=NC=CC=C43
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Br J Cancer
DRD4 promotes chemo-resistance and cancer stem cell-like phenotypes by mediating the activation of the Akt/β-catenin signaling axis in liver cancer. [Abstract]2024 Oct;131(7):1212-1223. PMID: 39174739 -
Psychopharmacology (Berl)
Contrasting effects of DOI and lisuride on impulsive decision-making in delay discounting task. [Abstract]2022 Nov;239(11):3551-3565. PMID: 36107207 -
Solvent & Solubility
H2O : ≥ 100 mg/mL (275.27 mM)
DMSO : 32.26 mg/mL (88.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
0.1 M HCl : 25 mg/mL (68.82 mM; ultrasonic and adjust pH to 3 with HCl)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Bristow LJ, et al. Schizophrenia and L-745,870, a novel dopamine D4 receptor antagonist. Trends Pharmacol Sci. 1997 Jun;18(6):186-8. [Content Brief]
[2]. Patel S, et al. Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor. J Pharmacol Exp Ther. 1997 Nov;283(2):636-47. [Content Brief]
[3]. Kulagowski JJ, et al. 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. J Med Chem. 1996 May 10;39(10):1941-2. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| 0.1 M HCl / DMSO / H2O | 1 mM | 2.7527 mL | 13.7635 mL | 27.5270 mL | 68.8174 mL |
| 5 mM | 0.5505 mL | 2.7527 mL | 5.5054 mL | 13.7635 mL | |
| 10 mM | 0.2753 mL | 1.3763 mL | 2.7527 mL | 6.8817 mL | |
| 15 mM | 0.1835 mL | 0.9176 mL | 1.8351 mL | 4.5878 mL | |
| 20 mM | 0.1376 mL | 0.6882 mL | 1.3763 mL | 3.4409 mL | |
| 25 mM | 0.1101 mL | 0.5505 mL | 1.1011 mL | 2.7527 mL | |
| 30 mM | 0.0918 mL | 0.4588 mL | 0.9176 mL | 2.2939 mL | |
| 40 mM | 0.0688 mL | 0.3441 mL | 0.6882 mL | 1.7204 mL | |
| 50 mM | 0.0551 mL | 0.2753 mL | 0.5505 mL | 1.3763 mL | |
| 60 mM | 0.0459 mL | 0.2294 mL | 0.4588 mL | 1.1470 mL | |
| DMSO / H2O | 80 mM | 0.0344 mL | 0.1720 mL | 0.3441 mL | 0.8602 mL |
| H2O | 100 mM | 0.0275 mL | 0.1376 mL | 0.2753 mL | 0.6882 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
L-745870 hydrochloride Related Classifications
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