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.
Licensing Information
Sold with the permission of Merck Sharp and Dohme Ltd.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| physiological saline | 21.81 | 50mM with gentle warming | |
| water | 43.62 | 100 |
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 |
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Product Datasheets
References
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
Keywords: L-745,870 trihydrochloride, supplier, selective, D4, antagonists, Dopamine, Receptors, dopaminergic, L745870, D4, Receptors, D4, Receptors, Tocris Bioscience
