L-745,870 TRIHYDROCHLORIDE
L-745,870 TRIHYDROCHLORIDE Basic information
- Product Name:
- L-745,870 TRIHYDROCHLORIDE
- Synonyms:
-
- L-745,870 TRIHYDROCHLORIDE
- 3HCl
- 3-(4-[4-CHLOROPHENYL]PIPERAZIN-1-YL)-METHYL-1H-PYRROLO[2,3-B]PYRIDINE TRIHYDROCHLORIDE
- L 745870
- 3-[[4-(4-Chlorophenyl)-1-piperazinyl]methyl]-1H-pyrrolo[2,3-b]pyridine
- 1H-Pyrrolo[2,3-b]pyridine, 3-[[4-(4-chlorophenyl)-1-piperazinyl]methyl]-
- L-745,870 trihydroch
- L 745870,L745870
- CAS:
- 158985-00-3
- MF:
- C18H19ClN4
- MW:
- 326.82
- Mol File:
- 158985-00-3.mol
L-745,870 TRIHYDROCHLORIDE Chemical Properties
- Boiling point:
- 571.4±50.0 °C(Predicted)
- Density
- 1.31±0.1 g/cm3(Predicted)
- storage temp.
- Desiccate at +4°C
- solubility
- DMSO:16.5(Max Conc. mg/mL);50.49(Max Conc. mM)
- pka
- 8.20±0.20(Predicted)
- form
- Solid
- color
- White to off-white
- Water Solubility
- water: soluble
L-745,870 TRIHYDROCHLORIDE Usage And Synthesis
Uses
L-745,870 is a drug which acts as a dopamine receptor antagonist selective for the D4 subtype, and has antipsychotic effects in animal models, though it was not effective in human trials.
Definition
ChEBI: 3-[[4-(4-chlorophenyl)-1-piperazinyl]methyl]-1H-pyrrolo[2,3-b]pyridine is a member of piperazines.
Biological Activity
A highly potent and selective D 4 dopamine receptor antagonist; L-745,870 has K i values of 0.51, 2300 and 960 nM for D 4 , D 3 and D 2 subtypes respectively and > 1000-fold selectivity over 5-HT 2 , D 1 and D 5 receptors.
in vivo
L-745870 has good pharmacokinetic properties (20-60% oral bioavailability and plasma t1/2 2.1-2.8 hours) in both rat and monkey, and excellent brain penetration with high brain to plasma ratios in rat[2].
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[2].
IC 50
Human D4 Receptor: 4.3 nM (Ki); D2 Receptor: 960 nM (Ki); D3 Receptor: 2300 nM (Ki)
L-745,870 TRIHYDROCHLORIDESupplier
- Tel
- 821-50328103-801 18930552037
- 3bsc@sina.com
- Tel
- 400 638 7771
- sales@heowns.com
- Tel
- 021-58958002 18930822973
- sales@uhnshanghai.com
- Tel
- 888-539-0666
- info@emmx.com
- Tel
- 15076683720
- klq@cw-bio.com
L-745,870 TRIHYDROCHLORIDE(158985-00-3)Related Product Information
- hypochlorous acid
- 1-(2,9-diazabicyclo[4.3.0]nona-2,4,7,10-tetraen-7-yl)-N,N-dimethyl-methanamine
- 1-(4-Chlorophenyl)piperazine dihydrochloride
- 1H-Pyrrolo[2,3-b]pyridine, 3-(1-piperazinylmethyl)-
- 3-METHYL-7-AZAINDOLE
- 3-([4-(4-CHLOROPHENYL)PIPERAZIN-1-YL]METHYL)-1H-PYRROLO(2,3-B)PYRIDINE HYDROCHLORIDE
- 7-Azaindole
- L-745,870 TRIHYDROCHLORIDE