| Identification | Back Directory | [Name]
L-745,870 TRIHYDROCHLORIDE | [CAS]
158985-00-3 | [Synonyms]
3HCl
L 745870
L-745,870 TRIHYDROCHLORIDE
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]-
3-(4-[4-CHLOROPHENYL]PIPERAZIN-1-YL)-METHYL-1H-PYRROLO[2,3-B]PYRIDINE TRIHYDROCHLORIDE | [Molecular Formula]
C18H19ClN4 | [MDL Number]
MFCD01074795 | [MOL File]
158985-00-3.mol | [Molecular Weight]
326.82 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
8.20±0.20(Predicted) | [color ]
White to off-white | [Water Solubility ]
water: soluble | [InChI]
1S/C18H19ClN4/c19-15-3-5-16(6-4-15)23-10-8-22(9-11-23)13-14-12-21-18-17(14)2-1-7-20-18/h1-7,12H,8-11,13H2,(H,20,21) | [InChIKey]
OGJGQVFWEPNYSB-UHFFFAOYSA-N | [SMILES]
Clc1ccc(cc1)N2CCN(CC2)Cc3c4c([nH]c3)nccc4 |
| Hazard Information | Back Directory | [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) |
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cjbscvictory
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13348960310 |
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https://www.weikeqi-biotech.com/ |
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