| Identification | Back Directory | [Name]
L-745,870 trihydrochloride | [CAS]
866021-03-6 | [Synonyms]
L-745
870 trihydrochloride
brain-penetrant,orally,α-adrenoceptors,Antipsychotic,Inhibitor,Dopamine Receptor,L-745870 trihydrochloride,D4-receptor,5-HT2,inhibit,L745870 trihydrochloride,L 745870 trihydrochloride | [Molecular Formula]
C18H20Cl2N4 | [MDL Number]
MFCD01074795 | [MOL File]
866021-03-6.mol | [Molecular Weight]
363.29 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 30 mg/ml
DMSO: 30 mg/ml
Ethanol: 5 mg/mlPBS (pH 7.2): 10 mg/ml | [form ]
Powder | [Water Solubility ]
Soluble to 100 mM in water |
| 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. | [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[1].
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]. | [IC 50]
Human D4 Receptor: 4.3 nM (Ki); D2 Receptor: 960 nM (Ki); D3 Receptor: 2300 nM (Ki) | [storage]
Desiccate at +4°C | [References]
[1] S PATEL. Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor.[J]. Journal of Pharmacology and Experimental Therapeutics, 1997, 283 2: 636-647.
[2] PHILIPPE HUOT. L-745,870 reduces L-DOPA-induced dyskinesia in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-lesioned macaque model of Parkinson’s disease.[J]. Journal of Pharmacology and Experimental Therapeutics, 2012, 342 2: 576-585. DOI: 10.1124/jpet.112.195693 |
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| Company Name: |
Energy Chemical
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021-58432009 400-005-6266 |
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http://www.energy-chemical.com |
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