L-745,870 trihydrochloride

Product NameL-745,870 trihydrochloride
CAS866021-03-6
MFC18H20Cl2N4
MW363.29
EINECS
MOL File866021-03-6.mol

Chemical Properties

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

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.

in vivo

L-745870 has good pharmacokinetic properties (20-60% oral bioavailability and plasma t_1/2 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