ChemicalBook > CAS DataBase List > L-745,870 trihydrochloride

L-745,870 trihydrochloride

Product Name
L-745,870 trihydrochloride
CAS No.
866021-03-6
Chemical Name
L-745,870 trihydrochloride
Synonyms
L-745;870 trihydrochloride;L-745870 trihydrochloride, brain penetrant D4 antagonist;brain-penetrant,orally,α-adrenoceptors,Antipsychotic,Inhibitor,Dopamine Receptor,L-745870 trihydrochloride,D4-receptor,5-HT2,inhibit,L745870 trihydrochloride,L 745870 trihydrochloride
CBNumber
CB83167502
Molecular Formula
C18H20Cl2N4
Formula Weight
363.29
MOL File
866021-03-6.mol
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L-745,870 trihydrochloride Property

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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

TRC
Product number
L009800
Product name
L-745,870Trihydrochloride
Packaging
50mg
Price
$160
Updated
2021/12/16
ApexBio Technology
Product number
B5043
Product name
L-745,870trihydrochloride
Packaging
10mg
Price
$219
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
INB0004659
Product name
L-745,870 TRIHYDROCHLORIDE
Purity
95.00%
Packaging
5MG
Price
$498.49
Updated
2021/12/16
ApexBio Technology
Product number
B5043
Product name
L-745,870trihydrochloride
Packaging
50mg
Price
$921
Updated
2021/12/16
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L-745,870 trihydrochloride Chemical Properties,Usage,Production

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

L-745,870 trihydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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L-745,870 trihydrochloride Suppliers

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Shanghai YuanYe Biotechnology Co., Ltd.
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866021-03-6, L-745,870 trihydrochlorideRelated Search:


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  • L-745870 trihydrochloride, brain penetrant D4 antagonist
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