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
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
N-Bromosuccinimide Price
- Product number
- L009800
- Product name
- L-745,870Trihydrochloride
- Packaging
- 50mg
- Price
- $160
- Updated
- 2021/12/16
- Product number
- B5043
- Product name
- L-745,870trihydrochloride
- Packaging
- 10mg
- Price
- $219
- Updated
- 2021/12/16
- Product number
- INB0004659
- Product name
- L-745,870 TRIHYDROCHLORIDE
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $498.49
- Updated
- 2021/12/16
- Product number
- B5043
- Product name
- L-745,870trihydrochloride
- Packaging
- 50mg
- Price
- $921
- Updated
- 2021/12/16
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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