3-([4-(4-CHLOROPHENYL)PIPERAZIN-1-YL]METHYL)-1H-PYRROLO(2,3-B)PYRIDINE HYDROCHLORIDE
3-([4-(4-CHLOROPHENYL)PIPERAZIN-1-YL]METHYL)-1H-PYRROLO(2,3-B)PYRIDINE HYDROCHLORIDE Basic information
- Product Name:
- 3-([4-(4-CHLOROPHENYL)PIPERAZIN-1-YL]METHYL)-1H-PYRROLO(2,3-B)PYRIDINE HYDROCHLORIDE
- Synonyms:
-
- 3-([4-(4-CHLOROPHENYL)PIPERAZIN-1-YL]METHYL)-1H-PYRROLO(2,3-B)PYRIDINE HYDROCHLORIDE
- L-745,870 HYDROCHLORIDE
- L745870,dopamine,L 745870,inhibit,penetration,receptor,Human,brain,Inhibitor,neuroleptics,L-745870,Dopamine Receptor,L 745870 hydrochloride,L745870 hydrochloride
- L-745870 hydrochloride, 10 mM in DMSO
- CAS:
- 1173023-36-3
- MF:
- C18H20Cl2N4
- MW:
- 363.28
- Mol File:
- Mol File
3-([4-(4-CHLOROPHENYL)PIPERAZIN-1-YL]METHYL)-1H-PYRROLO(2,3-B)PYRIDINE HYDROCHLORIDE Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- H2O: 0.2 mg/mL
- form
- solid
- color
- white
- Water Solubility
- H2O: 0.2mg/mL
ethanol: 1.4mg/mL
0.1 M HCl: 5.5mg/mL
MSDS
- Language:English Provider:SigmaAldrich
3-([4-(4-CHLOROPHENYL)PIPERAZIN-1-YL]METHYL)-1H-PYRROLO(2,3-B)PYRIDINE HYDROCHLORIDE Usage And Synthesis
Uses
L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors[1][2][3].
Biological Activity
Selective D4 dopamine receptor antagonist.
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 mM (Ki)
References
[1] Bristow LJ, et al. Schizophrenia and L-745,870, a novel dopamine D4 receptor antagonist. Trends Pharmacol Sci. 1997 Jun;18(6):186-8. DOI:10.1016/s0165-6147(97)01066-3
[2] Patel S, et al. Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor. J Pharmacol Exp Ther. 1997 Nov;283(2):636-47. PMID:9353380
[3] Kulagowski JJ, et al. 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. J Med Chem. 1996 May 10;39(10):1941-2. DOI:10.1021/jm9600712
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