| Identification | Back Directory | [Name]
3-([4-(4-CHLOROPHENYL)PIPERAZIN-1-YL]METHYL)-1H-PYRROLO(2,3-B)PYRIDINE HYDROCHLORIDE | [CAS]
1173023-36-3 | [Synonyms]
L-745,870 HYDROCHLORIDE
3-([4-(4-CHLOROPHENYL)PIPERAZIN-1-YL]METHYL)-1H-PYRROLO(2,3-B)PYRIDINE HYDROCHLORIDE
L745870,dopamine,L 745870,inhibit,penetration,receptor,Human,brain,Inhibitor,neuroleptics,L-745870,Dopamine Receptor,L 745870 hydrochloride,L745870 hydrochloride | [Molecular Formula]
C18H20Cl2N4 | [MDL Number]
MFCD01529971 | [MOL File]
1173023-36-3.mol | [Molecular Weight]
363.28 |
| Chemical Properties | Back Directory | [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 | [InChI]
1S/C18H19ClN4.ClH/c19-15-3-5-16(6-4-15)23-10-8-22(9-11-23)13-14-12-21-18-17(14)2-1-7-20-18;/h1-7,12H,8-11,13H2,(H,20,21);1H | [InChIKey]
GFFJYISJZJIKAF-UHFFFAOYSA-N | [SMILES]
Cl.Clc1ccc(cc1)N2CCN(CC2)Cc3c[nH]c4ncccc34 |
| Hazard Information | Back Directory | [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) | [storage]
Store at -20°C | [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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