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3-([4-(4-Chlorophenyl)piperazin-1-yl]methyl)-1H-pyrrolo(2,3-b)pyridine hydrochloride manufacturers
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| | 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: | 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;3-((4-(4-chlorophenyl)azine-1-yl)methyl)-1H-pyridinebenzo[2,3-b]pyridinehydrochloride;3-([4-(4-Chlorophenyl)piperazin-1-yl]methyl)-1H-pyrrolo(2,3-b)pyridine hydrochloride | | CAS: | 1173023-36-3 | | MF: | C18H20Cl2N4 | | MW: | 363.28 | | EINECS: | | | Product Categories: | | | Mol File: | Mol File | ![3-([4-(4-Chlorophenyl)piperazin-1-yl]methyl)-1H-pyrrolo(2,3-b)pyridine hydrochloride Structure](StructureFile/ChemBookStructure4/GIF/CB3387546.gif) |
| | 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 | | 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 |
| WGK Germany | 3 | | Storage Class | 11 - Combustible Solids |
| | 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 |
| | 3-([4-(4-Chlorophenyl)piperazin-1-yl]methyl)-1H-pyrrolo(2,3-b)pyridine hydrochloride Preparation Products And Raw materials |
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