| Identification | Back Directory | [Name]
5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methylbenzo[b]thiophene-2-sulfonamide hydrochloride | [CAS]
209481-24-3 | [Synonyms]
SB 271046A
SB 271046A; SB-271046A
SB-271046A >=98% (HPLC)
4-[(3-chloro-1,4-dioxonaphthalen-2-yl)amino]benzenesulfonamide
5-Chloro-N-(4-methoxy-3-piperazin-1-yl-phenyl)-3-methyl-2-benzo-thiophenesulfonamide hydrochloride
5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methylbenzo[b]thiophene-2-sulfonamide hydrochloride
Benzo[b]thiophene-2-sulfonaMide, 5-chloro-N-[4-Methoxy-3-(1-piperazinyl)phenyl]-3-Methyl-, Monohydrochloride | [Molecular Formula]
C20H22ClN3O3S2.HCl | [MDL Number]
MFCD10565914 | [MOL File]
209481-24-3.mol | [Molecular Weight]
488.451 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
DMSO: >20mg/mL | [form ]
powder | [color ]
White to light brown | [InChI]
1S/C20H22ClN3O3S2.ClH/c1-13-16-11-14(21)3-6-19(16)28-20(13)29(25,26)23-15-4-5-18(27-2)17(12-15)24-9-7-22-8-10-24;/h3-6,11-12,22-23H,7-10H2,1-2H3;1H | [InChIKey]
RMXZRJYGJMSDQK-UHFFFAOYSA-N | [SMILES]
Cl.COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N4CCNCC4 |
| Hazard Information | Back Directory | [Uses]
5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-benzo[b]thiophene-2-sulfonamide Hydrochloride is a 5-Hydroxytryptamine6 receptor antagonist. | [Biological Activity]
The first potent and selective 5-HT6 antagonist. Training in cognitive tasksas well as administration SB-271046induces an increase in pERK1/2 and pCREB1 levelswhile CREB2 levels are significantly reduced; cognition-enhancing properties of SB-271046 are attributed to the effect on pERK1/2not pCREB1/2. SB-271046 reverses MK-801-inducedbut not scopolamine-inducedlearning impairments. Howeverwith coadministration of galanthamineboth types of learning impairments were ameliorated. | [in vivo]
SB 271046 Hydrochloride (10?mg/kg; p.o.) produces an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of ?0.1?mg/kg p.o. and maximum effect at 4?h post-dose[1]. | Animal Model: | Male Sprague Dawley rats[1] | | Dosage: | 10?mg/kg | | Administration: | P.o. | | Result: | Produced an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of ?0.1?mg?kg?1 p.o. and maximum effect at 4?h post-dose. The level of anticonvulsant activity achieved correlated well with the blood concentrations of SB-271046 (EC50 of 0.16?μM) and brain concentrations of 0.01-0.04?μM at Cmax.
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| [IC 50]
5-HT6 Receptor: 8.92-9.02 (pKi); 5-HT1D Receptor: 6.55 (pKi); 5-HT1A Receptor: 6.35 (pKi); 5-HT1B Receptor: 6.05 (pKi); 5-HT1F Receptor: 5.95 (pKi); 5-HT2A Receptor: 5.62 (pKi); 5-HT2B Receptor: 5.41 (pKi); 5-HT7 Receptor: 5.39 (pKi); 5-HT4 Receptor: 5.27 (pKi); 5-HT1E Receptor: <4.99 (pKi); Human 5-HT2C Receptor: 5.73 (pKi) | [storage]
Desiccate at RT |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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