5-Chloro-3-Methyl-Benzo[b]Thiophene-2-Carboxylic Acid (4-Methoxy-3-Piperazin-1-yl-Phenyl)-AMide H
SB271046
CAS: 209481-20-9
Molecular Formula: C20H22ClN3O3S2
5-Chloro-3-Methyl-Benzo[b]Thiophene-2-Carboxylic Acid (4-Methoxy-3-Piperazin-1-yl-Phenyl)-AMide H - Names and Identifiers
5-Chloro-3-Methyl-Benzo[b]Thiophene-2-Carboxylic Acid (4-Methoxy-3-Piperazin-1-yl-Phenyl)-AMide H - Physico-chemical Properties
| Molecular Formula | C20H22ClN3O3S2 |
| Molar Mass | 451.99 |
| Density | 1.400 |
| Melting Point | 240-241℃ (DEC.) |
| Boling Point | 664.3±65.0 °C(Predicted) |
| pKa | 7.61±0.50(Predicted) |
| Storage Condition | Desiccate at RT |
| In vitro study | SB-271046 effectively substituted [125I]-SB-258585 with pKi 9.02, 8.55 and 8.81 for rat and pig striatum and human tail shell membranes, respectively. SB-271046 competitive antagonism of 5-HT induced adenylate cyclase activity stimulation, pA2 was 8.71. In the functional adenylate cyclase assay, SB-271046 was a competitive antagonist, and pA2 was 8.7, which is consistent with its better binding affinity. SB-271046 had no significant inhibitory activity against most human P450 enzymes. |
| In vivo study | In the maximum electroconvulsive seizure threshold (MEST) test in rats, the minimum effective oral dose of 0.1 mg/kg was increased over a wide range of doses SB-271046, and after 4 hours, the maximum effect is achieved. Levels of anticonvulsant activity there was a good correlation between plasma concentrations at SB-271046 (EC50 of 0.16 μm) and brain concentrations at Cmax of 0.01 μM-0.04 μm. SB-271046 treated rats, were moderate brain osmotic agents (10%), had low blood clearance (7.7/min/kg), good half-life (4.8 hours), excellent oral bioavailability (>80%). SB-271046 treatment of rat frontal cortex and dorsal hippocampus increased extracellular glutamate levels by 3-fold and 2-fold, respectively, indicating that it can be used to treat cognitive and memory dysfunction. SB-271046 Wistar rats were orally fed at a dose of 20 mg/kg for 30 minutes, and then trained. After 6 hours of training, it was found that the Scopolamine(0.8 mg/kg, intraperitoneal injection) was significantly reversed. Memory loss due to treatment. SB-271046 at a dose of 10 mg/kg subcutaneous injection) in the frontal cortex of rats, significantly increased the extracellular levels of glutamic acid and aspartic acid, this effect is Tetrodotoxin dependent, reaching a maximum, 375.4% and 215.3%, respectively, before injection. |
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Product Name: SB271046 Visit Supplier Webpage Request for quotation
CAS: 209481-20-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 209481-20-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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