607742-69-8
607742-69-8 structure
- Name: SB742457
- Chemical Name: 3-(benzenesulfonyl)-8-piperazin-1-ylquinoline
- CAS Number: 607742-69-8
- Molecular Formula: C19H19N3O2S
- Molecular Weight: 353.438
- Catalog: Biochemical Inhibitor Neuronal Signaling 5-HT Receptor Antagonist
- Create Date: 2018-08-03 18:29:20
- Modify Date: 2024-01-02 20:51:05
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SB742457 is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors.IC50 Value: 9.63 (pKi)Target: 5-HT6 ReceptorSB-742457, a 5-HT6 receptor antagonist, which extends into Alzheimer disease (AD) sufferers further highlights the therapeutic promise of this mechanistic approach. Alzheimer's disease is a devastating neurological condition characterized by a progressive decline in cognitive performance accompanied by behavioral and psychological syndromes, such as depression and psychosis. With the subsequent development of selective 5-HT6 receptor antagonists, preclinical studies in rodents and primates have elucidated the function of this receptor subtype in more detail. It is increasingly clear that blockade of 5-HT6 receptors leads to an improvement of cognitive performance in a wide variety of learning and memory paradigms and also results in anxiolytic and antidepressant-like activity. SB-742457 is generally safe and well tolerated and may be efficacious in Alzheimer disease.
| Name | 3-(benzenesulfonyl)-8-piperazin-1-ylquinoline |
|---|---|
| Synonyms |
SB-742,457
Quinoline,3-(phenylsulfonyl)-8-(1-piperazinyl) RVT-101 GSK-742457 3-(phenylsulfonyl)-8-(piperazin-1-yl)quinoline Intepirdine Quinoline, 3-(phenylsulfonyl)-8-(1-piperazinyl)- UNII-2IOB2M82HY SB-742457 3-(Phenylsulfonyl)-8-(1-piperazinyl)quinoline SB742457 |
| Description | SB742457 is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors.IC50 Value: 9.63 (pKi)Target: 5-HT6 ReceptorSB-742457, a 5-HT6 receptor antagonist, which extends into Alzheimer disease (AD) sufferers further highlights the therapeutic promise of this mechanistic approach. Alzheimer's disease is a devastating neurological condition characterized by a progressive decline in cognitive performance accompanied by behavioral and psychological syndromes, such as depression and psychosis. With the subsequent development of selective 5-HT6 receptor antagonists, preclinical studies in rodents and primates have elucidated the function of this receptor subtype in more detail. It is increasingly clear that blockade of 5-HT6 receptors leads to an improvement of cognitive performance in a wide variety of learning and memory paradigms and also results in anxiolytic and antidepressant-like activity. SB-742457 is generally safe and well tolerated and may be efficacious in Alzheimer disease. |
|---|---|
| Related Catalog | |
| References |
[6]. SB-742457 |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 608.3±45.0 °C at 760 mmHg |
| Molecular Formula | C19H19N3O2S |
| Molecular Weight | 353.438 |
| Flash Point | 321.7±28.7 °C |
| Exact Mass | 353.119812 |
| PSA | 70.68000 |
| LogP | 2.10 |
| Vapour Pressure | 0.0±1.7 mmHg at 25°C |
| Index of Refraction | 1.649 |
| Storage condition | -20℃ |
|
~73%
607742-69-8 |
| Literature: GLAXO GROUP LIMITED Patent: WO2005/26125 A1, 2005 ; Location in patent: Page/Page column 21-22 ; WO 2005/026125 A1 |
|
~84%
607742-69-8 |
| Literature: GLAXO GROUP LIMITED Patent: WO2007/39238 A1, 2007 ; Location in patent: Page/Page column 14-16 ; |
|
~69%
607742-69-8 |
| Literature: Emmett, Edward J.; Hayter, Barry R.; Willis, Michael C. Angewandte Chemie - International Edition, 2013 , vol. 52, # 48 p. 12679 - 12683 Angew. Chem., 2013 , vol. 125, # 48 p. 12911 - 12915,5 |
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~%
607742-69-8 |
| Literature: Journal of Medicinal Chemistry, , vol. 57, # 9 p. 3884 - 3890 |
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~%
607742-69-8 |
| Literature: Journal of Medicinal Chemistry, , vol. 57, # 9 p. 3884 - 3890 |
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~%
607742-69-8 |
| Literature: Journal of Medicinal Chemistry, , vol. 57, # 9 p. 3884 - 3890 |
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~%
607742-69-8 |
| Literature: Journal of Medicinal Chemistry, , vol. 57, # 9 p. 3884 - 3890 |
