| dbo:abstract | - La SB-271046 es un fármaco que se utiliza en investigación científica. Fue uno de los primeros receptores antagonistas 5-HT6 selectivos en ser descubiertos a través de del Banco de Compuestos de SmithKline Beecham utilizando receptores 5-HT6 clonados como objetivo, con un compuesto inicial desarrollado en SB-271046 a través de un estudio relación estructura-actividad (SAR de sus siglas en inglés). Se encontró que la SB-271046 es un in vitro potente y selectivo, teniendo una buena biodisponibilidad oral in vivo, pero pobre penetración de la barrera hematoencefálica; así, posteriores trabajos SAR han sido realizados, permitiendo mejorar los antagonistas 5-HT6 tales como SB-357134 y SB-399885. (es)
- SB-271046 is a drug which is used in scientific research. It was one of the first selective 5-HT6 receptor antagonists to be discovered, and was found through high-throughput screening of the SmithKline Beecham Compound Bank using cloned 5-HT6 receptors as a target, with an initial lead compound being developed into SB-271046 through a structure-activity relationship (SAR) study. SB-271046 was found to be potent and selective in vitro and had good oral bioavailability in vivo, but had poor penetration across the blood–brain barrier, so further SAR work was then conducted, which led to improved 5-HT6 antagonists such as SB-357,134 and SB-399,885. SB-271046 was found to increase levels of the excitatory amino acid neurotransmitters glutamate and aspartate, as well as dopamine and noradrenaline in the frontal cortex and hippocampus of rats, and 5-HT6 antagonists have been shown to produce nootropic effects in a variety of animal studies. Suggested applications of these drugs include treatment of schizophrenia and other psychiatric disorders. (en)
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| rdfs:comment | - La SB-271046 es un fármaco que se utiliza en investigación científica. Fue uno de los primeros receptores antagonistas 5-HT6 selectivos en ser descubiertos a través de del Banco de Compuestos de SmithKline Beecham utilizando receptores 5-HT6 clonados como objetivo, con un compuesto inicial desarrollado en SB-271046 a través de un estudio relación estructura-actividad (SAR de sus siglas en inglés). (es)
- SB-271046 is a drug which is used in scientific research. It was one of the first selective 5-HT6 receptor antagonists to be discovered, and was found through high-throughput screening of the SmithKline Beecham Compound Bank using cloned 5-HT6 receptors as a target, with an initial lead compound being developed into SB-271046 through a structure-activity relationship (SAR) study. SB-271046 was found to be potent and selective in vitro and had good oral bioavailability in vivo, but had poor penetration across the blood–brain barrier, so further SAR work was then conducted, which led to improved 5-HT6 antagonists such as SB-357,134 and SB-399,885. (en)
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| rdfs:label | - SB-271046 (es)
- SB-271046 (en)
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