SB-271046 is a drug which is used in scientific research. It was one of the first selective
5-HT6receptorantagonists 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.[1] 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.[2]
^Minabe Y, Shirayama Y, Hashimoto K, Routledge C, Hagan JJ, Ashby CR (April 2004). "Effect of the acute and chronic administration of the selective 5-HT6 receptor antagonist SB-271046 on the activity of midbrain dopamine neurons in rats: an in vivo electrophysiological study". Synapse. 52 (1): 20–8.
doi:
10.1002/syn.20002.
PMID14755629.
S2CID25687099.
^de Foubert G, O'Neill MJ, Zetterström TS (July 2007). "Acute onset by 5-HT(6)-receptor activation on rat brain brain-derived neurotrophic factor and activity-regulated cytoskeletal-associated protein mRNA expression". Neuroscience. 147 (3): 778–85.
doi:
10.1016/j.neuroscience.2007.04.045.
PMID17560041.
S2CID37184427.
^Loiseau F, Dekeyne A, Millan MJ (January 2008). "Pro-cognitive effects of 5-HT6 receptor antagonists in the social recognition procedure in rats: implication of the frontal cortex". Psychopharmacology. 196 (1): 93–104.
doi:
10.1007/s00213-007-0934-5.
PMID17922111.
S2CID35795618.
SB-271046 is a drug which is used in scientific research. It was one of the first selective
5-HT6receptorantagonists 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.[1] 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.[2]
^Minabe Y, Shirayama Y, Hashimoto K, Routledge C, Hagan JJ, Ashby CR (April 2004). "Effect of the acute and chronic administration of the selective 5-HT6 receptor antagonist SB-271046 on the activity of midbrain dopamine neurons in rats: an in vivo electrophysiological study". Synapse. 52 (1): 20–8.
doi:
10.1002/syn.20002.
PMID14755629.
S2CID25687099.
^de Foubert G, O'Neill MJ, Zetterström TS (July 2007). "Acute onset by 5-HT(6)-receptor activation on rat brain brain-derived neurotrophic factor and activity-regulated cytoskeletal-associated protein mRNA expression". Neuroscience. 147 (3): 778–85.
doi:
10.1016/j.neuroscience.2007.04.045.
PMID17560041.
S2CID37184427.
^Loiseau F, Dekeyne A, Millan MJ (January 2008). "Pro-cognitive effects of 5-HT6 receptor antagonists in the social recognition procedure in rats: implication of the frontal cortex". Psychopharmacology. 196 (1): 93–104.
doi:
10.1007/s00213-007-0934-5.
PMID17922111.
S2CID35795618.