SB742457 - CAS 607742-69-8
Catalog number: B0084-404961
Category: Inhibitor
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5-HT Receptor
SB742457 is a selective 5-HT6 receptor antagonist with potential cognition, memory, and learning-enhancing effects.It was under development by GlaxoSmithKline for the treatment of Alzheimer's disease.
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B0084-404961 50 mg $239 In stock
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SB742457; SB 742457; SB-742457; RVT-101; RVT 101; RVT101. intepirdine. GSK 742457; GSK742457; GSK-742457
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1.Effect of sertindole on extracellular dopamine, acetylcholine, and glutamate in the medial prefrontal cortex of conscious rats: a comparison with risperidone and exploration of mechanisms involved.
Mørk A;Witten LM;Arnt J Psychopharmacology (Berl). 2009 Sep;206(1):39-49. doi: 10.1007/s00213-009-1578-4. Epub 2009 Jun 9.
RATIONALE: ;Second-generation antipsychotics have some beneficial effect on cognition. Recent studies, furthermore, indicate differential effects of second-generation antipsychotics on impairment in executive cognitive function.;OBJECTIVE: ;We evaluated the effect of the second-generation antipsychotic drug, sertindole, on extracellular levels of dopamine (DA), acetylcholine (ACh), and glutamate (Glu) in the rat medial prefrontal cortex (mPFC). Risperidone was studied for comparison. Moreover, selective serotonin 5-HT(2A), 5-HT(2C), and 5-HT(6) receptor antagonists were used, given alone and in combination with the preferential DA D(2) receptor antagonist, haloperidol, to further clarify the action of the two drugs.;MATERIALS AND METHODS: ;Rats were treated acutely with vehicle or drugs, and extracellular levels of neurotransmitters were assessed by microdialysis in freely moving animals.;RESULTS: ;Sertindole and risperidone significantly increased extracellular levels of DA. Haloperidol; the 5-HT(2A) receptor antagonist, M100907; the 5-HT(2C) receptor antagonist, SB242084; and the 5-HT(6) receptor antagonist, GSK-742457, induced minor increases in levels of DA, but the three latter compounds raised the DA levels notably in combination with haloperidol.
2.The 5-HT₂C receptor agonist, lorcaserin, and the 5-HT₆ receptor antagonist, SB-742457, promote satiety; a microstructural analysis of feeding behaviour.
Higgs S;Cooper AJ;Barnes NM Psychopharmacology (Berl). 2016 Feb;233(3):417-24. doi: 10.1007/s00213-015-4112-x. Epub 2015 Oct 28.
RATIONALE: ;Whilst the FDA-approved anorectic, lorcaserin and various 5-hydroxytryptamine (5-HT)6 receptor antagonists reduce feeding, a direct assessment of their impact upon feeding behaviour is less clear. We therefore examined the action of lorcaserin and the clinical-stage developmental candidate 5-HT6 receptor antagonist, SB-742457, upon microstructural analysis of licking behaviour. Such analysis provides a rich source of information about the mechanisms controlling food intake.;OBJECTIVES: ;The objective of the present study was to gain insight into the influence upon feeding behaviour of the 5-HT2C receptor agonist, lorcaserin and the developmental 5-HT6 receptor antagonist, SB-742457.;METHODS: ;The impact of lorcaserin and SB-742457 upon licking behaviour of non-deprived rats for a glucose solution was assessed using microstructural analysis.;RESULTS: ;Lorcaserin (0.1-3.0 mg/kg) displayed a dose-dependent ability to reduce glucose consumption via reduction in the number of bouts of licking. A similar action was evident with SB-742457, but only at the lowest dose tested (3.0 mg/kg).;CONCLUSIONS: ;The behavioural actions of both lorcaserin and SB-742457 demonstrate they directly promote satiety.
3.Characterization of [³H]Lu AE60157 ([³H]8-(4-methylpiperazin-1-yl)-3-phenylsulfonylquinoline) binding to 5-hydroxytryptamine₆ (5-HT₆) receptors in vivo.
Witten L;Bang-Andersen B;Nielsen SM;Miller S;Christoffersen CT;Stensbøl TB;Brennum LT;Arnt J Eur J Pharmacol. 2012 Feb 15;676(1-3):6-11. doi: 10.1016/j.ejphar.2011.11.029. Epub 2011 Dec 4.
The serotonin6 (5-HT(6)) receptor has received attention for its proposed role in cognitive impairments associated with schizophrenia and Alzheimer's disease. This has lead to a search for selective 5-HT(6) receptor ligands useful for in vivo imaging in animals and humans. The novel 5-HT(6) receptor antagonist Lu AE60157 (8-(4-methylpiperazin-1-yl)-3-phenylsulfonylquinoline) displays high affinity for the human (h) 5-HT(6) receptor (K(d) 0.2nM), and broad profiling in 60 additional binding and enzyme assays showed that Lu AE60157 displays 16-fold selectivity to the h5-HT(2A) receptor (K(i) 3.2nM) and >100-fold selectivity to all other evaluated targets. Lu AE60157 was labeled with tritium in the N-methyl group and evaluated as a radioligand in vitro as well as in vivo in rats and mice. Autoradiography experiments showed that [(3)H]Lu AE60157 bound preferentially to rat brain regions with expected high 5-HT(6) receptor density. Furthermore, [(3)H]Lu AE60157 showed good brain penetration after systemic administration and high (about 75%) specific in vivo binding to the striatal 5-HT(6) receptor in rats. The striatal binding of [(3)H]Lu AE60157 was fully displaced by selective 5-HT(6) receptor antagonists (SB-742457; Lu AE58054) and antipsychotics known to inhibit the binding of 5-HT(6) receptors in vitro (clozapine; olanzapine; sertindole), but was not displaced by antipsychotics lacking high 5-HT(6) receptor affinities (risperidone; haloperidol; quetiapine).
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CAS 607742-69-8 SB742457

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