2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. SB357134

SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats.

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SB357134 Chemical Structure

SB357134 Chemical Structure

CAS No. : 219963-52-7

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SB357134 Related Antibodies

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

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Description

SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats[1].

In Vitro

SB-357134 (0.1, 0.3, 1, and 3 μM) concentration-dependently inhibits the 5-HT-mediated increased level of cAMP, which is surmountable at high 5-HT concentrations, consistent with competitive antagonism[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SB357134 Related Antibodies
In Vivo

SB-357134 dose-dependently inhibits the specific [125I]SB-258585 binding[1].
SB-357134 (0.03-30 mg/kg; 0-24 h; p.o.; single dose) produces a potent and dose-related anticonvulsant effect in the rat MEST model, with a minimum significantly effective dose of 0.1 mg/kg[1].
Chronic administration of SB-357134 (10 mg/kg; p.o.; twice daily; 7 days) significantly shortens path length compared to vehicle and acute administration of SB-357134[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague–Dawley rats[1]
Dosage: 0.03–30 mg/kg
Administration: 0-24 h; p.o.; 0.03–30 mg/kg
Result: Produced a potent and dose-related anticonvulsant effect in the rat MEST model, with a minimum significantly effective dose of 0.1 mg/kg. Increased seizure threshold up to 123±12% at the highest dose tested of 30 mg/kg. At 10 mg/kg, exhibited a rapid onset of action, significantly increasing seizure threshold from a control value of 21.7 to 26.7 mA at 1 h postdose. Observed Peak activity within 4–6 h postdose. With the exception of an unexplained loss of activity at 12 h, had a long duration of action of 21 h in this model.
Animal Model: Sprague–Dawley rats[1]
Dosage: 10 mg/kg
Administration: 10 mg/kg; p.o.; twice daily; 7 days
Result: Significantly shortened path length when administered chronically compared to vehicle and administered acutely.
Molecular Weight

523.21

Formula

C17H18Br2FN3O3S
CAS No.
SMILES

O=S(C1=CC=C(C(N2CCNCC2)=C1)OC)(NC3=CC(Br)=CC(F)=C3Br)=O
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Purity & Documentation
References
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SB357134 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SB357134219963-52-7SB 357134SB-3571345-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorRatbrain penetrant5-HT6 receptorInhibitorinhibitorinhibit

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