| Identification | Back Directory | [Name]
SB-357134 | [CAS]
219963-52-7 | [Synonyms]
SB-357134
Benzenesulfonamide, N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-(1-piperazinyl)- | [Molecular Formula]
C17H18Br2FN3O3S | [MOL File]
219963-52-7.mol | [Molecular Weight]
523.21 |
| Hazard Information | Back Directory | [Uses]
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 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]. | 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. |
| [References]
[1] Stean TO, et al. Pharmacological profile of SB-357134: a potent, selective, brain penetrant, and orally active 5-HT(6) receptor antagonist. Pharmacol Biochem Behav. 2002 Apr;71(4):645-54. DOI:10.1016/s0091-3057(01)00742-0 |
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