Molecular Formula | C18H28N2O3SHCl |
Solubility | Soluble in water (100 mM ), DMSO (100 mM ), phosphate buffered saline (5 mM ), and |
Appearance | powder |
Storage Condition | 2-8°C |
Use | A selective and potent SR-7 antagonist. |
In vitro study | SB-269970 inhibits 5-CT stimulated adenylate cyclase activity on guinea pig hippocampal cell membrane. SB-269970 (0.03 μm, 0.1 μm, 0.3 μm and 1 μm) will shift the 5-CT concentration response curve to the right, this effect correlated with the SB-269970 concentration but did not change significantly for the 5-CT maximal response. SB-269970 (1 M) alone has little effect on the efflux of 5-HT. SB-269970 inhibited the activity of 5-CT-stimulated adenylate cyclase on the membrane of guinea pig hippocampus. SB-269970 (0.03 μm, 0.1 μm, 0.3 μm and 1 μm) will shift the 5-CT concentration response curve to the right, this effect correlated with the SB-269970 concentration but did not change significantly for the 5-CT maximal response. SB-269970 (1 M) alone has little effect on the efflux of 5-HT. |
In vivo study | SB-269970 (10 mg/kg and 30 mg/kg) can significantly reduce the effect of ampetamine by 25 and 27%, respectively, and can block the effect of ketamine by 38% (10 mg/kg). And 30% (30 mg/kg). SB-269970 significantly attenuated ampetamine-induced ADHD in wild-type mice but had no effect on 5-HT7 knockout mice. Systemic SB-269970 (30 mg/kg) treatment significantly reversed the disruption of PPI caused by ampetamine but did not increase the amount of PPI itself compared to the control group. SB-269970 can significantly reverse the MK-801-induced defect but has no effect on the scopolamin-induced. SB-269970 normalizes MK-801 induced glutamate but has no effect on the release of dopamine in the cortex. SB-269970 (0.5 or 1 mg/kg) showed specific anti-Anxiety-like effects in the rat Vogel drinking water test, the elevated plus maze test and the mouse four-plate test. In addition, SB-269970 (5 or 10 mg/kg) had antidepressant effects in forced swimming and tail suspension experiments in mice. 0.3, 1 and 3 μg SB-269970 had anti-collision effects that were lower than diazepa (40 μg), while 3 and 10 μg SB-269970 had anti-collision effects with imipramine (0.1 μg). SB-269970 (10 mg/kg and 30 mg/kg) can significantly reduce the effect of ampetamine by 25 and 27%, respectively, the effect of ketamine was blocked by 38% (10 mg/kg) and 30% (30 mg/kg). SB-269970 significantly attenuated ampetamine-induced ADHD in wild-type mice but had no effect on 5-HT7 knockout mice. Compared with the control group, the systemic administration was SB-269970 (30 mg/kg) treatment can significantly reverse the destruction of PPI caused by AMP, but does not increase the content of PPI itself. SB-269970 can significantly reverse the MK-801-induced defect but has no effect on the scopolamin-induced. SB-269970 normalizes MK-801 induced glutamate but has no effect on the release of dopamine in the cortex. SB-269970 (0.5 or 1 mg/kg) showed specific anti-Anxiety-like effects in the rat Vogel drinking water test, the elevated plus maze test and the mouse four-plate test. In addition, SB-269970 (5 or 10 mg/kg) had antidepressant effects in forced swimming and tail suspension experiments in mice. 0.3, 1 and 3 μg SB-269970 had anti-collision effects that were lower than diazepa (40 μg), while 3 and 10 μg SB-269970 had anti-collision effects with imipramine (0.1 μg). Compared with the obvious anti-immobility effect |
WGK Germany | 3 |