| 中文名称 | 酒石酸酮色林 |
| 英文名称 | KETANSERIN TARTRATE |
| CAS号 | 83846-83-7 |
| 分子式 | C26H28FN3O9 |
| 分子量 | 545.52 |
| EINECS号 | 281-062-8 |
| 熔点 | 183~186℃ |
| 溶解度 | 乙醇:3.3mg/mL |
| 形态 | 固体 |
| 颜色 | 白色 |
| 水溶解性 | Soluble to 10 mM in water |
| 危险品标志 | T |
| 危险类别码 | 25 |
| 安全说明 | 22-36/37/39-45 |
| 危险品运输编号 | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS号 | VA1411195 |
| 海关编码 | 29335990 |
| 危险等级 | 6.1 |
| 毒性 | LD50 oral in rat: 129mg/kg |
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5-HT 2 Receptor
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hERG current 0.11 μM (IC 50 ) |
Ketanserin at 0.3 μM inhibits the voltage-dependent step current (I hERG.step ) and tail current (I hERG.tail ) of hERG channels with a 5-min exposure. The synergistic effect observed for AA with 5-HT is, also, blocked by the 5-HT receptor blockers cyproheptadine (IC 50 =22.0±7 μM), Ketanserin (IC 50 =152±23 μM). Ketanserin (50-350 μM) inhibits the synergism by blocking the receptor in a dose-dependent manner. The IC 50 value of Cyproheptadine is 22±7 μM and Ketanserin is 152±23 μM. Ketanserin inhibits platelet aggregation with an IC 50 of 240 (169-339) nM.
Ketanserin is a 5-HT2A receptor antagonist. Ketanserin significantly reduces BDNF protein levels in numerous brain regions (CA1 and CA3 of the hippocampus, prefrontal cortex, central amygdaloid nucleus, dorsomedial hypothalamic nucleus, dentate gyrus, shell of the nucleus accumbens and midbrain periaqueductal gray). 5-HT 2A antagonist Ketanserin can significantly reduce BDNF mRNA levels in various brain regions.