中文名 | 酒石酸酮色林 |
英文名 | ketanserin tartrate |
别名 | 酮色酒石酸 酒石酸酮色林 酒石酸酮舍林 酒石酸酮色啉盐 酮舍林酒石酸盐 酮舍林酒石酸盐(标准品) 3-(2-(4-(4-氟苯甲酰基)哌啶-1-基)乙基)喹唑啉-2,4(1H,3H)-二酮 2,3-二羟基琥珀酸盐 |
英文别名 | kjk-945 R 41468 ketanserin tartrate R 41468 TARTRATE SALT KETANSERIN HYDROGEN TARTRATE 4(1h,3h)-quinazolinedione,3-(2-(4-(4-fluorobenzoyl)-1-piperidinyl)ethyl)-( 3-(2-(4-(p-fluorobenzoyl)-1-piperidinyl)ethyl)-2,4(1h,3h)-quinazolinedionel 3-[2-[4-(4-fluorobenzoyl)piperidino]ethyl]quinazoline-2,4(1H,3H)-dione [R-(R*,R*)]-tartrate |
CAS | 83846-83-7 |
EINECS | 281-062-8 |
化学式 | C26H28FN3O9 |
分子量 | 545.52 |
InChI | InChI=1/C22H22FN3O3.C4H6O6/c23-17-7-5-15(6-8-17)20(27)16-9-11-25(12-10-16)13-14-26-21(28)18-3-1-2-4-19(18)24-22(26)29;5-1(3(7)8)2(6)4(9)10/h1-8,16H,9-14H2,(H,24,29);1-2,5-6H,(H,7,8)(H,9,10)/t;1-,2+ |
熔点 | 183~186℃ |
溶解度 | 乙醇: 3.3mg/ml |
存储条件 | 2-8°C |
外观 | 固体 |
颜色 | white |
物化性质 | 白色或类白色粉末 |
MDL号 | MFCD00084651 |
体外研究 | 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. |
体内研究 | 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. |
危险品标志 | T - 有毒物品 |
风险术语 | 25 - 吞食有毒。 |
安全术语 | S22 - 切勿吸入粉尘。 S36/37/39 - 穿戴适当的防护服、手套和护目镜或面具。 S45 - 若发生事故或感不适,立即就医(可能的话,出示其标签)。 |
危险品运输编号 | UN 2811 6.1/PG 3 |
WGK Germany | 3 |
RTECS | VA1411195 |
海关编号 | 29335990 |
Hazard Class | 6.1 |
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