CAS NO: | 912342-28-0 |
生物活性 | TCB2 is an agonist of serotonin5-HT2Areceptor. | ||||||||||||||||
IC50& Target |
| ||||||||||||||||
体外研究 (In Vitro) | The selective 5-HT2Aagonist TCB2 at 30 nM produces a marked shift to the right in the competition curve obtained with the 5-HT1Areceptor agonist ipsapirone from [3H]-8-OHDPAT binding sites in both areas of the brain. A significant increase in the mean Kivalue is obtained with TCB2, demonstrating a reduction in the affinity of the high-affinity 5-HT1Aagonist binding sites by the 5-HT2Aagonist in both regions. In the case of hippocampus, there are also indications for antagonistic effects of ketanserin[2]. | ||||||||||||||||
体内研究 (In Vivo) | In an initial dose-response study, TCB2 (0.5, 1.0, and 2.5 mg/kg) and DOI (0.5, 1.0, 2.5, and 5.0 mg/kg) induce head twitches in C57BL/6J mice in a dose-dependent manner compared to vehicle. Head twitches induced by TCB2 and DOI are similar across the doses, with the exception that at the highest dose (5.0 mg/kg), TCB2 induces half as many head twitches as does DOI (p=0.021). Confirming 5-HT2A mediation of the head twitch response, in two separate studies, pretreatment with the selective 5-HT2Aantagonist MDL 11,939 (1.0 mg/kg) block head twitches induced by DOI (2.5 mg/kg) and by TCB2 (2.5 mg/kg; p<0.0001). Compared to vehicle, corticosterone levels are increased following TCB2 (5.0 mg/kg, p=0.01; 10.0, p=0.012; with a trend following 2.5 mg/kg, p=0.079) and DOI (10.0 mg/kg, p=0.035)[1]. | ||||||||||||||||
分子量 | 353.05 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C11H15Br2NO2 | ||||||||||||||||
CAS 号 | 912342-28-0 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 100 mg/mL(283.25 mM;ultrasonic and warming and heat to 60℃) H2O : 25 mg/mL(70.81 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
维奥蛋白资源库 - 中文蛋白资源 CopyRight © 2010-2024 |