CAS NO: | 62717-42-4 |
包装 | 价格(元) |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 291.77 |
Cas No. | 62717-42-4 |
Formula | C16H18ClNO2 |
Solubility | ≥29.2 mg/mL in DMSO; ≥14.75 mg/mL in H2O with ultrasonic; ≥3 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 1-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine-7,8-diol hydrochloride |
Canonical SMILES | OC1=C(O)C=C2C(CCNCC2C3=CC=CC=C3)=C1.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次半岛bd体育手机客户端 溶解度各有差异,仅做参考。若实验所需浓度过大至半岛bd体育手机客户端 溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
SKF38393 HCl(SKF38393)是多巴胺D1受体的选择性激动剂[1],IC50值为110 nM [2]。
有两种功能类型的多巴胺受体,D1和D2受体[3]。前额皮层(PFC)D1受体(D1R)的活化引起‘倒U型’剂量反应。太少或太多D1R的刺激可削弱空间工作记忆[4]。
6-OHDA减少了纹状体神经元中编码P物质和D1多巴胺受体的mRNA的特异性表达。随后每天注射SKF-38393逆转了这一还原效果。SKF-38393还增加了强啡肽的mRNA[5]。D1Rs激活环AMP依赖性蛋白激酶,刺激腺苷酸环化酶,调节神经元的生长和分化,并改变多巴胺D2受体介导的细胞活动和行为[3]。在96孔板测定中,MCF-7细胞的接种参与了乳腺癌的体外筛选过程。1天之后,用SKF 38393培养细胞2天。数据表明,SKF 38393显著地降低了MCF-7细胞的增殖。IC50值是0.1 +/- 0.03 μM[6]。
在麻醉、人为气息奄奄及加拉明处理的大鼠中,静脉给药SKF 38393显著地改变了多巴胺的细胞活性。在这些大鼠中,可观察到放电率的增加和减少[7]。
参考文献:
[1]. Rimondini R, Ferré S, Giménez-Llort L, et al. Differential effects of selective adenosine A1 and A2A receptor agonists on dopamine receptor agonist-induced behavioral responses in rats. European journal of pharmacology, 1998, 347(2): 153-158.
[2]. Altar CA, Marien MR. Picomolar affinity of 125I-SCH 23982 for D1 receptors in brain demonstrated with digital subtraction autoradiography. The Journal of neuroscience, 1987, 7(1): 213-222.
[3]. Sunahara RK, Niznik HB, Weiner DM, et al. Human dopamine D1 receptor encoded by an intronless gene on chromosome 5. 1990, 347:80-83.
[4]. Vijayraghavan S, Wang M, Birnbaum SG, et al. Inverted-U dopamine D1 receptor actions on prefrontal neurons engaged in working memory. Nature neuroscience, 2007, 10(3): 376-384.
[5]. Gerfen CR, Engber TM, Mahan LC, et al. D1 and D2 dopamine receptor-regulated gene expression of striatonigral and striatopallidal neurons. Science, 1990, 250(4986): 1429-1432.[6]. Johnson DE, Ochieng J, Evans SL. The growth inhibitory properties of a dopamine agonist (SKF 38393) on MCF-7 cells. Anti-cancer drugs, 1995, 6(3): 471-474.
[7]. Carlson JH, Bergstrom DA, Weick BG, et al. Neurophysiological investigation of effects of the D-1 agonist SKF 38393 on tonic activity of substantia nigra dopamine neurons. Synapse, 1987, 1(5): 411-416.