human organic cation transporters

Trimipramine maleate (Surmontil maleate) 是一种 5-HT 受体拮抗剂，对 5-HT1C、5-HT2和 5-HT1A 受体的 pKi 值分别为 6.39、8.10和 4.66。

cDPCP is a platinum-containing DNA-crosslinking agent.1Unlike cisplatin or oxaliplatin , cDPCP forms monofunctional DNA adducts. It is transported into cells by organic cation transporter 1 (OCT1) and OCT2, inhibiting proliferation of MDCK cells expressing the human transporters with IC50values of 8.1 and 1.5 μM, respectively. cDPCP inhibits RNA polymerase II-mediated transcription in a reporter assay using HeLa cells. It increases survival in murine S180 sarcoma and P388 leukemia models when administered at doses of 40 and 80 mg/kg, respectively.2 1.Lovejoy, K.S., Todd, R.C., Zhang, S., et al.cis-Diammine(pyridine)chloroplatinum(II), a monofunctional platinum(II) antitumor agent: Uptake, structure, function, and prospectsProc. Natl. Acad. Sci. USA105(26)8902-9807(2008) 2.Hollis, L.S., Amundsen, A.R., and Stern, E.W.Chemical and biological properties of a new series of cis-diammineplatinum(II) antitumor agents containing three nitrogen donors: cis-[Pt(NH3)2(N-donor)Cl]+J. Med. Chem.32128-136(1989)

Trimipramine N-oxide 为三环抗抑郁药trimipramine的活性代谢物，其对人去甲肾上腺素单胺转运体(hNAT)、血清素(hSERT)、多巴胺(hDAT)以及人体有机阳离子转运蛋白(hOCT1与hOCT2)的IC50值分别为11.7、3.59、9.4、9.35及27.4 nM。因此，Trimipramine N-oxide在忧郁和焦虑研究中有应用价值。

6-hydroxy Buspirone是抗焦虑化合物buspirone的活性代谢产物，通过细胞色素P450（CYP）亚型CYP3A4从buspirone转化而来。该化合物在大鼠海马和背侧缝核的5-羟色胺（5-HT）受体亚型5-HT1A上具有亲和力（EC50s分别为4和1 µM），并作为多巴胺D2、D3、D4受体拮抗剂（IC50s分别为3.1、4.9、和0.85 µM）。同时，它还以浓度依赖性方式抑制表达人类转运体的S2近端小管细胞中的有机阳离子转运体1（OCT1）、OCT2和OCT3。