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Search Results for " human organic cation transporters "

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抑制剂 & 化合物

1

天然产物

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Cat. No. Product Name Target Signaling Pathways
T74582 Trimipramine N-oxide

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。
T36745 cDPCP

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 ad...
T83909 6-hydroxy Buspirone

BMY 28674,BMS-52821

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。

化合物

Trimipramine N-oxide
Cat.No: T74582
Synonym:
Target:
cDPCP
Cat.No: T36745
Synonym:
Target:
6-hydroxy Buspirone
Cat.No: T83909
Synonym: BMY 28674,BMS-52821
Target:
Cat. No. Product Name Target Signaling Pathways
T1045 Trimipramine maleate

Surmontil maleate,马来酸三甲丙咪嗪,三甲丙咪嗪马来酸盐

Dopamine Receptor; 5-HT Receptor; Antibacterial; Adrenergic Receptor; Norepinephrine; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience
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。

天然产物

Trimipramine maleate
Cat.No: T1045
Synonym: Surmontil maleate,马来酸三甲丙咪嗪,三甲丙咪嗪马来酸盐
Target: Dopamine Receptor, 5-HT Receptor, Antibacterial, Adrenergic Receptor, Norepinephrine, Histamine Receptor
TargetMol Loading
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