What is renal OCT2 substrate?
What is renal OCT2 substrate?
OCT2 is a primarily renal uptake transporter that is expressed on the basolateral (blood) side of proximal tubule cells. It plays a key role in the disposition and renal clearance of mostly cationic drugs and endogenous compounds.
What are OCT2 inhibitors?
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What is MATE1 substrate?
Substrates for MATE1 and MATE2-K are typical organic cations, TEA, 1-methyl-4-phenylpyridinium (MPP), metformin, cimetidine, procainamide and so on (Table 2) (Tanihara et al., 2007).
What is organic cation transporter2?
Organic cation transporter 2 (OCT2) is the key transporter for cation influx in the renal epithelial cells. It involves in the first step of renal elimination that uptakes drug molecules from blood, across the basolateral membrane, into the proximal tubule cell.
What is Bcrp substrate?
BCRP SUBSTRATES Substrates of BCRP initially were reported to be a wide range of chemotherapeutics such as mitoxantrone, camptothecin derivates, flavopiridol, and methotrexate (1). Notably, several TKIs such as imatinib, gefitinib, and nilotinib are BCRP substrates (1,13).
What is MATE2?
MATE2 is an electroneutral, Na+-independent, pH-dependent proton antiporter with 13 predicted membrane-spanning domains. Unusually for SLC drug transporters, MATE2 functions as an efflux transporter in vivo [3-5][3-5][3-5].
What drugs are BCRP substrates?
BCRP substrates are not limited to chemotherapeutics. Drugs that have been shown to be BCRP substrates include, among others, prazosin, glyburide, cimetidine, sulfasalazine, and rosuvastatin (1,13). Nucleoside and nucleotide analogs such as AZT and lamivudine are also BCRP substrates (1).
What does BCRP stand for?
ABCG2, more commonly referred to as BCRP (Breast Cancer Resistance Protein), is an efflux transporter that serves two major drug transport functions. Firstly, it restricts the distribution of its substrates into organs such as the brain, testes, placenta, and across the gastrointestinal tract (GIT).
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What drugs are BCRP inhibitors?
BCRP inhibitors include, among others, fumitremorgin C (FTC), the FTC analogue Ko143, the acridone carboxamide derivative GF120918, anti-HIV protease inhibitors nelfinavir and ritonavir, the dietary flavonoids chrysin and biochanin A, the tyrosine kinase inhibitors gefitinib and imatinib [5, 16, 36], and herb extracts …
What is PGP substrate?
Substrates of P-glycoprotein are susceptible to changes in pharmacokinetics due to drug interactions with P-gp inhibitors or inducers. Some of these substrates include colchicine, ciclosporin, dabigatran, digoxin, diltiazem, fexofenadine, indinavir, morphine, and sirolimus.
What is a BCRP substrate?