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INFLUX GUT CELL APICAL MEMBRANE
ASBT, PEPT-1, MCT-1, OATP-2B1/1A2, NPT, NT-1/2, AAT, OCT-1
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EFFLUX GUT CELL APICAL MEMBRANE
Pgp/MDR-1, MPR-2, BCRP
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INFLUX GUT CELL BLOOD MEMBRANE
MCT-1
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EFFLUX GUT CELL BLOOD MEMBRANE
MRP-3
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INFLUX LIVER CANALICULAR MEMBRANE
None
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EFFLUX LIVER CANALICULAR MEMBRANE
Pgp, MRP2, BSEP, MATE, BCRP
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INFLUX LIVER SINUSOIDAL MEMBRANE
OATP-1B1/1B3/2B1, NTCP, OAT-2, OCT-1, MCT-2
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EFFLUX LIVER SINUSOIDAL MEMBRANE
MRP-3
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INFLUX KIDNEY BRUSH BORDER MEMBRANE
OCT-N1/N2, OATP 1A2, PEPT-1/2, ASBT, CNT-1/2, NT-1/2, Ascorbic acid Transporter, Inorganic Sulfate ion
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EFFLUX KIDNEY BRUSH BORDER MEMBRANE
MRP-2/4, MATE, Pgp, BCRP, OATK-1/2
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INFLUX KIDNEY BASOLATERAL MEMBRANE
OAT-1/2/3, OCT-1/2/3
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EFFLUX KIDNEY BASOLATERAL MEMBRANE
MRP-3, OST-ALPHA/BETA
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ABCs = ?
Pgp, BCRP, MPR-2, BSEP, MATE
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ASBT can transport what? (3 things)
Taurocholate, Urso/Cheno-deoxycholic acid
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ASBT stands for
Apical Sodium-dependent Bile acid Transporter
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PEPT-1 transports? (6 things/groups; 3 of which has e.g.)
- -Penicillins
- -Amino-cephalosporins
- -ACE inhibitors (E.g. statins/bestatins)
- -Peptidomemetic prodrugs (Antiviral nucleosides such as Acyclovir/Valacyclovir)
- -Short-chain peptides
- -Di/Tri-peptides (E.g. Beta-lactam antibiotics: Cepha-, Cefa-)
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PEPT1 stands for what? It is coupled with? Therefore it is affected by change in?
- Oligopeptide Transporter 1
- Proton Coupled therefore affected by pH
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MCT-1 transports? (1 group; 3 examples)
Simple Carboxylic acids (Salicylic acid, benzoic acids, Gamma hydroxybutyrate (GHB))
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MCT-1 stands for?
Monocarboxylic acid Transporter 1
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OATP stands for ? What types are there? What is it inhibited by ?
- Organic Anion Transporting Polypeptide.
- 1B1/1B3/1A2/2B1 types
- Inhibited by grapefruit juice
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OATP 2B1/1A2 tranports what ?
- Endogenous substrates (e.g. steroid conjugates E1S)
- Xenobiotics (e.g. statins)
Examples for above: Estrone sulfate, benzylpenicillin, pravastatin, glibenclamide
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OATP 1B1/1B3 transports what ?
- Endogenous substrates: Taurocholate, bile acids, bilirubin
- Anions: Estrogen sulfate, E217G, Ace inhibitors (enalapril[Vasotec], temocaprilat), HMG Co-A inhibitor (statins-pravastatin, rosuvastatin, atorvastatin), BSP, methotrexate, peptides
- Steroids: Ouabain, thyroid hormones
- Cations - fexofenadine (Allegra), ajmalinium, quaternary ammonium compounds (vercuronium, N-methylquinidine)
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NPT stands for ?
Sodium-dependent Phosphate Transporter
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NPT looks for what molecules in a drug?
P=O and ONa
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NPT transports ?
- Fosfomycin (antibacterial)
- Foscarnet (antiviral)
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Amino Acid Transporter transports ?
- Gabapentin (seizures)
- Baclofen (spasticity)
- D-cycloserine (antibiotics)
- L-dopa
- Methyldopa
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OCT stands for ? And how many types ?
Organic Cation Transporter 1/2/3
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OCT-1 in the GUT transports ?
Antivirals (Acyclovir, ganciclovir)
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OCT-1 in LIVER transports ?
- Procainamide ethylbromide (PAEB)
- Tetramethylammonium (TEA)
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OCT-1/2/3 in KIDNEY transports what ?
- Procaineamide ethylbromide
- tetraethylammonium
- cimetidine
- choline
- cisplatin,
- corticosterone
- desipramine
- histamine
- procainamide
- quinidine
- ritonavir,
- saquinavir
- verapamil
- metformin
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NT stands for ? How many types are there?
Nucleoside transporter 1/2/3/4/5
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NT-1 transports what? What do the drugs look like?
Allopurinol and Azathiprine. Look like purines
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NT-2 transports what? What do the drugs look like?
Gemcitabine, cytarabine and 5-Fluorouracil. Look like pyrimidines
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NT-1/2/3/4/5 in LIVER transports what?
- Acyclovir
- HIV inhibitors - AZT (Zidovudine), ddl, ddc, ribavirin
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MCT-2 stands for?
Monocarboxylic acid transporter 2 and is a proton cotransporter
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MCT-2 transports?
Bigger carboxylic acids like lactate, pyruvate and benzoate
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NTCP stands for?
Sodium-dependent Taurocholate coTransporting polypeptide
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NTCP transports?
- Bile Acids - Taurocholate (TCA), cholic acid, URSO
- Statins - Pitavastatin, rosuvastatin, atorvastatin
- Anions - Estrone 3-sulfate (E1S), E217G, Bromosulfophthalein (BSP)
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OAT stands for? How many types?
Organic Anion Transporter 1/2/3
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OAT-2 transports?
P-aminohippurate, NSAIDs, salicylate, cephalorsporins
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OAT-1/3 transports? And Uses what transport system and, in that system, with what compound? Inhibited by?
Transports P-aminohippurate (PAH), Penicillins, Uric acid, probenecid, salicylic acid, acetylsalicyclic acid, indomethacin, prostaglandins, cephaloridine
Uses tertiary transport system with alpha keotglutarate
Inhibited by probenecid
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OCTN-1 transports?
Electroneutral substrates: Beta-lactam antibiotics, cephaloridine, cefoselis, cefepime, cefluprenam
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OCTN-2 is a?
Sodium-carnitine cotransporter
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Ascorbic acid transporter and inorganic sulfate ion transporter are dependent on?
Na
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Pgp stands for? and is also known as? What does that one stand for?
P-glycoprotein. AKA MDR1 - Multidrug resistance protein 1
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Pgp/MDR1 mostly transports drugs that are? (2 things)
Lipophilic and anti-cancer
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Pgp/MDR1 transports?
- ·
- Vinca Alkyloids (vinblastine, vincristine)
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- Anthracyclines (doxorubicin, daunorubicin)
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- Taxanes (Paclitaxel, docetaxel)
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- Epipodophyllotoxins (etoposide, teniposide)
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- Steroids (aldosterone, dexamethasone)
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- HIV Protease Inhibitors (Indivavir, saquinavir,
- nelfinavir, ritonavir)
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- Cardiac glycosides (digoxin)
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- Peptides (leupeptin, pepstatin A)
- ·
- Antihypertensives (propranolol, verapamil)
- ·
- Others (cyclosporins, rhodamine 123)
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MRP-2 stands for?
Multidrug resistance-associated protein 2
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MRP2 transports?
- §
- Conjugates: Glucuronides, glutathione, and
- sulfate
- §
- Statins: Pravastatin and cerivastatin
- §
- HIV protease inhibitors: Saqunavir, Ritonavir,
- and Indinavir
- §
- ACE inhibitors: enalapril and enalaprilat
- §
- Others: Etoposide, benzylpencillin, vincristine
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BCRP stands for?
Breast cancer resistance protein
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BCRP transports?
- §
- Sulfate conjugates (E1S):
- Phytoestrogens, flavonoids, cimetidine sulfate, conjugates of steroids (estrone
- sulfate), 4-methylumbelliferone sulfate
- §
- Anticancer drugs: Mitoxantrone, topotecan,
- vinblastine, methotrexate, 9-aminocamptothecin, rubitecan, anthracyclines (-rubicins)
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BSEP stands for?
Bile salt export pump
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BSEP transports?
Bile acids, pravastatin, rosuvastatin
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MATE stands for?
Multidrug and toxic compound extrusion
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MATE transports?
- §
- Ethidum aminoglycosides (Kanamycin, treptomycin)
- §
- Fluoroquinolones (ciprofloxacin, daunomycin,
- doxorubicin, norfloxacin)
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OATK-1 is a?
Methotrexate transporter
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OATK-2 transports?
Taurocholate, methotrexate, folate, prostaglandin E2
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