International Scholarly Research Notices / 2014 / Article / Tab 4

Review Article

Transendothelial Transport and Its Role in Therapeutics

Table 4

Major neurotransmitter transporters occur at blood brain barrier.

NeurotransmittersTransporter/mechanismLocationInflux or efflux/functionReferences

NeurotransmittersDiffusion Membrane of presynaptic and postsynaptic neuron fiber Influx[86]

CholineCarrier-mediated processMembrane of presynaptic and postsynaptic neuron fiberInflux and efflux regulate the formation of acetylcholine in the central nervous system.[87]

AcetylcholineFacilitated diffusion, saturable glycoproteins (Pgp) transport systemNeuronal circuits of brain, membrane of presynaptic, and postsynaptic neuron fiberInflux, Synaptic transmission, occurs in peripheral nervous system. [86, 8890]

GlycineReceptor mediatedMembrane receptorsMakes the postsynaptic membrane more permeable to Cl-ions.

AspartateAspartate ion channelMembrane receptors

GlutamateGlutamate chloride-independent membrane transport systemMembrane receptors

Glutamate/asparateATP-driven Na+-K+-aseMembrane receptors

Biogenic amines, norepinephrineNorepinephrine transporter, uptake1 and uptake2 carrier-mediated transporters, Net (Slc6a2), Dat (Slc6a3), and Sert (Slc6a4) NorepinephrineNorepinephrine transporter Alzheimer's disease and attention deficient hyperactivity disorder [68, 92, 93]
[9496]; [97]

MelatoninMembrane receptorsMelatonin receptors in the area postrema located outside the blood-brain barrier[98, 99]

PeptidesMembrane receptors[100]

Cholecystokinin-1 receptor agonistCholecystokinin-1 receptor agonistMembrane receptors[101, 102]

GI hormone Membrane receptors[103, 104]

Insulin, transferrin, insulin-like growth factors and vasopressinReceptor-mediated transcytosisMembrane receptors[105]


GABA (GAT2, BGT1)Amino acid transporterGABAGABA imposes inhibitory effects on the brain neurons that show protective role during hypoxia or ischemia, active transport into the astrocyte glial cells

Nucleoside transporters

nucleoside transporters (ENTes & ENTei)
Nucleoside transportersNucleosidePurine and pyrimidine nucleosides, purine, and pyrimidine nucleosides

Ion transporters

Na/K-ATPaseActive transportPotassiumNerve conduction

Ca-ATPaseActive transportCalciumBone marrow

SodiumActive transportSodiumNerve conduction

Potassium, chlorideActive transportPotassium/chloride cotransporterNerve conduction

ATP-binding cassette (ABC) transporters

P-glycoprotein (P-gp) multidrug resistance transporter
Mdr1a [Mdr3], Mdr1a [Mdr3],
Mdr1b [Mdr1], and
Mdr2; human MDR1 & 2)
Active transportOrganic, hydrophobic, and amphipathic cations: -adrenergic blockers, anthracyclines,
cyclosporine A, digoxin, etoposide, glucocorticoids, loperamide,
morphine, phenytoin, vecuronium, verapamil, and vinca alkaloids
Inhibition of drug transport

Multidrug resistance associated protein (MRP1)Active transportAmphipathic anions and glutathione, glucuronide and sulfate conjugates:
benzylpenicillin, doxorubicin, etoposide,
methotrexate, vinblastine, and

MRP2 (c-MOAT)Active transportOrganic anionsEfflux

MRP3 (MOAT-D)Active transportMethotrexate, anionic conjugatesEfflux

MRP4 (MOATB)Active transportNucleoside-based antiviralsEfflux

MRP5 (MOAT-C)Active transportCyclic nucleotides, glutathione conjugates, and organic anionsEfflux

MRP6 (MOAT-E)Active transportPeptidesEfflux

Breast cancer resistance protein BCRP)Active transportSimilar to P-gp substrates; camptothecin derivatives, daunorubicin, doxorubicin,
mitoxantrone, and topotecan

OCT1-3, Active transportMonoamine neurotransmitters, cationic neurotoxins, amantadine, memantine, desipramine, dopamine, and serotoninInflux and efflux

OCTN1Active transportAntiarrhythmic drugs, tetraethylammonium verapamilInflux and efflux

OCTN2-lactam antibiotics, L-carnitine, and tetraethylammoniumInflux and efflux

Organic ion transporting polypeptide 1 (oatp1, OATP1)Active transportBulky organic cations, glucuronide conjugates, steroid hormones, estrone sulfate, indinavir, nelfinavir, opioid agonists, and ouabainInflux and efflux

Oatp2, OATP2Active transportAmphipathic anions: bile acids, cholate, digoxin, estrogen conjugates, opioid agonists, and ouabain, taurocholate; dehydroepiandrosterone sulfate and
estrone-1-sulfate efflux; 26-enkephalin;
Influx and efflux

Oatp3Active transportDigoxin, 26-enkephalin, fexofenadine 3,5,3-triiodo-L-thyronineInflux and efflux

BBB-specific anion transporter type 1 (Bsat1,
Active transportT4Influx and efflux

OATP-A, OAT1, OAT3Active transportAmphipathic anions, bile acids, deltorphin
II, estrone-1-sulfate, fexofenadine,
opioid peptides, and benzylpenicillin Cimetidine, dehydroepiandrosterone sulfate, estrone sulfate,
indoxyl sulfate, and PAH
Influx and efflux

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