Carrier-Mediated Delivery of Low-Molecular-Weight N-Containing Drugs across the Blood–Brain Barrier or the Blood–Retinal Barrier Using the Proton-Coupled …

T Tashima - Future Pharmacology, 2023 - mdpi.com
While it is true that pharmacotherapy has achieved desired health outcomes, significant
unmet medical needs persist in the field of central nervous system (CNS) drugs, particularly …

The mystery of the human proton-organic cation antiporter: one transport protein or many?

A Sachkova, O Jensen, C Dücker, S Ansari… - Pharmacology & …, 2022 - Elsevier
About 30% of all small molecular drugs are organic cations (OCs). If these are more or less
hydrophilic, they require membrane transporters to pass through biological membranes …

Several orphan solute carriers functionally identified as organic cation transporters: Substrates specificity compared with known cation transporters

KEM Redeker, J Brockmöller - Journal of Biological Chemistry, 2024 - jbc.org
Organic cations comprise a significant part of medically relevant drugs and endogenous
substances. Such substances need organic cation transporters for efficient transfer via cell …

Substrates of the human brain proton-organic cation antiporter and comparison with organic cation transporter 1 activities

DA Doetsch, S Ansari, O Jensen, L Gebauer… - International Journal of …, 2022 - mdpi.com
Many organic cations (OCs) may be transported through membranes by a genetically still
uncharacterized proton-organic cation (H+ OC) antiporter. Here, we characterized an …

Pharmacophore-based discovery of substrates of a novel drug/proton-antiporter in the human brain endothelial hCMEC/D3 cell line

M Smirnova, L Goracci, G Cruciani, L Federici… - Pharmaceutics, 2022 - mdpi.com
A drug/proton-antiporter, whose the molecular structure is still unknown, was previously
evidenced at the blood-brain barrier (BBB) by functional experiments. The computational …

Harnessing Pharmacogenomics in Clinical Research on Psychedelic‐Assisted Therapy

A Halman, R Conyers, C Moore, D Khatri… - Clinical …, 2025 - Wiley Online Library
Psychedelics have recently re‐emerged as potential treatments for various psychiatric
conditions that impose major public health costs and for which current treatment options …

Region-independent active CNS net uptake of marketed H+/OC antiporter system substrates

F Bällgren, Y Hu, S Li, L Van De Beek… - Frontiers in Cellular …, 2024 - frontiersin.org
The pyrilamine-sensitive proton-coupled organic cation (H+/OC) antiporter system facilitates
the active net uptake of several marketed organic cationic drugs across the blood-brain …

High-throughput expression and purification of human solute carriers for structural and biochemical studies

S Raturi, H Li, YN Chang, A Scacioc… - Journal of Visualized …, 2023 - ora.ox.ac.uk
Solute carriers (SLCs) are membrane transporters that import and export a range of
endogenous and exogenous substrates, including ions, nutrients, metabolites …

Dysfunction of the Neurovascular Unit by Psychostimulant Drugs

TTL Vo, D Shin, E Ha, JH Seo - International Journal of Molecular …, 2023 - mdpi.com
'Drug abuse'has been recognized as one of the most pressing epidemics in contemporary
society. Traditional research has primarily focused on understanding how drugs induce …

An extended substrate spectrum of the proton organic cation antiporter and relation to other cation transporters

C Ali Khan, N Kirsch, J Brockmöller… - Basic & Clinical …, 2024 - Wiley Online Library
Most central nervous system (CNS) active drugs are organic cations, which need carrier
proteins for efficient transfer through the blood–brain barrier (BBB). A genetically still …