ArticleHandbook of experimental pharmacology2021
Organic Cation Transporter (OCT/OCTN) Expression at Brain Barrier Sites: Focus on CNS Drug Delivery.
Article in Handbook of experimental pharmacology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
22 citing papers in PubMed, 28 citations in OpenAlex.
- Hepatic drug transporters in pharmacotherapy: mechanisms, therapeutic targeting, and clinical translation.Naunyn-Schmiedeberg's archives of pharmacology · 2026Review
- C1qc Mediates Blood-Brain Barrier Disruption in a Mouse Model of Intracerebral Haemorrhage Through Microglia-Derived Migrasomes.Journal of extracellular vesicles · 2026Article
- Article
- A Remarkable Tale: Increased Retinal Fluorescence Following Application of Permanent Marker Ink to Mouse Tails.Investigative ophthalmology & visual science · 2026Article
- Gabapentin CNS exposure and analgesic response are modulated by OCT2 genotype in patients with chronic neuropathic pain.Frontiers in pharmacology · 2026Article
- Diverse Applications of the Anti-Diabetic Drug Metformin in Treating Human Disease.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Delocalized quinolinium-macrocyclic peptides, an atypical chemotype for CNS penetration.Science advances · 2024Article
- Metabolite transport across central nervous system barriers.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2024Review
- Circadian ABCG2 Expression Influences the Brain Uptake of Donepezil across the Blood-Cerebrospinal Fluid Barrier.International journal of molecular sciences · 2024Article
- Article
- CNS Drug Delivery in Stroke: Improving Therapeutic Translation From the Bench to the Bedside.Stroke · 2024Review
- Non-Invasive Drug Delivery across the Blood-Brain Barrier: A Prospective Analysis.Pharmaceutics · 2023Review
- Uptake Transporters at the Blood-Brain Barrier and Their Role in Brain Drug Disposition.Pharmaceutics · 2023Review
- Targeting Non-Coding RNA for CNS Injuries: Regulation of Blood-Brain Barrier Functions.Neurochemical research · 2023Review
- Current Update on Transcellular Brain Drug Delivery.Pharmaceutics · 2022Review
- Peptides as Pharmacological Carriers to the Brain: Promises, Shortcomings and Challenges.Molecular pharmaceutics · 2022Review
- Targeting organic cation transporters at the blood-brain barrier to treat ischemic stroke in rats.Experimental neurology · 2022Article
- Transport Mechanisms at the Blood-Brain Barrier and in Cellular Compartments of the Neurovascular Unit: Focus on CNS Delivery of Small Molecule Drugs.Pharmaceutics · 2022Review
- Increased/Targeted Brain (Pro)Drug Delivery via Utilization of Solute Carriers (SLCs).Pharmaceutics · 2022Review
- Blood-Brain Barrier Transporters: Opportunities for Therapeutic Development in Ischemic Stroke.International journal of molecular sciences · 2022Review
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Therapeutic delivery to the central nervous system (CNS) continues to be a considerable challenge in the pharmacological treatment and management of neurological disorders. This is primarily due to the physiological and biochemical characteristics of brain barrier sites (i.e., blood-brain barrier (BBB), blood-cerebrospinal fluid barrier (BCSFB)). Drug uptake into brain tissue is highly restricted by expression of tight junction protein complexes and adherens junctions between brain microvascular endothelial cells and choroid plexus epithelial cells. Additionally, efflux transport proteins expressed at the plasma membrane of these same endothelial and epithelial cells act to limit CNS concentrations of centrally acting drugs. In contrast, facilitated diffusion via transporter proteins allows for substrate-specific flux of molecules across the plasma membrane, directing drug uptake into the CNS. Organic Cation Transporters (OCTs) and Novel Organic Cation Transporters (OCTNs) are two subfamilies of the solute carrier 22 (SLC22) family of proteins that have significant potential to mediate delivery of positively charged, zwitterionic, and uncharged therapeutics. While expression of these transporters has been well characterized in peripheral tissues, the functional expression of OCT and OCTN transporters at CNS barrier sites and their role in delivery of therapeutic drugs to molecular targets in the brain require more detailed analysis. In this chapter, we will review current knowledge on localization, function, and regulation of OCT and OCTN isoforms at the BBB and BCSFB with a particular emphasis on how these transporters can be utilized for CNS delivery of therapeutic agents.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.