Considerations in the development of reversibly binding PET radioligands for brain imaging

V W. Pike - Current Medicinal Chemistry, 2016 - benthamdirect.com
The development of reversibly binding radioligands for imaging brain proteins in vivo, such
as enzymes, neurotransmitter transporters, receptors and ion channels, with positron …

Phase 0/microdosing approaches: time for mainstream application in drug development?

T Burt, G Young, W Lee, H Kusuhara… - Nature Reviews Drug …, 2020 - nature.com
Phase 0 approaches—which include microdosing—evaluate subtherapeutic exposures of
new drugs in first-in-human studies known as exploratory clinical trials. Recent progress …

Unbound Brain-to-Plasma Partition Coefficient, Kp,uu,brain—a Game Changing Parameter for CNS Drug Discovery and Development

I Loryan, A Reichel, B Feng, C Bundgaard… - Pharmaceutical …, 2022 - Springer
Purpose More than 15 years have passed since the first description of the unbound brain-to-
plasma partition coefficient (Kp, uu, brain) by Prof. Margareta Hammarlund-Udenaes, which …

Comparative pharmacology of risperidone and paliperidone

M Corena-McLeod - Drugs in R&D, 2015 - Springer
Antipsychotics, risperidone, and risperidone's active metabolite, paliperidone (9-
hydroxyrisperidone), are related molecules used for the treatment of schizophrenia and …

Engineering extracellular vesicles for ROS scavenging and tissue regeneration

A Abdal Dayem, E Yan, M Do, Y Kim, Y Lee, SG Cho… - Nano …, 2024 - Springer
Stem cell therapy holds promise for tissue regeneration, yet significant challenges persist.
Emerging as a safer and potentially more effective alternative, extracellular vesicles (EVs) …

Canine and feline P‐glycoprotein deficiency: What we know and where we need to go

KL Mealey, JG Owens… - Journal of Veterinary …, 2023 - Wiley Online Library
In 2001 the molecular genetic basis of so‐called “ivermectin sensitivity” in herding breed
dogs was determined to be a P‐glycoprotein deficiency caused by a genetic variant of the …

Quantitative determination of luminal and abluminal membrane distributions of transporters in porcine brain capillaries by plasma membrane fractionation and …

Y Kubo, S Ohtsuki, Y Uchida, T Terasaki - Journal of pharmaceutical …, 2015 - Elsevier
Abluminal or luminal localization of transporter in plasma membranes at the blood–brain
barrier (BBB) is critical for their physiological and pharmacological roles. Therefore, the …

Targeted separation of antibacterial peptide from protein hydrolysate of anchovy cooking wastewater by equilibrium dialysis

W Tang, H Zhang, L Wang, H Qian, X Qi - Food Chemistry, 2015 - Elsevier
Anchovy (Engraulis japonicus) cooking wastewater (ACWW) is a by-product resulted from
the production of boiled–dried anchovies in the seafood processing industry. In this study …

Radioligand development for molecular imaging of the central nervous system with positron emission tomography

M Honer, L Gobbi, L Martarello, RA Comley - Drug Discovery Today, 2014 - Elsevier
Highlights•The development of radioligands for imaging of the brain with PET is
discussed.•The in vitro and preclinical evaluation of candidate radioligands is described.• …

A dialysis-based in vitro drug release assay to study dynamics of the drug-protein transfer of temoporfin liposomes

CM Wallenwein, MV Nova, C Janas, L Jablonka… - European Journal of …, 2019 - Elsevier
Today, a growing number of nanotherapeutics is utilized to deliver poorly soluble
compounds using the intravenous route of administration. The drug release and the direct …