Region-independent active CNS net uptake of marketed H+/OC antiporter system substrates [PDF]
Frontiers in Cellular NeuroscienceThe 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 barrier (BBB).
Frida Bällgren +5 more
doaj +2 more sources
Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats. [PDF]
Pharmacol Res Perspect, 2021 Unbound concentrations of of 14 commercial drugs in rat liver, muscle, and blood Abstract The unbound concentrations of 14 commercial drugs, including five non‐efflux/uptake transporter substrates—Class I, five efflux transporter substrates—class II and four influx transporter substrates—Class III, were simultaneously measured in rat liver, muscle, and
Wang S +11 more
europepmc +2 more sources
The putative proton-coupled organic cation antiporter is involved in uptake of triptans into human brain capillary endothelial cells [PDF]
Fluids and Barriers of the CNSBackground Triptans are anti-migraine drugs with a potential central site of action. However, it is not known to what extent triptans cross the blood–brain barrier (BBB).
Nana Svane +8 more
doaj +2 more sources
Positive chronotropic action of HCN channel antagonism in human collecting lymphatic vessels. [PDF]
Physiol Rep, 2022 Hyperpolarisation‐activated cyclic‐nucleotide gated (HCN) channels primarily determine sinoatrial pacemaking. In human lymphatic vessels HCN channel proteins are also expressed but have a negligible functional role in ex vivo phasic activity when investigated using the HCN inhibitors ivabradine, ZD7288 and caesium.
Majgaard J +4 more
europepmc +2 more sources
Spectrophotometric Methods for the Assay of Pyrilamine Maleate Using Chromogenic Reagents [PDF]
E-Journal of Chemistry, 2010 Simple, accurate and reproducible UV spectrophotometric methods were established for the assay of pyrilamine maleate (PYRA) based on the formation of oxidative coupling and precipitation, charge transfer complexation products.
V. Annapurna +3 more
doaj +2 more sources
Comparative analysis of the uptake of the H+/OC antiporter substrate oxycodone across and into brain endothelial and parenchymal cells with in vitro–in vivo extrapolation [PDF]
Fluids and Barriers of the CNSBackground In vitro evaluation of substances utilizing the putative proton‑coupled organic cation (H+/OC) antiporter for active uptake across the blood-brain barrier (BBB) and brain cell membranes requires a thorough understanding of cellular ...
Frida Bällgren +8 more
doaj +2 more sources
Oceanapia magna Sponge Presents Dual Effect on the Gastrointestinal Motility of Rodents: In Vitro and In Vivo Assays [PDF]
Frontiers in Pharmacology, 2020 Oceanapia magna Santos-Neto, Nascimento, Cavalcanti and Pinheiro sponges are distributed across tropical worldwide seas. Some studies of marine products have shown interesting activities in smooth muscle models.
Joedna Cavalcante Pereira +12 more
doaj +2 more sources
Analytical and Pharmacological Characterization of 1-(Furan-2-Carbonyl)-LSD (1F-LSD) and Comparison With 1-(Thiophene-2-Carbonyl)-LSD (1T-LSD). [PDF]
Drug Test AnalThe novel lysergamide 1‐(furan‐2‐carbonyl)‐LSD (1F‐LSD) was analytically characterized. 1F‐LSD showed LSD‐like activity in vivo similar to 1‐(thiophene‐2‐carbonyl)‐LSD (1T‐LSD) used for comparison. Administration studies in mice and LC–MS analysis revealed that 1F‐LSD served as a prodrug.
Brandt SD +5 more
europepmc +2 more sources
The Active Glucuronide Metabolite of the Brain Protectant IMM-H004 with Poor Blood–Brain Barrier Permeability Demonstrates a High Partition in the Rat Brain via Multiple Mechanisms [PDF]
PharmaceuticsBackground: Glucuronidation is an essential metabolic pathway for a variety of drugs. IMM-H004 is a novel neuroprotective agent against ischemic stroke, and its glucuronide metabolite IMM-H004G exhibits similar pharmacological activity.
Jianwei Jiang +6 more
doaj +2 more sources
The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors
British Journal of Pharmacology, Volume 180, Issue S2, Page S23-S144, October 2023., 2023 The Concise Guide to PHARMACOLOGY 2023/24 is the sixth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of approximately 1800 drug targets, and about 6000 interactions with about 3900 ligands.
Stephen P. H. Alexander +165 more
wiley +1 more source