Results 11 to 20 of about 2,422 (193)

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

Frontiers in Cellular Neuroscience
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 barrier (BBB).
Frida Bällgren, Yang Hu, Shannuo Li, Lara van de Beek, Margareta Hammarlund-Udenaes, Irena Loryan   +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]

Pharmacology Research &Perspectives, Volume 9, Issue 5, October 2021., 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
Shuyao Wang, Chun Chen, Chi Guan, Liping Qiu, Lei Zhang, Shaofeng Zhang, Hongyu Zhou, Hongwen Du, Chen Li, Yaqiong Wu, Hang Chang, Tao Wang   +11 more
wiley   +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 CNS
Background 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, Alberte Bay Villekjær Pedersen, Anne Rodenberg, Burak Ozgür, Lasse Saaby, Christoffer Bundgaard, Mie Kristensen, Peer Tfelt-Hansen, Birger Brodin   +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, Indyra Alencar Duarte Figueiredo, Filipe Rodolfo Moreira Borges de Oliveira, Sarah Rebeca Dantas Ferreira, Giulyane Targino Aires Moreno, Tania Maria Sarmento da Silva, Ulisses dos Santos Pinheiro, Barbara Viviana de Oliveira Santos, Barbara Viviana de Oliveira Santos, Bagnólia Araújo da Silva, Bagnólia Araújo da Silva, Fabiana de Andrade Cavalcante, Fabiana de Andrade Cavalcante   +12 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 CNS
Background 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, Nana Svane, Aghavni Ginosyan, Alberte Bay Villekjaer Pedersen, Shannuo Li, Jessica Mahajan, Morten Schallburg Nielsen, Birger Brodin, Irena Loryan   +8 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 Testing and Analysis, Volume 17, Issue 8, Page 1283-1293, August 2025.
The 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.
Simon D. Brandt, Pierce V. Kavanagh, Sarah Gare, Simon P. Elliott, Alexander Stratford, Adam L. Halberstadt   +5 more
wiley   +2 more sources

Association of Inpatient Prescribing of First‐Generation Antihistamines With Delirium in Older Adults: A Cross‐Sectional Study [PDF]

Journal of the American Geriatrics Society, Volume 73, Issue 11, Page 3475-3483, November 2025.
ABSTRACT Background Small studies have reported associations between first‐generation antihistamines and delirium. It is unclear whether first‐generation antihistamines cause clinically important delirium among older adult inpatients. Objective To estimate the association between inpatient physician prescribing of first‐generation antihistamines and ...
Alanna C. Bridgman, Mohammad Arshad Imrit, Surain B. Roberts, Mina Tadrous, Nathan M. Stall, Michael Fralick, Jennifer Watt, Amol A. Verma, Fahad Razak, Aaron M. Drucker   +9 more
wiley   +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]

Pharmaceutics
Background: 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, Lijun Luo, Ziqian Zhang, Xiao Liu, Naihong Chen, Yan Li, Li Sheng   +6 more
doaj   +2 more sources

Pyrilamine in the horse: detection and pharmacokinetics of pyrilamine and its major urinary metaboliteO‐desmethylpyrilamine [PDF]

Journal of Veterinary Pharmacology and Therapeutics, 2009
Pyrilamine is an antihistamine used in human and veterinary medicine. As antihistamines produce central nervous system effects in horses, pyrilamine has the potential to affect the performance of racehorses. In the present study,O‐desmethylpyrilamine (O‐DMP) was observed to be the predominant equine urinary metabolite of pyrilamine.
L, Dirikolu, A F, Lehner, J D, Harkins, W E, Woods, W, Karpiesiuk, R S, Gates, M, Fisher, T, Tobin   +7 more
openaire   +2 more sources

The widely used antihistamine mepyramine causes topical pain relief through direct blockade of nociceptor sodium channels

The FASEB Journal, Volume 35, Issue 12, December 2021., 2021
Abstract Mepyramine, a first‐generation antihistamine targeting the histamine H(1) receptor, was extensively prescribed to patients suffering from allergic reactions and urticaria. Serious adverse effects, especially in case of overdose, were frequently reported, including drowsiness, impaired thinking, convulsion, and coma.
Jizhe Hao, Lucie Brosse, Caroline Bonnet, Myriam Ducrocq, Françoise Padilla, Virginie Penalba, Angélique Desplat, Jérôme Ruel, Patrick Delmas   +8 more
wiley   +1 more source