Comparative tolerability of dopamine D2/3 receptor partial agonists for schizophrenia

N Keks, J Hope, D Schwartz, H McLennan, D Copolov… - CNS drugs, 2020 - Springer
Aripiprazole, brexpiprazole and cariprazine differ from all other second-generation
antipsychotics due to partial agonism at the dopamine D2 and D3 receptors. In contrast to …

[HTML][HTML] Quantitative prediction of pharmacokinetic properties of drugs in humans: Recent advance in in vitro models to predict the impact of efflux transporters in the …

Y Hashimoto, K Michiba, K Maeda… - Journal of Pharmacological …, 2022 - Elsevier
Efflux transport systems are essential to suppress the absorption of xenobiotics from the
intestinal lumen and protect the critical tissues at the blood-tissue barriers, such as the blood …

Brain histamine H1 receptor occupancy after oral administration of desloratadine and loratadine

T Nakamura, K Hiraoka, R Harada… - Pharmacology …, 2019 - Wiley Online Library
Some histamine H1 receptor (H1R) antagonists induce adverse sedative reactions caused
by blockade of histamine transmission in the brain. Desloratadine is a second‐generation …

Involvement of proton-coupled organic cation antiporter in varenicline transport at blood-brain barrier of rats and in human brain capillary endothelial cells

T Kurosawa, K Higuchi, T Okura, K Kobayashi… - Journal of …, 2017 - Elsevier
Varenicline is a selective partial α 4 β 2 nicotinic acetylcholine receptor agonist, which is
used to help achieve smoking cessation. Here, we investigated varenicline transport at the …

Analyzing the clinical efficacy and safety of levocetirizine based on its receptor occupancy, intraclass comparison and role in the treatment of CSU: an AROG …

K Sardana, C Srinivasan, M Girdhar… - Expert Review of …, 2024 - Taylor & Francis
Introduction Chronic spontaneous urticaria (CSU) is characterized by urticaria persisting for
more than 6 weeks and leading to significant morbidity. Antihistamines, especially sgAH …

The antagonistic activity of H1 receptor antagonists as medicinal foods

S Zhou, G Huang, G Chen - Trends in Food Science & Technology, 2020 - Elsevier
At present, there are many kinds of H 1 receptor antagonists as medicinal foods in clinical
application, which can be divided into ethylenediamine antagonist, aminoether antagonist …

[HTML][HTML] The Efficacy of Bepotastine Besilate Compared With Hydroxyzine Pamoate for Preventing Infusion Reactions to the First Dose of Rituximab in Patients With …

Y Kitahiro, K Yamamoto, K Yakushijin… - JMIR Research …, 2024 - researchprotocols.org
Background Rituximab, an anti-CD20 monoclonal antibody, can cause infusion reactions
(IRs), especially during the initial rituximab infusion therapy. Generally, patients are …

Molecular Determinants of the Kinetic Binding Properties of Antihistamines at the Histamine H1 Receptors

H Akimoto, Y Uesawa, S Hishinuma - International Journal of Molecular …, 2021 - mdpi.com
The binding affinity of ligands for their receptors is determined by their kinetic and
thermodynamic binding properties. Kinetic analyses of the rate constants of association and …

3. 創薬現場における薬物の中枢移行性評価

小澤誠 - 谷本学校毒性質問箱, 2022 - jstage.jst.go.jp
抄録 血液と脳組織との間には脳毛細血管内皮細胞 (brain microvascular endothelial cell:
BMEC) を実体とする血液脳関門 (blood brain barrier: BBB) が存在し, 血液と脳組織の間で行 …