We compared the antihistamine effect of four new antihistamines with olopatadine, which is used to treat equine allergic diseases. Six healthy Thoroughbred horses received oral doses of olopatadine (50 mg), levocetirizine (50 mg), bilastine (200 mg), rupatadine (100 mg), and desloratadine (50 mg) at >2-week intervals. The effects were investigated by measurement of the wheal area induced by histamine intradermal injection, and inhibition rate was compared with positive and negative controls. The maximum wheal inhibition rate (mean ± SD) of olopatadine (85.3% ± 7.7%) was significantly higher than those of bilastine (51.1% ± 11.8%), rupatadine (55.3% ± 6.6%), and desloratadine (59.8% ± 6.4%), but not levocetirizine (85.4% ± 8.0%). Levocetirizine is expected to have a high antihistamine effect on horses.
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http://dx.doi.org/10.1292/jvms.24-0412 | DOI Listing |
J Vet Med Sci
January 2025
Equine Research Institute, Japan Racing Association.
We compared the antihistamine effect of four new antihistamines with olopatadine, which is used to treat equine allergic diseases. Six healthy Thoroughbred horses received oral doses of olopatadine (50 mg), levocetirizine (50 mg), bilastine (200 mg), rupatadine (100 mg), and desloratadine (50 mg) at >2-week intervals. The effects were investigated by measurement of the wheal area induced by histamine intradermal injection, and inhibition rate was compared with positive and negative controls.
View Article and Find Full Text PDFJ Med Chem
January 2025
Amsterdam Institute of Molecular and Life Sciences (AIMMS), Division of Medicinal Chemistry, Faculty of Science, Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ Amsterdam, The Netherlands.
Analysis of structure-kinetic relationships (SKR) can contribute to an improved understanding of receptor-ligand interactions. Here, fragment (4-(2-benzylphenoxy)-1-methylpiperidine) was used in different fragment growing approaches to mimic the putative binding mode of the long residence time (RT) ligands olopatadine, acrivastine, and levocetirizine at the histamine H receptor (HR). SKR analyses reveal that introduction of a carboxylic acid moiety can increase RT at HR up to 11-fold.
View Article and Find Full Text PDFSpectrochim Acta A Mol Biomol Spectrosc
February 2025
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sinai University -Kantara branch, Ismailia 341636, Egypt. Electronic address:
The development of analytical methods that adhere to the principles of sustainable green chemistry is essential in the modern scientific arena. This research presents two novel methods for the concurrent quantification of olopatadine (OLO) and mometasone (MOM), targeting sustainable green chemistry principles in their raw materials, dosage forms and combined nasal spray formulations. The first method is a rapid isocratic high-performance liquid chromatography (HPLC) that achieves excellent resolution within 4 min, with retention times of 2.
View Article and Find Full Text PDFADMET DMPK
August 2024
Molecular Pharmaceutics Lab., College of Pharmaceutical Sciences, Ritsumeikan University, 1-1-1, Noji-higashi, Kusatsu, Shiga 525-8577, Japan.
Background And Purpose: The food effects on oral drug absorption are challenging to predict from in vitro data. Food intake has been reported to reduce the oral absorption of several zwitterionic antihistamine drugs. However, the mechanism for this negative food effect has not been clear.
View Article and Find Full Text PDFAAPS PharmSciTech
September 2024
Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, P. R. China.
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