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Pharmacological profile of astemizole-derived compounds at the histamine H1 and H4 receptor - H1/H4 receptor selectivity

Wager, Eva, Wittmann, Hans-Joachim, Elz, Sigurd and Strasser, Andrea (2014) Pharmacological profile of astemizole-derived compounds at the histamine H1 and H4 receptor - H1/H4 receptor selectivity. Naunyn-Schmiedeberg's Archives of Pharmacology 387, pp. 235-250.

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Abstract

Astemizole, a H1R antagonist shows high affinity to the histamine H1 receptor but only a moderate affinity to the histamine H4 receptor. This study aims to modify the astemizole to keep high affinity to the histamine H1 receptor and to increase affinity to the histamine H4 receptor. Therefore, 13 astemizole-derived compounds and astemizole-JNJ7777120-derived hybrid compounds were synthesized and ...

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Item type:Article
Date:2014
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Identification Number:
ValueType
24241585PubMed ID
10.1007/s00210-013-0926-4DOI
Keywords:Histamine H1 receptor . Histamine H4 receptor . Astemizole . JNJ7777120 . DualH1R/H4R ligands . Molecular dynamics
Dewey Decimal Classification:600 Technology > 615 Pharmacy
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Item ID:29839
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