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Cover Feature: Light‐Switchable Antagonists for the Histamine H 1 Receptor at the Isolated Guinea Pig Ileum (ChemMedChem 6/2019)
Author(s) -
Rustler Karin,
Pockes Steffen,
König Burkhard
Publication year - 2019
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201900136
Subject(s) - photochromism , histamine , ileum , chemistry , guinea pig , azobenzene , antagonist , stereochemistry , receptor , biophysics , biochemistry , photochemistry , pharmacology , biology , molecule , organic chemistry , endocrinology
The Cover Feature shows the organ‐pharmacological investigation of photochromic azobenzene‐based antagonists at the native G‐protein‐coupled histamine H 1 receptor (H 1 R) expressed in smooth muscles of the guinea pig ileum. The molecular structure of the most active azobenzene‐based photochromic antagonist is highlighted in its two isomeric states, which can be interconverted from trans to cis via irradiation with blue light and back isomerized by thermal relaxation resulting in a difference in antagonistic activity of factor 46. The silhouette in the background displays the organ bath for the isolated ileum assay under constant irradiation with blue light using a water‐cooled photoreactor. More information can be found in the Full Paper by Karin Rustler, Steffen Pockes, and Burkhard König on page 636 in Issue 6, 2019 (DOI: 10.1002/cmdc.201800815).