Related Experiment Video
Updated: Jun 16, 2026

Basophil Activation Test for Allergy Diagnosis
Published on: May 31, 2021
Acidic elements in histamine H(3) receptor antagonists
Kerstin Sander1, Yvonne von Coburg, Jean-Claude Camelin
1Johann Wolfgang Goethe University, Institute of Pharmaceutical Chemistry, ZAFES/LiFF/CMP, Max-von-Laue-Str. 9, 60438 Frankfurt/Main, Germany.
Abstract:
Antagonists of the human histamine H(3) receptor (hH(3)R) often contain a second basic moiety, which is well known to boost affinity on this histamine receptor subtype. Here, we prepared compounds with acidic moieties of different pK(a) values to figure out that the hH(3)R tolerates these functionalities when added to a common pharmacophore blueprint. Depending on the acidic, electronic and steric features the designed ligands showed hH(3)R affinities in the nanomolar concentration range. Additionally, selected ligands were tested but failed as dual acting hH(3)R/hPPAR (human peroxisome proliferator-activated receptor) ligands.
Related Concept Videos
Acid Suppressive Drugs for Peptic Ulcer Disease: Histamine H2-Receptor Antagonists
Cholinergic Antagonists: Chemistry and Structure-Activity Relationship
Basicity of Heterocyclic Aromatic Amines
Upper Respiratory Drugs: First and Second-Generation Antihistamines
Histamine binds to specific receptor sites, known as H1 receptors, on tissue cells, triggering inflammation and swelling. Antihistamines combat these effects by competing with histamine for these receptor sites. By...
Acid Suppressive Drugs for Peptic Ulcer Disease: Proton Pump Inhibitors
Gastric acid, a potent cocktail of hydrogen and chloride ions, is produced in specialized parietal cells within the...
Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers
Nonselective α-blockers: Nonselective α-blockers contain haloalkylamine or imidazoline moieties. Phenoxybenzamine, with a haloalkylamine...

