Synthesis and Histamine H1 Receptor Agonist Activity of a Series of 2-Phenylhistamines, 2-Heteroarylhistamines, and Analogs

…, S Elz, M Garbarg, W Schunack

Index: Leschke, Christian; Elz, Sigurd; Garbarg, Monique; Schunack, Walter Journal of Medicinal Chemistry, 1995 , vol. 38, # 8 p. 1287 - 1294

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Citation Number: 72

Abstract

1H-imidazol-4-yllethanamine (39)) was significantly more potent than histamine (39: pD2= 6.81, relative activity= 128%). The 2-substituted histamine analogues were partial HI receptor agonists on the endothelium-denuded isolated guinea pig aorta with PECBO values generally smaller than observed on the guinea pig ileum, but the rank order of potency was found to be similar. The contractile effects on guinea pig ileum and aorta, ...