Chemical differentiation of histamine H1-and H2-receptor agonists

GJ Durant, CR Ganellin…

Index: Durant,G.J. et al. Journal of Medicinal Chemistry, 1975 , vol. 18, p. 905 - 909

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Citation Number: 294

Abstract

Histamine exists predominantly as the NT-H tautomer of the monocation (IIa) at a physiological pH of 7.4 and structure-activity studies indicate that this tautomer is likely to be the pharmacologically active species for both HI and HP receptors. Effective Hz-receptor agonists appear to require a prototropic tautomeric system whereas HI-receptor agonists do not need to be tautomeric. This identifies a chemical difference in the receptor ...