This article reviews the development of our knowledge of the actions of histamine which
have taken place during the course of the 20th century. Histamine has been shown to have a …

A rational approach to the design of centrally acting agents is presented, based initially
upon a comparison of the physicochemical propertiesof three typical histamine H2 receptor …

Some G-protein-coupled receptors display ‘constitutive activity’, that is, spontaneous activity
in the absence of agonist 1 , 2 , 3 , 4 . This means that a proportion of the receptor …

The opening chapter summarizes various ways to modify the properties of a drug to make a
new drug analogue that improves patient drug therapy. There are 12 principles exemplified (…

To maintain Ca 2+ entry during T lymphocyte activation, a balancing efflux of cations is
necessary. Using three approaches, we demonstrate that this cation efflux is mediated by Ca 2+ -…

Histamine exists predominantly as the NT-H tautomer of the monocation (Ha) at a physiological
pH of 7.4 and struc-ture-activity studies indicate that this tautomer is likely to be the …

G protein-coupled receptors (GPCRs) are allosteric proteins that adopt inactive (R) and active
(R * ) conformations in equilibrium. R * is promoted by agonists or occurs spontaneously, …

A cholecystokinin (CCK)-inactivating peptidase was purified and identified as a membrane-bound
isoform of tripeptidyl peptidase II (EC 3.4.14.10), a cytosolic subtilisin-like peptidase of …

The reference compounds for histamine H 3 -receptor antagonists carry as a common feature
an imidazole moiety substituted in the 4-position. Very recently novel ligands lacking an …

Closely related structural analogues of prazosin have been synthesised and tested for
inhibition and activation of Transport-P in order to identify the structural features of the prazosin …