Histamine receptors: specific ligands, receptor biochemistry, and signal transduction.
During the past few years, there has been a tremendous increase in our understanding of the histamine receptors. Important progress has been made in the development of H1-receptor agonists and the rationalization of H1-receptor-ligand interaction. The recent observation of constitutive H1- and H2-receptor activity has led to a reclassification of H1- and H2-antagonists. For the H3-receptor, a wide variety of selective and potent ligands are currently available and await clinical application. The recent cloning of the H3-receptor gene and the anticipated generation of transgenic mice will facilitate this development. Within the field of signal transduction, a previously unanticipated complexity has been unravelled. With the cloning of the H3-receptor gene, a similar complexity is to be expected.
Vrije Universiteit, Amsterdam, The Netherlands.
Remko A
RA
Bakker
Hendrik
H
Timmerman
Rob
R
Leurs
D000818:Animals; D016718:Arachidonic Acid / Q000378:metabolism; D020013:Calcium Signaling; D019204:GTP-Binding Proteins / Q000502:physiology; D006801:Humans; D008958:Models, Molecular; D019001:Nitric Oxide Synthase / Q000378:metabolism; D011968:Receptors, Histamine / Q000737:chemistry / Q000235:genetics / Q000502:physiology*; D015398:Signal Transduction; D010738:Type C Phospholipases / Q000378:metabolism
D011968:Receptors, Histamine; D016718:Arachidonic Acid; D019001:Nitric Oxide Synthase; D010738:Type C Phospholipases; D019204:GTP-Binding Proteins