Imidazoline recognition sites and stomach function.
Radioligand binding experiments carried out in cell membranes from rat and human stomach revealed the existence of non-adrenoceptor [3H]clonidine and [3H]idazoxan binding sites and of [3H]DTG (1,2-di-(2-tolyl)guanidine) binding sites. In rat stomach, specific binding was inhibited by imidazolines and guanidines and by non-imidazoline sigma-site ligands, respectively, at different rank orders of affinity, suggesting the existence of non-I1/non-I2 [3H]clonidine binding sites, I2-imidazoline binding sites as well as sigma 2-like-sites. These sites are not directly related to a postsynaptic contractile effect on rat gastric smooth muscle or to acid release from isolated gastric glands. Finally, we demonstrated that the gastric pathogen Helicobacter pylori is able to form and to release the endogenous imidazoline receptor ligand agmatine and that considerable amounts of agmatine are present in human gastric juice. The quantities of agmatine were higher in gastric juice from H. pylori-positive than H. pylori-negative patients.
Molderings
G J
GJ
Institute of Pharmacology and Toxicology, University of Bonn, Germany. molderings@ibm.rhrz.uni-bonn.de
Burian
M
M
Menzel
S
S
Donecker
K
K
Homann
J
J
Nilius
M
M
Göthert
M
M
D000818:Animals; D001665:Binding Sites; D005744:Gastric Acid / Q000378:metabolism; D005753:Gastric Mucosa / Q000187:drug effects / Q000502:physiology*; D016481:Helicobacter Infections / Q000503:physiopathology; D016480:Helicobacter pylori; D006801:Humans; D007093:Imidazoles / Q000493:pharmacokinetics / Q000494:pharmacology*; D054755:Imidazoline Receptors; D051381:Rats; D011955:Receptors, Drug / Q000502:physiology*; D013270:Stomach / Q000187:drug effects / Q000502:physiology*
D007093:Imidazoles; D054755:Imidazoline Receptors; D011955:Receptors, Drug