Avtor/Urednik     Čarman-Kržan, M
Naslov     Characterisation of histamine-H1 receptor binding sites in bovine, rat and guinea pig thoracic aorta
Tip     članek
Vir     Agents Actions
Vol. in št.     , št. Spec Issue
Leto izdaje     1992
Obseg     str. C406-9
Jezik     eng
Abstrakt     Radioligand binding studies elucidating the localization of vascular histaminergic-H1 receptors using 3H-mepyramine demonstrate that, in addition to histaminergic-H1 receptors associated with the vascular smooth muscle membranes of bovine thoracic aorta, these receptor binding sites are also present on the endothelial layer of bovine aorta. The receptor number in the vascular smooth muscle membranes was diminished when the aorta was rubbed of endothelium prior to the membrane preparation (Bmax=58.5 vs 53.7 fmol/mg protein). As shown in a further study, vascular smooth muscle histamine receptors are homogeneous (high affinity sites only - KD=3.11 nM), whereas high and low affinity sites exist in the endothelium (KD=2.19 nM and 32.0 nM respectively). There are species differences in the binding characteristics between bovine, rat and guinea pig vascular smooth muscle histaminergic-H1 receptors: bovine and guinea pig vascular histamine receptors are homogeneous (high affinity sites) whereas two affinity sites for 3H-mepyramine binding exist in the rat.
Deskriptorji     RECEPTORS, HISTAMINE H1
AORTA
RATS
GUINEA PIGS
CATTLE
RADIOLIGAND ASSAY
TRITIUM
PYRILAMINE