The localization and characterization of bradykinin B-2 receptors in s
heep uterus was carried out using a radiolabelled B-2 receptor ligand,
Arg(0)-[Hyp(3),Thi(5),D-Tic(7),D-OiC(8)]bradykinin (HPP-HOE140). Comp
etition of the radioligand, [I-125]HPP-HOE140, from membrane preparati
ons of anoestrus sheep uterus by bradykinin agonists and antagonists r
evealed the presence of high- and low-affinity binding sites with liga
nd specificity typical of the bradykinin B-2 receptor. Using in vitro
autoradiography on tissue sections, intense binding was visible over t
he superficial epithelial layer of the endometrium and inner third of
the myometrium of anoestrus sheep uterus. Bradykinin Bz receptors in t
he myometrium were down regulated in pregnant sheep uterus. We demonst
rate that binding studies using [I-125]HPP-HOE140 offer high sensitivi
ty and specificity for characterization, quantitation and localization
of the bradykinin B-2 receptors in tissues and offers new information
on uterine bradykinin B-2 receptors.