Pharmacological characterization of bradykinin receptors in canine cultured tracheal smooth muscle cells

Abstract

receptor selective reagents. The up-regulation of the B2 receptor by forskolin was mediated through protein synthesis, since cycloheximide blocked this response. 7 It is concluded that the pharmacological characteristics of the bradykinin receptors in canine cultured TSMCs are primarily of the B2 receptor subtype.

Pharmacological and functional characterization of bradykinin receptors in canine cultured tracheal epithelial cells

“…In this study, the B1 receptor-selective antagonist, [Leu8, des-Arg9]-BK and agonist, des-Arg9-BK, gave no displacement at concentrations up to 10 gM, excluding the presence of B1 receptors in canine cultured TECs. The binding characteristics are similar to those of the BK receptors described for guinea-pig lung and trachea, canine and human tracheal smooth muscle cells, and rat myometrium (Farmer et al, 1989;Liebmann et al, 1991;Trifilieff et al, 1991;Yang et al, 1995 (Hock et al, 1991). The binding affinities for Hoe 140 and [D-Arg', Hyp3, Thi5'8, D-Phe7]-BK were 2.8 + 0.6 and 83.4 + 13.9 nM, respectively, corresponding to the high affinity for B2 receptors described in other tissues (Trifilieff et al, 1991;Eggerickx et al, 1992;Hess et al, 1994;Yang et al, 1995).…”

“…The pharmacological properties of the BK receptors are quite consistent with those of the B2 receptors (Farmer et al, 1989;Liebmann et al, 1991;Trifilieff et al, 1991;Yang et al, 1995). (Hock et al, 1991;Eggerickx et al, 1992;Marsh & Hill, 1992;Yang et al, 1994a).…”

“…[31H]-BK has been shown to label BK receptors in guinea-pig lung and trachea, human and canine tracheal smooth muscle cells, and rat myometrium (Farmer et al, 1989;Liebmann et al, 1991;Trifilieff et al, 1991;Yang et al, 1995 (Regoli et al, 1990). BK and kallidin have a high affinity for B2 receptors and a low affinity for B1 receptors (Regoli et al, 1990).…”

“…We have previously reported that BK induces an increase in phosphoinositide (PI) hydrolysis and a rise in intracellular Ca2+ ([Ca2 +],) in canine cultured tracheal smooth muscle cells which appears to be mediated via activation of the B2 receptors (Yang et al, 1994a,b). The existence of B2 receptor subtype in tracheal smooth muscle cells was further confirmed by a direct binding assay (Yang et al, 1995). However, there is no information on the distribution of BK receptor subtypes in canine tracheal epithelial cells (TECs).…”

“…On the basis of the relative potencies of these three agonists, preparations with higher affinity for BK than for des-Arg9-BK are considered to express B2 receptor activity, while preparations having opposite affinity are considered to express B, receptor activity (Proud & Kaplan, 1988; ' Author for correspondence. Regoli et al, 1990;Yang et al, 1995). The use of B2-selective antagonists has further strengthened the existence of such a receptor subtype (Regoli et al, 1990).…”