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

Luo, Shue Fen; Tsai, Chuen Tao; Wu, Wen Bin; Pan, Shiow Lin; Tsai, Yih Jeng; Yang, Che‐Hua

doi:10.1111/j.1476-5381.1996.tb16005.x

Cited by 8 publications

(16 citation statements)

References 35 publications

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“…2). The pharmacological properties of the BK receptors are consistent with those of B 2 receptors [8,17,18,32,33,37,38].…”

Section: Pharmacological Specificity Of [ 3 H]-bk Bindingsupporting

confidence: 54%

“…These results indicate that the receptors mediating the BK-induced [Ca 2+ ] i increase in CECs had similar pharmacological properties to those of kinin B 2 receptors [18,22,23,29,[36][37][38].…”

Section: Effects Of B 2 Receptor Antagonists On Bk-induced Ip Accumulsupporting

confidence: 53%

“…Several lines of evidence have demonstrated the presence of BK receptors in various tissues [18,32,33,37,38]. Both B 1 and B 2 are seven-transmembrane receptors coupled to G proteins; the transduction mechanism of these receptors is the stimulation of PI hydrolysis by PLC.…”

Section: Discussionmentioning

confidence: 99%

“…On the basis of the relative potencies of these three agonists, preparations with a higher affinity for BK than for des-Arg 9 -BK are considered to express B 2 receptor activity, while preparations having the opposite affinity are considered to express B 1 receptor activity [18,25,27,37,38]. The use of B 2 -selective antagonists has further strengthened the idea of the existence of such a receptor subtype [27].…”

Section: Introductionmentioning

confidence: 99%

“…In many cell types, including the human astrocytoma cell line D384 [2], bovine [21] and canine [35] tracheal smooth muscle cells, canine tracheal epithelial cells [18] and rat vascular smooth muscle cells [38], BK receptors activate phospholipase C (PLC)-mediated phosphoinositide (PI) hydrolysis in the plasma membrane. Subsequently, the resultant inositol 1,4,5-trisphosphate releases Ca 2+ from its intracellular stores [22,23,29,36,38].…”

Section: Introductionmentioning

confidence: 99%

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Characterization of Bradykinin Receptors in Canine Cultured Corneal Epithelial Cells: Pharmacological and Functional Studies

et al. 2002

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The pharmacological properties of bradykinin (BK) receptors were characterized in canine cultured corneal epithelial cells (CECs) using [³H]-BK as a radioligand. Analysis of binding isotherms gave an apparent equilibrium dissociation constant of 0.34 ± 0.07 nM and a maximum receptor density of 179 ± 23 fmol/mg protein. Neither a B₁ receptor-selective agonist (des-Arg⁹-BK) nor antagonist ([Leu⁸, des-Arg⁹]-BK) significantly inhibited [³H]-BK binding to CECs, thus excluding the presence of B₁ receptors in canine CECs. The specific binding of [³H]-BK to CECs was inhibited by B₂ receptor-selective agonists (BK and kallidin) and antagonists (Hoe 140 and [D-Arg⁰, Hyp³, Thi^5,8, D-Phe⁷]-BK), with a best fit using a one-binding-site model. The order of potency for the inhibition of [³H]-BK binding was BK = Hoe 140 > kallidin > [D-Arg⁰, Hyp³, Thi^5,8, D-Phe⁷]-BK. Stimulation of CECs by BK produced a concentration-dependent accumulation of inositol phosphates (IP) and an initial transient peak of intracellular Ca²⁺. B₂ receptor-selective antagonist ([D-Arg⁰, Hyp³, Thi^5,8, D-Phe⁷]-BK) significantly antagonized the BK-induced responses with dissociation constants of 6.0–6.1. Pretreatment of CECs with pertussis toxin (PTX) or cholera toxin did not alter the BK-induced IP accumulation. Incubation of CECs in the absence of external Ca²⁺ led to a significant attenuation of the IP accumulation induced by BK. These results demonstrate that BK directly stimulates phospholipase C-mediated signal transduction through BK B₂ receptors via a PTX-insensitive G protein in canine CECs. This effect may function as the transducing mechanism for BK-mediated cellular responses.

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“…2). The pharmacological properties of the BK receptors are consistent with those of B 2 receptors [8,17,18,32,33,37,38].…”

Section: Pharmacological Specificity Of [ 3 H]-bk Bindingsupporting

confidence: 54%

Section: Effects Of B 2 Receptor Antagonists On Bk-induced Ip Accumulsupporting

confidence: 53%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Characterization of Bradykinin Receptors in Canine Cultured Corneal Epithelial Cells: Pharmacological and Functional Studies

et al. 2002

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Characterization of bradykinin receptors in canine cultured corneal epithelial cells: Pharmacological and functional studies

et al. 2002

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The pharmacological properties of bradykinin (BK) receptors were characterized in canine cultured corneal epithelial cells (CECs) using [(3)H]-BK as a radioligand. Analysis of binding isotherms gave an apparent equilibrium dissociation constant of 0.34 +/- 0.07 nM and a maximum receptor density of 179 +/- 23 fmol/mg protein. Neither a B(1) receptor-selective agonist (des-Arg(9)-BK) nor antagonist ([Leu(8), des-Arg(9)]-BK) significantly inhibited [(3)H]-BK binding to CECs, thus excluding the presence of B(1) receptors in canine CECs. The specific binding of [(3)H]-BK to CECs was inhibited by B(2) receptor-selective agonists (BK and kallidin) and antagonists (Hoe 140 and [D-Arg(0), Hyp(3), Thi(5,8), D-Phe(7)]-BK), with a best fit using a one-binding-site model. The order of potency for the inhibition of [(3)H]-BK binding was BK = Hoe 140 > kallidin > [D-Arg(0), Hyp(3), Thi(5,8), D-Phe(7)]-BK. Stimulation of CECs by BK produced a concentration-dependent accumulation of inositol phosphates (IP) and an initial transient peak of intracellular Ca(2+). B(2) receptor-selective antagonist ([D-Arg(0), Hyp(3), Thi(5,8), D-Phe(7)]-BK) significantly antagonized the BK-induced responses with dissociation constants of 6.0-6.1. Pretreatment of CECs with pertussis toxin (PTX) or cholera toxin did not alter the BK-induced IP accumulation. Incubation of CECs in the absence of external Ca(2+) led to a significant attenuation of the IP accumulation induced by BK. These results demonstrate that BK directly stimulates phospholipase C-mediated signal transduction through BK B(2) receptors via a PTX-insensitive G protein in canine CECs. This effect may function as the transducing mechanism for BK-mediated cellular responses.

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Mechanisms of bradykinin-mediated Ca2+ signalling in canine cultured corneal epithelial cells

Huang

Chien

Hsiao

et al. 2001

Cellular Signalling

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

Cited by 8 publications

References 35 publications

Characterization of Bradykinin Receptors in Canine Cultured Corneal Epithelial Cells: Pharmacological and Functional Studies

Characterization of Bradykinin Receptors in Canine Cultured Corneal Epithelial Cells: Pharmacological and Functional Studies

Characterization of bradykinin receptors in canine cultured corneal epithelial cells: Pharmacological and functional studies

Mechanisms of bradykinin-mediated Ca2+ signalling in canine cultured corneal epithelial cells

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