DesArg9D-Arg[Hyp3,Thi5,D-Tic7,Oic8]bradykinin (desArg10-[Hoe140]) is a bradykinin B1 receptor antagonist

Wirth, Klaus; Breipohl, Gerhard; Stechl, Jens; Knolle, Jochen; Henke, S.; Schölkens, Bernward A.

doi:10.1016/0014-2999(91)90824-a

Cited by 74 publications

(25 citation statements)

References 6 publications

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“…The affinity of [Leu8,des-Arg']-BK in these two preparations is lower than its affinity reported previously in the rabbit aorta (pA2 6.8; Regoli et al, 1978) and mesenteric artery (pA2 6.5; Churchill & Ward, 1986 (Regoli & Barab6, 1980;Butt et al, 1994a,b), and no complication in interpretation due to differences between species needs to be taken into account (see Hall, 1992;Hall et al, 1993). The novel B1 receptor antagonist [des-Arg'I-Hoel40 (Wirth et al, 1991) has a ten fold higher affinity than [Leu8,des-Argl-BK.…”

Section: Phosphatidylinositol Hydrolysis Measurementmentioning

confidence: 73%

Bradykinin B₁ receptors in the rabbit urinary bladder: induction of responses, smooth muscle contraction, and phosphatidylinositol hydrolysis

Butt

Dawson

Hall

1995

British J Pharmacology

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1 The aim of this study was to analyse the pharmacological characteristics, and second-messenger coupling-mechanisms, of bradykinin B1 receptors in an intact tissue, the rabbit urinary bladder; and to investigate the influence of inhibition of endogenous peptidases on kinin activities. 2 In preparations of rabbit mucosa-free urinary bladder, at 90 min after mounting of the preparations, bradykinin (1 nM-10 fM) evoked contractile responses. In contrast, the B1 receptor-selective agonist [des-Argl-BK (10 nM-10-JM) was only weakly active at this time. Contractile responses to [des-Argl-BK increased with time of tissue incubation in the organ bath, reaching a maximum after 3 h, when the pD2 estimates were 6.4 ± 0.3 for bradykinin, and 6.9 + 0.2 for [des-Arg9]-BK. [Leu8,des-Argj-BK inhibited responses to bradykinin under these conditions (n = 4). and B2 receptors, but does not require conversion by peptidases in order to activate B1 receptors. We demonstrate, for the first time, B. receptor-coupling to phosphatidylinositol hydrolysis in an intact tissue preparation.

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Section: Phosphatidylinositol Hydrolysis Measurementmentioning

confidence: 73%

Bradykinin B₁ receptors in the rabbit urinary bladder: induction of responses, smooth muscle contraction, and phosphatidylinositol hydrolysis

Butt

Dawson

Hall

1995

British J Pharmacology

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“…HPP‐des‐Arg 10 ‐Hoe 140 (3‐4 hydroxyphenyl‐propionyl‐desArg 9 ‐D‐Arg°‐[Hyp 3 , Thi 5 , D‐Tic 7 , Oic 8 ]‐bradykinin [BK]) and HPP‐Hoe 140 (3‐4 hydroxyphenyl‐propionyl‐D‐Arg°‐[Hyp 3 , Thi 5 , D‐Tic 7 , Oic 8 ]‐BK) were developed from the selective B 1 receptor antagonist desArg 10 ‐Hoe 140 (Wirth et al, 1991) and the B 2 receptor antagonist Hoe 140 or Icatibant (Hock et al, 1991), respectively. They were synthesized in the laboratory of D. Regoli (Department of Pharmacology, Université de Sherbrooke, Canada).…”

Section: Methodsmentioning

confidence: 99%

Influence of γ‐irradiation on poly(methyl methacrylate)

Suarez

Mano

Monteiro

et al. 2002

J of Applied Polymer Sci

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Poly(methyl methacrylate) (PMMA) was ␥-irradiated (5-20 kGy) by a 137 Cs source at room temperature in air. The changes in the molecular structure attributed to ␥-irradiation were studied by mechanical testing (flexure and hardness), size-exclusion chromatography, differential scanning calorimetry, thermal gravimetric analysis, and both Fourier transform infrared and solution 13 C-NMR spectroscopy. Scanning electron microscopy was used to investigate the influence of the dose of ␥ rays on the fracture behavior of PMMA. The experimental results confirm that the PMMA degradation process involves chain scission. It was also observed that PMMA presents a brittle fracture mechanism and modifications in the color, becoming yellowish. The mechanical property curves show a similar pattern when the ␥-radiation dose increases.

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“…It has been proposed that BK receptor classification should be extended to include B 3 subtypes (Farmer et al 1989a,b, Hall 1997 as the presence of B 3 receptors has been demonstrated in guinea-pig trachea and taenia caeci (Field et al 1992a,b). BK is a potent B 2 receptor agonist (Regoli & Barabé 1980, Hall 1992) with HOE-140 being a potent and selective B 2 receptor antagonist (Wirth et al 1991a,b, Hock et al 1991. Des-Arg 9 -BK is a potent B 1 receptor agonist (Regoli & Barabé 1980, Hall 1992 with des-Arg 9 (leu 8 )BK reported to be a selective B 1 receptor antagonist (Churchill & Ward 1986, Field et al 1992a, Hall 1992, Campos & Calixto 1994, Drummond & Cocks 1995.…”

Section: Introductionmentioning

confidence: 99%

Characterisation of kinin receptors on the human isolated umbilical artery

Abbas

Clayton²,

Marshall³

et al. 1998

Journal of Endocrinology

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The aim of this study was to determine the kinin responses on human umbilical artery (HUA) and to characterise the kinin receptors present on this tissue. The HUA was found to constrict in response to both the B 2 receptor agonist, bradykinin (BK), and the B 1 receptor agonist, des-Arg 9 -BK. The presence of indomethacin (2·79 µM) was found to have no significant effect on the responses to BK and des-Arg 9 -BK. The presence of the B 2 receptor antagonist, HOE-140 (+2·79 µM indomethacin), resulted in a concentration-related rightward displacement of the concentration-effect curves to BK. The antagonism of the constrictor responses to BK by HOE-140 was found to be competitive (pA 2 =7·5). The responses to BK were not significantly affected by the B 1 receptor antagonist des-Arg 9 (leu 8 )BK. The presence of des-Arg 9 (leu 8 )BK (+2·79 µM indomethacin) resulted in a concentrationrelated rightward displacement of the concentration-effect curve to des-Arg 9 -BK. The antagonism of the response to des-Arg 9 -BK by des-Arg 9 (leu 8 )BK was found to be competitive (pA 2 =5·9). The responses to des-Arg 9 -BK were not significantly affected by HOE-140. The results of the present study suggest that the products of the cyclooxygenase pathway are not involved in the kinin constrictor response on HUA and indicate the presence of B 1 and B 2 receptors on this tissue.

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DesArg9D-Arg[Hyp3,Thi5,D-Tic7,Oic8]bradykinin (desArg10-[Hoe140]) is a bradykinin B1 receptor antagonist

Cited by 74 publications

References 6 publications

Bradykinin B₁ receptors in the rabbit urinary bladder: induction of responses, smooth muscle contraction, and phosphatidylinositol hydrolysis

Bradykinin B₁ receptors in the rabbit urinary bladder: induction of responses, smooth muscle contraction, and phosphatidylinositol hydrolysis

Influence of γ‐irradiation on poly(methyl methacrylate)

Characterisation of kinin receptors on the human isolated umbilical artery

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DesArg9D-Arg[Hyp3,Thi5,D-Tic7,Oic8]bradykinin (desArg10-[Hoe140]) is a bradykinin B1 receptor antagonist

Cited by 74 publications

References 6 publications

Bradykinin B1 receptors in the rabbit urinary bladder: induction of responses, smooth muscle contraction, and phosphatidylinositol hydrolysis

Bradykinin B1 receptors in the rabbit urinary bladder: induction of responses, smooth muscle contraction, and phosphatidylinositol hydrolysis

Influence of γ‐irradiation on poly(methyl methacrylate)

Characterisation of kinin receptors on the human isolated umbilical artery

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Product

Resources

About

Bradykinin B₁ receptors in the rabbit urinary bladder: induction of responses, smooth muscle contraction, and phosphatidylinositol hydrolysis

Bradykinin B₁ receptors in the rabbit urinary bladder: induction of responses, smooth muscle contraction, and phosphatidylinositol hydrolysis