Bradykinin receptors and their antagonists

Regoli, Doménico; Allogho, S Nsa; Rizzi, Anna; Gobeil, Fernand

doi:10.1016/s0014-2999(98)00165-4

Cited by 234 publications

(183 citation statements)

References 69 publications

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“…The present study provides the first evidence that under physiological conditions (distant from anesthesia and acute surgical trauma), coronary vasodilation in both conductance and resistance vessels produced by intracoronary des-Arg 9 -bradykinin is mediated by bradykinin B 1 receptors. This is supported by the fact that Hoe 140, a selective B 2 receptor antagonist, 16,17 did not block the effects of des-Arg 9 -bradykinin and that this effect was blocked in vitro by a B 1 receptor antagonist, des-Arg 9 ,[Leu 8 ]-bradykinin. In anesthetized greyhounds, intracoronary injection of a small dose of des-Arg 9 -bradykinin increased CBFv but did not modify CD, whereas a larger dose of des-Arg 9 -bradykinin increased both CBFv and CD in association with systemic effects.…”

Section: Discussionmentioning

confidence: 92%

Stimulation of Bradykinin B ₁ Receptors Induces Vasodilation in Conductance and Resistance Coronary Vessels in Conscious Dogs

Houël

Héloire

et al. 2000

Circulation

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Background-Constitutive bradykinin B 1 receptors have been identified in dogs; however, their physiological implications involving the coronary circulation remain to be determined. This study examined, in conscious dogs, the coronary response to des-Arg 9 -bradykinin (a B 1 receptor agonist) and the mechanisms involved. Methods and Results-Eleven dogs were instrumented with a left ventricular micromanometer, a circumflex coronary catheter, a cuff occluder, a Doppler flow probe, and ultrasonic crystals to measure coronary blood flow velocity (CBFv) and coronary diameter (CD). Intracoronary des-Arg 9 -bradykinin (3 to 100 ng/kg) and bradykinin (0.1 to 10 ng/kg) did not modify systemic hemodynamics but dose-dependently increased CBFv and CD. Des-Arg 9 -bradykinin was less potent than bradykinin. Hoe 140 (a B 2 antagonist, 10 g/kg) abolished the effects of bradykinin but did not influence the effects of des-Arg 9 -bradykinin. When CBFv increase was prevented by the cuff occluder, CD responses to bradykinin and des-Arg 9 -bradykinin were maintained. Intracoronary lisinopril (0.75 mg) increased the CD response to bradykinin, with only minimal effect on CBFv, and extended the duration of the effect. Lisinopril did not alter des-Arg 9 -bradykinin responses. Intracoronary N -nitro-L-arginine (2 mg/kg) decreased the CD effect of bradykinin and prevented the CBFv and CD effects of des-Arg 9 -bradykinin. The relaxing effect of des-Arg 9 -bradykinin on isolated coronary rings was prevented by des-Arg 9 ,[Leu 8 ]-bradykinin. Conclusions-In the conscious dog, B 1 receptors are present in coronary vessels, and their stimulation produces vasodilation in conductance and resistance vessels, which is mediated essentially by NO but not modulated by angiotensin-converting enzyme. However, the coronary vasodilation induced by B 1 receptor stimulation is not as great as that produced by B 2 receptor stimulation.

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Section: Discussionmentioning

confidence: 92%

Stimulation of Bradykinin B ₁ Receptors Induces Vasodilation in Conductance and Resistance Coronary Vessels in Conscious Dogs

Houël

Héloire

et al. 2000

Circulation

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“…Действие кининов в организме реализуется путём взаимодействия с рецепторами двух типов -Б 1 и Б 2 рецепторами (Б 1 Р и Б 2 Р), относящимися к суперсемейству рецепторов, сопряжённых с G-белками (GPCR) [16,30]. Основные различия между Б 1 Р и Б 2 Р заключаются в их экспрессии, специфичности и физиологических эффектах, за которые они отвечают.…”

Section: классификация рецепторов кининовunclassified

“…У оптимальных пептидных антагонистов Б 2 Р сохранены аминокислотные остатки Arg 1 и Arg 9 , в отличие от агонистов и антагонистов Б 1 Р, где отсутствует аминокислотный остаток Arg 9 , как, например, в пептиде (Leu 8 )des-Arg 9 -Бк. Второе поколение пептидных антагонистов Б 1 Р включает в свою структуру N-концевой аминокислотный остаток Lys или его аналог Orn, который значительно повышает аффинность антагонистов по отношению к Б 1 Р человека [30]. Представителем второго поколения пептидных антагонистов Б 2 Р является икатибант [38].…”

Section: антагонисты рецепторов кининовunclassified

Ace inhibitors - activators of kinin receptors

Kugaevskaya

Elisseeva

2011

BIOMED KHIM

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Angiotensin converting enzyme (ACE) inhibitors are widely used for treatment of cardiovascular diseases. The effects of ACE inhibitors on the human bradykinin receptors were investigated. The mode of action of ACE inhibitors is considered. There is evidence that ACE inhibitors exert effects on the vascular system that cannot be attributed simply to the inhibition of ACE activity and accumulation of locally produced bradykinin. ACE inhibitors augment bradykinin effects on receptors indirectly by inducing cross-talk between ACE and the B2 receptor when enzyme and receptor molecules are sterically close, possibly forming a heterodimer. ACE inhibitors activate B1 receptors directly and independently of ACE via the zink-binding consensus sequence HEXXH, which is present in B1, but not in B2 receptor. Particular structure of B2 and B1 are represented, as well as receptor amino acids coupled with the G-proteins. Activation of kinin receptors by ACE inhibitors leads to clinically beneficial effects of ACE inhibitors.

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“…Le récepteur B 2 est distribué de façon ubiquitaire et est présent notamment sur les cellules endothéliales, les cellules musculaires lisses, les fibroblastes, les cellules mésangiales et épithéliales, certains neurones, les astrocytes et les polynucléaires neutrophiles [3]. Plusieurs excellents agonistes et antagonistes sélectifs du récepteur B 2 , de nature peptidique ou non, ont été développés [4, 7,8…”

Section: Récepteur B 2 Des Kininesunclassified

“…Toutefois, chez le chien, le récepteur B 1 semble être constitutif et son activation cause une hypotension, une natriurèse et une vasodilatation rénale [17,18]. Des agonistes et des antagonistes peptidiques spécifiques de B 1 ont été développés [7][8][9] (Tableau IV). Des antagonistes non peptidiques du récepteur B 1 ne sont pas encore disponibles commercialement.…”

Section: Fonction Du Récepteur B 2 Dans L'inflammation Neurogéniqueunclassified

Dualité fonctionnelle des récepteurs des kinines en physiopathologie

2003

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Bradykinin receptors and their antagonists

Cited by 234 publications

References 69 publications

Stimulation of Bradykinin B ₁ Receptors Induces Vasodilation in Conductance and Resistance Coronary Vessels in Conscious Dogs

Stimulation of Bradykinin B ₁ Receptors Induces Vasodilation in Conductance and Resistance Coronary Vessels in Conscious Dogs

Ace inhibitors - activators of kinin receptors

Dualité fonctionnelle des récepteurs des kinines en physiopathologie

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Bradykinin receptors and their antagonists

Cited by 234 publications

References 69 publications

Stimulation of Bradykinin B 1 Receptors Induces Vasodilation in Conductance and Resistance Coronary Vessels in Conscious Dogs

Stimulation of Bradykinin B 1 Receptors Induces Vasodilation in Conductance and Resistance Coronary Vessels in Conscious Dogs

Ace inhibitors - activators of kinin receptors

Dualité fonctionnelle des récepteurs des kinines en physiopathologie

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Stimulation of Bradykinin B ₁ Receptors Induces Vasodilation in Conductance and Resistance Coronary Vessels in Conscious Dogs

Stimulation of Bradykinin B ₁ Receptors Induces Vasodilation in Conductance and Resistance Coronary Vessels in Conscious Dogs