Bradykinin Interaction with 5-Hydroxytryptamine, Norepinephrine, and Potassium Chloride in Rabbit Aorta

Rl, Garrett; Jh, Brown

doi:10.3181/00379727-139-36359

Cited by 5 publications

(6 citation statements)

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“…The possibility that BK contracted the aorta by releasing intramural prostaglandins was excluded by the absence of effect of indomethacin. These results confirm the findings of Garrett and Brown ( 1972), who in addition showed that atropine ( 1 0 -W ) did not influence the effect of BK. When the aortic strips were carefully dissected and incubated for 120 min, under the conditions described in this paper, all strips responded to BK, in contrast with the findings of Garrett and Brown (1972).…”

Section: A Ntugonists Of Bks In the Rabbit Aortasupporting

confidence: 91%

“…A similar lack s f sensitivity in more indomethacin provides strong evidence that than 50% of rabbit aortae was reported by BK and Octa do not stimulate the release of Garrett and Brown ( 1972).…”

Section: Perimentssupporting

confidence: 79%

“…At these concentrations, the antagonists were without effect on the tone of results of Garrett and Brown (1972) and in contrast with findings of others in rat and guinea pig mesenteric veins (Northover 1 9 6 7~~ 1967b), rabbit and dog saphenous veins (Ishioka et ab. 1965;Goldberg et a!.…”

Section: Specificity Of Receptors For Bk and Octa In Rabbit Aortaecontrasting

confidence: 79%

“…However, the sensitivity of the aorta to BK was quite low and only 30-4096 s f the preparations responded to the peptide. However, dose-response relationships for BK or other basic pharmacole~gicd aspects of BK were not described in detail by Garrett and Brown ( 1972).…”

Section: Introductionmentioning

confidence: 99%

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Receptors for bradykinin in rabbit aortae

Regoli¹,

Barabé²,

Park³

1977

Can. J. Physiol. Pharmacol.

249

109

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bradykinin in rabbit aortae. Can. J. Physiol. Pharmacol. 55,[855][856][857][858][859][860][861][862][863][864][865][866][867] Rabbit aorta strips respond to bradykinin (BK) and to the C-terminal fragment of BK, the octapeptide 1-8 BK (Octa) with sustained contractions which are presumably due to the stimulation of specific receptors, because they remain unchanged in presence of phentolamine, methysergide, mepyramine, 8-Leu-AT,,, and indomethacin. Experimental dose-response curves of BK and Octa are very similar to the theoretical curves predicted by the mass-action law and show the classical hyperbolic shape; ratios of doses producing 16% and 84% of maximum effects are 1 :20 for Qcta and 1: 19 for BK. The relations of stinlulus and effect are linear, suggesting that the extents of the contractions are proportional to the number of receptors occupied by the agonists.Stnicture-activity studies performed with fragments and analogues of BK and with analogues of Qcta have shown that 8-Phe is essential for activation of the aortic receptor, and plays an important role for the affinity. The octapeptide 1-8 sequence is more favorable than the nonapeptide. because BK (pD2 = 6.40) is less potent than Octa (pDs = 7.19) and 9-Ala BK is a partial agonist.Antagonists for both Octa and BK have been found by replacing 8-Phe with aliphatic residues (Ala. Nle, Leu, Leu-OMe) in the octapeptide. Affinities of 8-Leu-Octa (PA, = 6.75) and 8-Leu-OMe-Qcta (PA? = 6-66) for the aortic receptors are fairly high and the antagonism appears to be of the competitive type because pA, -pAIo is close to 0.95 for both compounds.The inhibitory effect of these two compounds are specific for Qcta and BK. It is concluded that rabbit aortae contain a new type of receptor for BK, different from those found in the intestine and the uterus of several species. REC;OLI: D., BARABB, J. et PARK, W. K. 1977. Receptors for bradykinin in rabbit aortae. Can. J. Physiol. Pharniacol. 55. 855-867.Les bandelettes d'aorte de lapin rtpondent la bradykinine (BK) et au fragment Cterminal de la BK, l'octapeptide 1-8 BK (Octa) par des contractions soutenues qui sont apparemment dues B la stimulation de ricepteurs spkcifiques. En fait, ces contractions ne sont pas modifites par la phentolamine, la mithylsergide, la mCpyramine, la 8-Leu-AtII et l'indomtthacine. Les courbes dose-rCponse expkrimentales de la BK et de l'Octa sont tr&s semblables aux courbes thtoriques prtvues par la loi d'action de masse et on la forme hyperbolique classique; les rapports entre les doses produisant 16% et 84% de la contraction maximale correspondent A 1 :20 pour l'octa et 1 :9 pour la BK. Les relations stimuluseffet sont 1inCaires et ainsi suggerent que l'ttendue des contractions est proportionnelle au nombre relatif de rtcepteurs occup~s par les agonistes.Des ttudes de structure-activitt utilisant des fragments et analogues de la BK et des analogues de 1'Octa ont dCmontrt que la 8-Phe est essentielle pour l'activation du rtcepteur aortique et peut jouer un r61e important dans l'affiniti.. La ...

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Section: A Ntugonists Of Bks In the Rabbit Aortasupporting

confidence: 91%

Section: Perimentssupporting

confidence: 79%

Section: Specificity Of Receptors For Bk and Octa In Rabbit Aortaecontrasting

confidence: 79%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Receptors for bradykinin in rabbit aortae

Regoli¹,

Barabé²,

Park³

1977

Can. J. Physiol. Pharmacol.

249

109

View full text Add to dashboard Cite

show abstract

“…Activation of B 2 receptors is one of the most studied effects of bradykinin in the vascular system. Although multiple intracellular pathways may be involved, accumulation of NO‐ and COX‐derived compounds is often found to be the primary mediator of the vascular activity of bradykinin (Burch & Axelrod, ; Campos & Calixto, ; Fasciolo et al, ; Garrett & Brown, ; Miyamoto et al, ; More, Kim, Zhao, et al, ; Palmer et al, ; Regoli et al, ; Sai et al, ; Starr & West, ). Using indomethacin, we were able to show that products of COX did not play any detectable role in bradykinin‐increased BP following exposure to LPS.…”

Section: Discussionmentioning

confidence: 99%

Bradykinin increases BP in endotoxemic rat: functional and biochemical evidence of angiotensin II AT₁/bradykinin B₂ receptor heterodimerization

Anton

Fernandes

Assreuy

et al. 2019

British J Pharmacology

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Background and Purpose Bradykinin may induce vasoconstriction in selected vessels or under specific experimental conditions. We hypothesized that inflammatory stimuli, such as endotoxin challenge, may induce the dimerization of AT1/B2 receptors, altering the vascular effects of bradykinin. Experimental Approach Wistar rats received LPS (1 mg·kg−1, i.p.) and were anaesthetized for assessment of BP. Mesenteric resistance arteries were used in organ baths and subjected to co‐immunoprecipitation and Western blot analyses. Key Results At 24 and 48 hr after LPS, bradykinin‐induced hypotension was followed by a sustained increase in BP, which was not found in non‐endotoxemic animals. The B2 receptor antagonist Hoe‐140 fully blocked the responses to bradykinin. The pressor effect of bradykinin was not prevented by prazosin, an α1‐adrenoceptor antagonist, but it was inhibited by the AT1 receptor antagonist losartan or the Rho‐kinase inhibitor Y‐27632. Endotoxemic rats also displayed enhanced pressor responses to angiotensin II, which were blocked by Hoe‐140. Co‐immunoprecipitation isolated using anti‐B2 or anti‐AT1 receptor antibodies showed that resistance arteries presented augmented levels of the AT1/B2 receptor complexes at 24 hr after LPS injection. The presence of AT1/B2 receptor heterodimers did correlate with the development of losartan‐sensitive contractile responses to bradykinin and potentiation of angiotensin II‐induced contraction, which was prevented by Hoe‐140. Conclusions and Implications Endotoxin challenge is a stimulus for AT1/B2 receptor heterodimerization in native vessels and shifts the B2 receptor‐dependent vascular effect of bradykinin to a more complex pathway, which also depends on AT1 receptors and their intracellular signalling pathways.

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Basic Pharmacological Properties

Müller‐Schweinitzer¹,

Weidmann²

1978

Ergot Alkaloids and Related Compounds

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Bradykinin Interaction with 5-Hydroxytryptamine, Norepinephrine, and Potassium Chloride in Rabbit Aorta

Cited by 5 publications

References 0 publications

Receptors for bradykinin in rabbit aortae

Receptors for bradykinin in rabbit aortae

Bradykinin increases BP in endotoxemic rat: functional and biochemical evidence of angiotensin II AT₁/bradykinin B₂ receptor heterodimerization

Basic Pharmacological Properties

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Bradykinin Interaction with 5-Hydroxytryptamine, Norepinephrine, and Potassium Chloride in Rabbit Aorta

Cited by 5 publications

References 0 publications

Receptors for bradykinin in rabbit aortae

Receptors for bradykinin in rabbit aortae

Bradykinin increases BP in endotoxemic rat: functional and biochemical evidence of angiotensin II AT1/bradykinin B2 receptor heterodimerization

Basic Pharmacological Properties

Contact Info

Product

Resources

About

Bradykinin increases BP in endotoxemic rat: functional and biochemical evidence of angiotensin II AT₁/bradykinin B₂ receptor heterodimerization