Antagonist pharmacology of adenosine A2B receptors from rat, guinea pig and dog

Fozard, John R.; Baur, François; Wolber, Cedric

doi:10.1016/s0014-2999(03)02078-8

Cited by 34 publications

(22 citation statements)

References 14 publications

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“…Combining the results of this previous study by Kim et al (2002) with our data, we propose that human, rabbit, and mouse A 2B ARs have similar binding characteristics, whereas dog and rat A 2B ARs can be categorized as having lower binding potency for xanthine antagonists. Our results also agree with those of Fozard et al (2003), who suggested that antagonist pharmacology of the dog A 2B AR differs from that of A 2B ARs from human, rat, and guinea pig based on pK b values calculated from bioassays of various smooth muscle preparations. In contrast, we observed no species differences in agonist binding to A 2B ARs.…”

Section: Discussionsupporting

confidence: 92%

“…In a search for more selective antagonists for the human A 2B AR, Kim et al (2000Kim et al ( , 2002 noticed that certain xanthine antagonists bound heterologously expressed recombinant rat A 2B ARs with up to 10-fold lower affinity compared with human A 2B ARs. Fozard et al (2003) also suggested that antagonist pharmacology of A 2B ARs differs significantly among human, dog, rat, and guinea pig.…”

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confidence: 99%

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Characterization of the A_2BAdenosine Receptor from Mouse, Rabbit, and Dog

Auchampach¹,

Kreckler²,

Wan³

et al. 2009

J Pharmacol Exp Ther

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Section: Discussionsupporting

confidence: 92%

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confidence: 99%

Characterization of the A_2BAdenosine Receptor from Mouse, Rabbit, and Dog

Auchampach¹,

Kreckler²,

Wan³

et al. 2009

J Pharmacol Exp Ther

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“…The finding that CGS-21680, a prototype A 2A receptor agonist, was inactive at 1 M suggests that the A 2A receptor may be ruled out (28). Furthermore, the potency of NECA is within the range of the potency described for this agonist as an A 2B receptor agonist (17). Likewise, and by the same argument, we may also discard the influence of A 3 receptors, because 2-Cl-IB-MECA, a high-affinity A 3 receptor agonist (27), was inactive as a vasoconstrictor and instead induced relaxations.…”

Section: Discussionmentioning

confidence: 86%

A_2Badenosine receptor mediates human chorionic vasoconstriction and signals through arachidonic acid cascade

Donoso¹,

López²,

Miranda³

et al. 2005

American Journal of Physiology-Heart and Circulatory Physiology

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Because adenosine is a vascular tone modulator, we examined the effect of adenosine and congeners in the vascular reactivity of isolated human placental vessels and in perfused cotyledons. We characterized its vasomotor action and tentatively identified the receptor subtypes and their intracellular signaling mechanisms. We recorded isometric tension from the circular layer of chorionic vessel rings maintained under 1.5 g of basal tension or precontracted with KCl. The relative order of potency of adenosine and structural analogs is consistent with the expression of A2B receptors, 5'-(N-ethylcarboxamido)adenosine (NECA) being the most potent. The maximal contraction ranged from 45% to 60% of the KCl standard response, except for an A2A receptor agonist that did not exceed 15%. Consistently, NECA was 100-fold more potent than adenosine to raise the perfusion pressure of ex vivo perfused cotyledons. In contrast, a selective A3 receptor agonist relaxed precontracted rings of chorionic vessels. Whereas a selective A3 receptor antagonist was ineffective to antagonize adenosine-induced contraction, A2 or A1 receptor antagonists reduced adenosine-induced vasoconstriction concentration-dependently. Denudation of the endothelial layer reduced adenosine- and NECA-induced contractions by 50-70%. Furthermore, indomethacin reduced adenosine- or NECA-induced contractions concentration-dependently in intact and endothelium-denuded rings. A thromboxane receptor antagonist blocked adenosine- and NECA-induced contractions in intact and endothelium-denuded rings, suggesting the involvement of an arachidonic acid metabolite as the mediator of the vasoconstriction. We propose that adenosine A2B receptors mediate the adenosine-induced contraction vasomotor effect in human chorionic vessels and that this involves synthesis of a thromboxane receptor activator or a related prostanoid.

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“…The stimulation of A 2B receptor in human beings activates the mast cells [13] , and as a result, increases the release of IL-8 [14] . The inhibition of A 2B receptors can have helpful therapeutic effects on asthma [15] and lead to the decrease of bronchospasm in response to such stimuli as AMP [16] .…”

Section: Introductionmentioning

confidence: 99%

Nigella Sativa’nın Biyoaktif Komponenti Olan Timokinon Ovalbuminle Uyarılmış Ginedomuzlarında Adenozin A2 Reseptörlerini Etkileyebilir

MIRZAMOHAMMADI¹,

Keyhanmanesh²,

Baradaran³

et al. 2016

Kafkas Univ Vet Fak Derg

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Thymoquinone has demonstrated anti-asthmatic effects in many studies but its exact mechanism is not yet fully known. This investigation aims to demonstrate its prophylactic effect in the presence of selective A2A and A2B adenosine receptors (AR) antagonist; MRS1706 and ZM241365, in sensitized guinea pigs. The gene expression of A2 AR in blood lymphocytes and lung tissue, lung pathological changes and blood cytokines were evaluated in seven groups. The experiments in blood lymphocytes and lung tissue showed that thymoquinone could increase A2AAR mRNA expression and decrease A2B AR mRNA expression significantly (P<0.001 to P<0.05); however sensitization had opposite effects. Administration of A2A receptor antagonist attenuated inflammation and A2B receptor antagonist could prevent asthma-induced inflammatory changes. Moreover, the administration of thymoquinone and A2Areceptor antagonist together relieved inflammation. Gene expression of A2B receptor showed that thymoquinone administration has more influence on blood lymphocytes while administration of the selective A2B receptor antagonist was more effective in lung tissue. The results showed some of the therapeutic effects of thymoquinone in reducing asthma symptoms might be partially mediated through A2 adenosine receptors. Keywords: Asthma, Adenosine, MRS1706, ZM241365, Gene expression Nigella Sativa'nın Biyoaktif Komponenti Olan Timokinon Ovalbuminle Uyarılmış Ginedomuzlarında Adenozin A 2 Reseptörlerini Etkileyebilir ÖzetTimokinonun birçok çalışmada anti-astmatik etkileri olduğu gösterilmesine rağmen tam mekanizması tamamıyla anlaşılamamıştır. Bu çalışma A2A ve A2B adenozin reseptör (AR) antagonistlerinin (MRS1706 ve ZM241365) mevcudiyetinde timokinonun uyarılmış ginedomuzlarındaki proflaktik etkisini araştırmak amacıyla yapılmıştır. Çalışmada toplam yedi grupta kan lenfositleri ve akciğer dokusunda A2 AR gen ekspresyonları, akciğerdeki patolojik değişiklikler ve kan sitokinleri değerlendirildi. Kan lenfositleri ve akciğer dokusunda yapılan incelemeler timokinonun A2AAR mRNA ekspresyonunu arttırdığını ve A2B AR mRNA ekspresyonunu ise anlamlı oranda azalttığını, ancak uyarılmanın ters etki yaptığını ortaya koydu (P<0.001 to P<0.05). A2A reseptör antagonisti yangıyı azaltırken ve A2B reseptör antagonisti astma tarafından oluşturulan yangısal değişikliklere karşı koruyucu etki gösterebilir. Ayrıca, timokinon ve A2A reseptör antagonistinin birlikte uygulanması yangıyı hafifletti. A2B reseptör gen ekspresyonu timokinon uygulamasının kan lenfositleri üzerinde daha etkili olduğunu A2B reseptör antagonistinin ise akciğer dokusunda daha etkili olduğunu gösterdi. Elde edilen sonuçlar astma semptomlarının azaltılmasında timokinon uygulamasının terapötik etkilerinin kısmen A2 adenozin reseptörleri yoluyla oluştuğunu göstermiştir.

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Antagonist pharmacology of adenosine A2B receptors from rat, guinea pig and dog

Cited by 34 publications

References 14 publications

Characterization of the A_2BAdenosine Receptor from Mouse, Rabbit, and Dog

Characterization of the A_2BAdenosine Receptor from Mouse, Rabbit, and Dog

A_2Badenosine receptor mediates human chorionic vasoconstriction and signals through arachidonic acid cascade

Nigella Sativa’nın Biyoaktif Komponenti Olan Timokinon Ovalbuminle Uyarılmış Ginedomuzlarında Adenozin A2 Reseptörlerini Etkileyebilir

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Antagonist pharmacology of adenosine A2B receptors from rat, guinea pig and dog

Cited by 34 publications

References 14 publications

Characterization of the A2BAdenosine Receptor from Mouse, Rabbit, and Dog

Characterization of the A2BAdenosine Receptor from Mouse, Rabbit, and Dog

A2Badenosine receptor mediates human chorionic vasoconstriction and signals through arachidonic acid cascade

Nigella Sativa’nın Biyoaktif Komponenti Olan Timokinon Ovalbuminle Uyarılmış Ginedomuzlarında Adenozin A2 Reseptörlerini Etkileyebilir

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Characterization of the A_2BAdenosine Receptor from Mouse, Rabbit, and Dog

Characterization of the A_2BAdenosine Receptor from Mouse, Rabbit, and Dog

A_2Badenosine receptor mediates human chorionic vasoconstriction and signals through arachidonic acid cascade