Polyamidoamine (PAMAM) dendrimer conjugate specifically activates the A3 adenosine receptor to improve post-ischemic/reperfusion function in isolated mouse hearts

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Polyamidoamine (PAMAM) dendrimer conjugate specifically activates the A3 adenosine receptor to improve post-ischemic/reperfusion function in isolated mouse hearts

BACKGROUND When stimulated by small molecular agonists, the A3 adenosine receptor (AR) mediates cardioprotective effects without inducing detrimental hemodynamic side effects. We have examined pharmacologically the protective properties of a multivalent dendrimeric conjugate of a nucleoside as a selective multivalent agonist for the mouse A3AR. RESULTS A PAMAM dendrimer fully substituted by c...

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Enhanced A3 adenosine receptor selectivity of multivalent nucleoside-dendrimer conjugates

BACKGROUND An approach to use multivalent dendrimer carriers for delivery of nucleoside signaling molecules to their cell surface G protein-coupled receptors (GPCRs) was recently introduced. RESULTS A known adenosine receptor (AR) agonist was conjugated to polyamidoamine (PAMAM) dendrimer carriers for delivery of the intact covalent conjugate to on the cell surface. Depending on the linking m...

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Identification and function of adenosine A3 receptor in afferent arterioles.

Adenosine plays an important role in regulation of renal microcirculation. All receptors of adenosine, A1, A2A, A2B, and A3, have been found in the kidney. However, little is known about the location and function of the A3 receptor in the kidney. The present study determined the expression and role of A3 receptors in mediating the afferent arteriole (Af-Art) response and studied the interaction...

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Adenosine A3 Receptor and Cardioprotection

Ischemic injury to the myocardium is a leading cause of morbidity and mortality around the globe.1 It is worth remembering, however, that this insult to the heart emerged only in the last few centuries, an instant in time from an evolutionary perspective. Thus, any cardioprotective responses to ischemic injury undoubtedly evolved for an entirely different purpose. Beyond pure academic interest,...

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The A3 adenosine receptor: history and perspectives.

By general consensus, the omnipresent purine nucleoside adenosine is considered a major regulator of local tissue function, especially when energy supply fails to meet cellular energy demand. Adenosine mediation involves activation of a family of four G protein-coupled adenosine receptors (ARs): A(1), A(2)A, A(2)B, and A(3). The A(3) adenosine receptor (A(3)AR) is the only adenosine subtype to ...

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ژورنال

عنوان ژورنال: BMC Pharmacology

سال: 2011

ISSN: 1471-2210

DOI: 10.1186/1471-2210-11-11