The Synthesis and Biological activity of a Highly Selective Adenosine A<sub>2a</sub>. Receptor Agonist

Borcherding, David R.; Lentz, Nelsen L.; Weintraub, Philip M.; Dudley, Mark W.; Secrest, Roberta J.; Kastner, Philip R.; Peet, Norton P.; Roussel, Hoechst Marion

doi:10.1080/07328319908044874

Cited by 3 publications

(1 citation statement)

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“…From the whole series, which includes 2-amino-, [80] 2-hydrazino-, [32,45,81] 2-alkoxy-, [82] 2-alkylthio-, [83][84][85] and 2-alkynyl-derivatives, [37,38,77,79] the compounds showing the highest A 2A affinity bore a phenylethyl (or cyclohexylethyl) group directly linked to the heteroatom or triple bond (see Table 1 compounds 4-9).…”

Section: -Substituted Adenosine Derivativesmentioning

confidence: 99%

Highlights on the Development of A_2A Adenosine Receptor Agonists and Antagonists

et al. 2007

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Although significant progress has been made in the past few decades demonstrating that adenosine modulates a variety of physiological and pathophysiological processes through the interaction with four subtypes of a family of cell-surface G-protein-coupled receptors, clinical evaluation of some adenosine receptor ligands has been discontinued. Major problems include side effects due to the wide distribution of adenosine receptors, low brain penetration (which is important for the targeting of CNS diseases), short half-life of compounds, or a lack of effects, in some cases perhaps due to receptor desensitization or to low receptor density in the targeted tissue. Currently, three A(2A) adenosine receptor agonists have begun phase III studies. Two of them are therapeutically evaluated as pharmacologic stress agents and the third proved to be effective in the treatment of acute spinal cord injury (SCI), while avoiding the adverse effects of steroid agents. On the other hand, the great interest in the field of A(2A) adenosine receptor antagonists is related to their application in neurodegenerative disorders, in particular, Parkinson's disease, and some of them are currently in various stages of evaluation. This review presents an update of medicinal chemistry and molecular recognition of A(2A) adenosine receptor agonists and antagonists, and stresses the strong need for more selective ligands at the A(2A) human subtype.

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Section: -Substituted Adenosine Derivativesmentioning

confidence: 99%

Highlights on the Development of A_2A Adenosine Receptor Agonists and Antagonists

et al. 2007

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ChemInform Abstract: The Synthesis and Biological Activity of a Highly Selective Adenosine A_2a Receptor Agonist.

Borcherding¹,

Lentz²,

Weintraub³

et al. 2000

ChemInform

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The Synthesis and Biological Activity of a Highly Selective Adenosine A 2a Receptor Agonist.-Compound (III) is shown to be the most selective A 2a receptor agonist reported to date having an A 1 /A 2 ratio of 2400. In addition, (III) reduces blood pressure in rats and dogs with only minimal effects on heart rate. -(BORCHERDING, DAVID R.; LENTZ, NELSEN L.; WEINTRAUB, PHILIP M.; DUDLEY, MARK W.; SECREST, ROBERTA; KASTNER, PHILIP R.; PEET, NORTON P.; Nucleosides Nucleotides 18 (1999) 10, 2175-2191; Hoechst Marion Russel, Inc., Bridgewater, NJ 08807, USA; EN)

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Antihypertensive profile of 2-thienyl-3,4-methylenedioxybenzoylhydrazone is mediated by activation of the A2A adenosine receptor

Leal

Pereira

Kümmerle

et al. 2012

European Journal of Medicinal Chemistry

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The Synthesis and Biological activity of a Highly Selective Adenosine A_2a. Receptor Agonist

Cited by 3 publications

References 9 publications

Highlights on the Development of A_2A Adenosine Receptor Agonists and Antagonists

Highlights on the Development of A_2A Adenosine Receptor Agonists and Antagonists

ChemInform Abstract: The Synthesis and Biological Activity of a Highly Selective Adenosine A_2a Receptor Agonist.

Antihypertensive profile of 2-thienyl-3,4-methylenedioxybenzoylhydrazone is mediated by activation of the A2A adenosine receptor

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The Synthesis and Biological activity of a Highly Selective Adenosine A2a. Receptor Agonist

Cited by 3 publications

References 9 publications

Highlights on the Development of A2A Adenosine Receptor Agonists and Antagonists

Highlights on the Development of A2A Adenosine Receptor Agonists and Antagonists

ChemInform Abstract: The Synthesis and Biological Activity of a Highly Selective Adenosine A2a Receptor Agonist.

Antihypertensive profile of 2-thienyl-3,4-methylenedioxybenzoylhydrazone is mediated by activation of the A2A adenosine receptor

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About

The Synthesis and Biological activity of a Highly Selective Adenosine A_2a. Receptor Agonist

Highlights on the Development of A_2A Adenosine Receptor Agonists and Antagonists

Highlights on the Development of A_2A Adenosine Receptor Agonists and Antagonists

ChemInform Abstract: The Synthesis and Biological Activity of a Highly Selective Adenosine A_2a Receptor Agonist.