| Therapeutic potential of A2 and A3 adenosine receptor: a review of novel patented ligands. | |
| | |
MedLine Citation:
|
PMID: 22435652 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
Adenosine exerts its effects by interacting with G-protein coupled receptors (GPCR) namely A(1), A(2A), A(2B) and A(3), respectively. These are involved in several diseases, for example and most importantly, Parkinson's disease, ischemia and inflammation. There is high interest in the development of potent and selective ligands for these adenosine receptor (AR) subtypes, primarily for their therapeutic potential but also as pharmacological tools in receptor studies. AREAS COVERED: This paper concentrates on reviewing the therapeutic potential of A(2) and A(3) ARs, which represent the most interesting subtypes of recent years. A general description of each receptor is reported with novel agonist and antagonist structures, patented in 2008 - 2011. PubMed and Free Patents Online databases were principally used to collect all the material. EXPERT OPINION: In the past years, by modulating A(2) and A(3)ARs, several new possible therapeutic applications were discovered. For this reason, research concerning AR ligands is still of great interest. In particular, few potent and selective A(2B) agonists and antagonists are actually reported and a clear SAR (structure-activity relationship) profile lacks for this AR subtype. At the A(3)AR, allosteric modulation may prevent problems related to the high difference between rat and human orthosteric sites and simplify the preclinical studies on A(3)AR. |
| | |
Authors:
|
Stephanie Federico; Giampiero Spalluto |
Publication Detail:
|
Type: Journal Article; Review Date: 2012-03-22 |
Journal Detail:
|
Title: Expert opinion on therapeutic patents Volume: 22 ISSN: 1744-7674 ISO Abbreviation: Expert Opin Ther Pat Publication Date: 2012 Apr |
Date Detail:
|
Created Date: 2012-04-05 Completed Date: 2012-07-30 Revised Date: 2013-05-20 |
Medline Journal Info:
|
Nlm Unique ID: 9516419 Medline TA: Expert Opin Ther Pat Country: England |
Other Details:
|
Languages: eng Pagination: 369-90 Citation Subset: IM |
Affiliation:
|
Università degli Studi di Trieste, Dipartimento di Scienze Chimiche e Farmaceutiche, Italy. sfederico@units.it |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Adenosine A2 Receptor Agonists
/
pharmacology Adenosine A2 Receptor Antagonists / pharmacology Adenosine A3 Receptor Agonists / pharmacology Adenosine A3 Receptor Antagonists / pharmacology Drug Design Humans Ligands Male Molecular Structure Patents as Topic Purinergic Agents / chemistry, pharmacology* Receptor, Adenosine A3 / drug effects*, metabolism Receptors, Adenosine A2 / drug effects*, metabolism Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
|
0/Adenosine A2 Receptor Agonists; 0/Adenosine A2 Receptor Antagonists; 0/Adenosine A3 Receptor Agonists; 0/Adenosine A3 Receptor Antagonists; 0/Ligands; 0/Purinergic Agents; 0/Receptor, Adenosine A3; 0/Receptors, Adenosine A2 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Water Oxidation Catalyzed by the Tetranuclear Mn Complex [Mn(IV)(4)O(5)(terpy)(4)(H(2)O)(2)](ClO(4))...
Next Document: Biofunctionalized calcium phosphate cement to enhance the attachment and osteodifferentiation of ste...