Recommended Conferences

2nd International Conference on Clinical Psychiatry

Miami, USA

Neuroscience Psychiatry

Dubai, UAE

Psychology and Mental Health

Chicago, USA
Related Subjects
 

Therapeutic potential of A2 and A3 adenosine receptor: a review of novel patented ligands

Author(s): Federico S, Spalluto G

Abstract

Introduction: Adenosine exerts its effects by interacting with G-protein coupled receptors (GPCR) namely A1, A2A, A2B and A3, 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 A2 and A3 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 A2 and A3ARs, 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 A2B agonists and antagonists are actually reported and a clear SAR (structure–activity relationship) profile lacks for this AR subtype. At the A3AR, allosteric modulation may prevent problems related to the high difference between rat and human orthosteric sites and simplify the preclinical studies on A3AR.

Similar Articles

The impact of coffee on health

Author(s): Cano-Marquina A, Tarín JJ, Cano A

Tolerance to the humoral and hemodynamic effects of caffeine in man

Author(s): Robertson D, Wade D, Workman R, Woosley RL, Oateshttp JA

Caffeine consumption

Author(s): Barone JJ, Roberts HR

Neuropsychiatric effects of caffeine

Author(s): Winston AP, Hardwick E, Jaberi N

Caffeine fatalities – four case reports

Author(s): Holmgren P, Nordén-Pettersson L, Ahlner J

Caffeine metabolism in patients with chronic liver disease

Author(s): Rodopoulos N, Wisén O, Norman A

Assessment of risk involved in the combination medicine of paracetamol and caffeine

Author(s): Uddin MS, Wali MW, Mamun AA, Asaduzzaman M, Amran MS, et al.

Caffeine for the sustainment of mental task performance: Formulations for military operations

Author(s): Vanderveen JE, Armstrong LE, Butterfield GE, Chenoweth WL, Dwyer JT, et al.

Effect of smoking on caffeine clearance

Author(s): Parsons WD, Neims AH

Pharmacokinetic profile of caffeine in the premature newborn infant with apnea

Author(s): Aranda JV, Cook CE, Gorman W, Collinge JM, Loughnan PM, et al.

Pharmacokinetic aspects of theophylline in premature newborns

Author(s): Aranda JV, Sitar DS, Parsons WD, Loughnan PM, Neims AH

Cytochrome P450-dependent metabolism of caffeine in Drosophila melanogaster

Author(s): Coelho A, Fraichard S, Le Goff G, Faure P, Artur Y, Ferveur JF, Heydel JM

Effects of caffeine on visual monitoring

Author(s): Baker WJ, Theologus GC

Seizures and epilepsy after ischemic stroke

Author(s): Camilo O, Goldstein LB

Crude caffeine reduces memory impairment and amyloid ß(1-42) levels in an Alzheimer's mouse model

Author(s): Chu YF, Chang WH, Black RM, Liu JR, Sompol P, et al.