![]() įishman P (2022) Drugs targeting the A 3 adenosine receptor: human clinical study data. īaraldi PG, Tabrizi MA, Gessi S, Borea PA (2008) Adenosine receptor antagonists: translating medicinal chemistry and pharmacology into clinical utility. Jacobson KA, Tosh DK, Jain S, Gao ZG (2019) Historical and current adenosine receptor agonists in preclinical and clinical development. Ĭhen G-J, Harvey BK, Shen H, Chou J, Victor A, Wang Y (2006) Activation of adenosine A 3 receptors reduces ischemic brain injury in rodents. Spinozzi E, Baldassarri C, Acquaticci L et al (2021) Adenosine receptors as promising targets for the management of ocular diseases. Jung S-M, Peyton L, Essa H, Choi D-S (2022) Adenosine receptors: emerging non-opioids targets for pain medications. Safadi R, Braun M, Francis A et al (2021) Randomised clinical trial: a phase 2 double-blind study of namodenoson in non-alcoholic fatty liver disease and steatohepatitis. ĭavid M, Gospodinov DK, Gheorghe N et al (2016) Treatment of plaque-type psoriasis with oral CF101: data from a phase II/III multicenter, randomized, controlled trial. Merighi S, Battistello E, Giacomelli L, Varani K, Vincenzi F, Borea PA et al (2019) Targeting A 3 and A 2A adenosine receptors in the fight against cancer. In: Varani K (ed) The adenosine receptors, the receptors, vol 34. Medicinal chemistry of the A 3 adenosine receptor. Jacobson KA, Tosh DK, Gao ZG, Yu J, Suresh RR, Rao H, Romagnoli R, Baraldi PG, Tabrizi MA (2018) Chapter 7. Keywordsīorea PA, Varani K, Vincenzi F, Baraldi PG, Tabrizi MA, Merighi S et al (2015) The A 3 adenosine receptor: history and perspectives. Both the historical development of this field and the current state of the clinical trial-directed medicinal chemistry are included in this chapter. ![]() The number of current clinical trials for A 3AR ligands has now grown, with A 3AR agonists accounting for the majority. Some A 3AR ligands are being developed as therapeutic candidate molecules for a variety of chronic (e.g., psoriasis, NASH, pain, cancer, glaucoma) and acute (stroke, cardiac ischemia) conditions. In recent years, a structural approach has been adopted for the discovery of novel A 3AR ligands, either to improve the potency of known ligands or to discover novel chemotypes for this receptor. Furthermore, prodrugs of some of these ligands have been reported, and their efficacy was demonstrated in animal models. The structure–affinity relationships and selectivity of A 3AR ligands compared to the other three ARs have been described. Numerous classes of selective agonists, antagonists, and allosteric modulators of the A 3 adenosine receptor (AR) have been reported.
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