Chemical Name: N-Bicyclo[2.2.1]hept-2-yl-5'-chloro-5'-deoxyadenosine
Biological Activity(±)-5'-Chloro-5'-deoxy-ENBA is a highly selective adenosine A1 receptor agonist (Ki values are 0.51, 1290, 1340 and 2740 nM at A1, A3, A2A and A2B receptors respectively). Reverses formaline-induced nocifensive behavior in mice; antinociceptive.
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N6-bicycloalkyladenosines with unusually high potency and selectivity for the adenosine A1 receptor.
Trivedi et al.
N6-cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice.
Franchetti et al.
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In the first work, we demonstrated that chronic systemic administration of 5′-chloro-5′-deoxy-(±)-ENBA (0.5 mg/kg, i.p.) reduced both mechanical allodynia and thermal hyperalgesia 3 and 7 days post-SNI, in a way prevented by DPCPX (3 mg/kg, i.p.), a selective A1 adenosine receptor antagonist, without exerting any significant change on the motor coordination or arterial blood pressure (Molecules. 2012, 17, 13712-13726. doi: 10.3390/molecules171213712).Then, the product has been used to clearly demonstrate that functionalA1ARs are expressed in microglia (Glia. 2014, 62,122-132. doi: 10.1002/glia.22592).In addition, we found that 5′Cl5′ d-(±)-ENBA, administered in combination with L-DOPA, reduced the development of abnormal involuntary movements. These results indicate the potential benefit of A1R agonists for the treatment of L-DOPA-induced dyskinesia and hyperkinetic disorders providing a mechanistic framework for the study of the interaction between DA and adenosine in the striatonigral system (Exp Neurol. 2014, 261, 733-43. doi: 10.1016/j.expneurol.2014.08.022).