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5'-Chloro-5'-deoxy-(±)-ENBA, a Potent and Selective Adenosine A1 Receptor Agonist, Alleviates Neuropathic Pain in Mice Through Functional Glial and Microglial Changes without Affecting Motor or Cardiovascular Functions

Livio Luongo, Riccardo Petrelli, Luisa Gatta, Catia Giordano, Francesca Guida, Patrizia Vita, Palmarisa Franchetti, Mario Grifantini, Vito Novellis, Loredana Cappellacci, Sabatino Maione
2012 Molecules  

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This study was undertaken in order to investigate the effect of chronic treatment with 5′-chloro-5′-deoxy-(±)-ENBA, a potent and highly selective agonist of human adenosine A 1 receptor, on thermal hyperalgesia and mechanical allodynia in a mouse model of neuropathic pain, the Spared Nerve Injury (SNI) of the sciatic nerve. 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
more » ... evented by DPCPX (3 mg/kg, i.p.), a selective A 1 adenosine receptor antagonist, without exerting any significant change on the motor coordination or arterial blood pressure. In addition, a single intraperitoneal injection of 5′-chloro-5′-deoxy-(±)-ENBA (0.5 mg/kg, i.p.) 7 days OPEN ACCESS Molecules 2012, 17 13713 post-SNI also reduced both symptoms for at least two hours. SNI was associated with spinal changes in microglial activation ipsilaterally to the nerve injury. Activated, hypertrophic microglia were significantly reduced by 5′-chloro-5′-deoxy-(±)-ENBA chronic treatment. Our results demonstrated an involvement of adenosine A 1 receptor in the amplified nociceptive thresholds and in spinal glial and microglial changes occurred in neuropathic pain, without affecting motor coordination or blood pressure. Our data suggest a possible use of adenosine A 1 receptor agonist in neuropathic pain symptoms.
doi:10.3390/molecules171213712 pmid:23174891 fatcat:b46uxpgnzvhvboqgmzzqqcjpny
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Livio Luongo, Riccardo Petrelli, Luisa Gatta, Catia Giordano, Francesca Guida, Patrizia Vita, Palmarisa Franchetti, Mario Grifantini, Vito Novellis, Loredana Cappellacci, Sabatino Maione. "5'-Chloro-5'-deoxy-(±)-ENBA, a Potent and Selective Adenosine A1 Receptor Agonist, Alleviates Neuropathic Pain in Mice Through Functional Glial and Microglial Changes without Affecting Motor or Cardiovascular Functions." Molecules 17.12 (2012) 13712-13726