HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

5'-Chloro-5'-deoxy-(±)-ENBA, a potent and selective adenosine A(1) receptor agonist, alleviates neuropathic pain in mice through functional glial and microglial changes without affecting motor or cardiovascular functions.

Abstract
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 prevented 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 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.
AuthorsLivio Luongo, Riccardo Petrelli, Luisa Gatta, Catia Giordano, Francesca Guida, Patrizia Vita, Palmarisa Franchetti, Mario Grifantini, Vito de Novellis, Loredana Cappellacci, Sabatino Maione
JournalMolecules (Basel, Switzerland) (Molecules) Vol. 17 Issue 12 Pg. 13712-26 (Nov 22 2012) ISSN: 1420-3049 [Electronic] Switzerland
PMID23174891 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Adenosine A1 Receptor Agonists
  • N(6)-(2-endo-norbornyl)adenosine
  • Norbornanes
  • Receptor, Adenosine A1
  • Xanthines
  • 1,3-dipropyl-8-cyclopentylxanthine
  • Adenosine
Topics
  • Adenosine (administration & dosage, analogs & derivatives)
  • Adenosine A1 Receptor Agonists (administration & dosage)
  • Animals
  • Cardiovascular System (drug effects)
  • Humans
  • Hyperalgesia (drug therapy, pathology)
  • Mice
  • Microglia (metabolism, pathology)
  • Motor Activity (drug effects)
  • Neuralgia (drug therapy)
  • Neuroglia (metabolism, pathology)
  • Norbornanes (administration & dosage)
  • Receptor, Adenosine A1 (metabolism)
  • Sciatic Nerve (drug effects, injuries)
  • Xanthines (administration & dosage)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: