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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
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
- Source :
- Molecules; Volume 17; Issue 12; Pages: 13712-13726, Molecules
- Publication Year :
- 2012
- Publisher :
- MDPI AG, 2012.
-
Abstract
- This study was undertaken in order to investigate the effect of chronic treatment with 5#8242;-chloro-5#8242;-deoxy-(#177;)-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#8242;-chloro-5#8242;-deoxy-(#177;)-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#8242;-chloro-5#8242;-deoxy-(#177;)-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#8242;-chloro-5#8242;-deoxy-(#177;)-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.
- Subjects :
- Agonist
SNi
Adenosine
glia
medicine.drug_class
Pharmaceutical Science
Motor Activity
Pharmacology
Adenosine receptor antagonist
Cardiovascular System
Article
Analytical Chemistry
Mice
A1 adenosine receptor
neuropathic pain
allodynia
Drug Discovery
medicine
Animals
Humans
Physical and Theoretical Chemistry
Receptor, Adenosine A1
business.industry
Organic Chemistry
Nerve injury
Norbornanes
Sciatic Nerve
Adenosine A1 Receptor Agonists
Nociception
Allodynia
Hyperalgesia
Chemistry (miscellaneous)
Xanthines
Anesthesia
Neuropathic pain
Neuralgia
Molecular Medicine
Microglia
Sciatic nerve
medicine.symptom
business
Neuroglia
Subjects
Details
- ISSN :
- 14203049
- Volume :
- 17
- Database :
- OpenAIRE
- Journal :
- Molecules
- Accession number :
- edsair.doi.dedup.....e2df52c056da9e23aa05dc773280ead5
- Full Text :
- https://doi.org/10.3390/molecules171213712