Abstract | BACKGROUND: METHODS: The screening study included acute tissue injury, chronic constriction injury (CCI), and spinal nerve ligation (SNL) models of neuropathic pain. RESULTS: All of the tested compounds sup-pressed the acetic acid-induced writhing response significantly in comparison to the control. In particular, compound JVP-8 was observed to be the most active compound with percent inhibition greater than that of the standard drug aspirin (97.8% inhibition of writhing response as against 97.0% shown by aspirin). In neuropathic pain studies, compound JVP-5 (100 mg/kg i.p.) emerged as the most active compound affording maximum protection against dynamic allodynia and mechanical hyperalgesia in the CCI model, and against spontaneous pain and mechanical hyperalgesia in SNL rats. CONCLUSION: In this study, we have demonstrated that combining phthalimide pharmacophore with GABA has evolved compounds effective for the treatment of neuropathic pain.
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Authors | Perumal Yogeeswari, Jegadeesan Vaigunda Ragavendran, Dharmarajan Sriram, Ramkumar Kavya, Kaliappan Vanitha, Harshini Neelakantan |
Journal | Pharmacology
(Pharmacology)
Vol. 81
Issue 1
Pg. 21-31
( 2008)
ISSN: 1423-0313 [Electronic] Switzerland |
PMID | 17785996
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | (c) 2008 S. Karger AG, Basel. |
Chemical References |
- Analgesics
- Phthalimides
- gamma-Aminobutyric Acid
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Topics |
- Analgesics
(chemistry, therapeutic use)
- Animals
- Disease Models, Animal
- Female
- Hyperalgesia
(drug therapy, metabolism)
- Male
- Mice
- Molecular Structure
- Neuralgia
(drug therapy, metabolism)
- Pain Measurement
- Phthalimides
(chemistry, therapeutic use)
- Rats
- Rats, Wistar
- Sciatic Nerve
(injuries)
- Spinal Nerves
(injuries)
- Structure-Activity Relationship
- gamma-Aminobutyric Acid
(analogs & derivatives, therapeutic use)
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