Neamine and 2-deoxystreptamine neomycin derivatives exhibit antinociceptive activity in rat models of phasic, incision and neuropathic pain
| Autor: | Ivone Carvalho, Wiliam A. Prado, Luis Otávio B. Zamoner, A.C. Rossaneis, A.P. Corrado |
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| Rok vydání: | 2015 |
| Předmět: |
Male
Nociception Pain Threshold Time Factors Pharmaceutical Science Pharmacology Nociceptive Pain Structure-Activity Relationship Threshold of pain medicine Reaction Time Animals Rats Wistar ED50 Neamine Injections Spinal Pain Measurement Analgesics Pain Postoperative Dose-Response Relationship Drug Molecular Structure Chemistry Antagonist Hexosamines Neomycin ESTÍMULOS Disease Models Animal Allodynia Neuropathic pain Neuralgia medicine.symptom medicine.drug Framycetin |
| Zdroj: | Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual) Universidade de São Paulo (USP) instacron:USP |
| Popis: | Objectives To assess the antinociceptive activity of the neomycin derivatives neamine and 2-deoxystreptamine following intraspinal administration in rats. Methods We used the tail-flick test and measured the threshold to mechanical stimulation in models of incisional and neuropathic pain. Key findings The derivatives produced antinociception in the tail-flick test and reduced mechanical allodynia in models of incisional and neuropathic pain. The approximate ED50 in milligrams (confidence limits in parenthesis) in these tests were 1.35 mg (0.61; 2.95), 0.20 mg (0.14; 0.27) and 0.28 mg (0.12; 0.63) for neamine, and 1.05 mg (0.68; 1.60), 0.78 mg (0.776; 0.783) and 0.79 mg (0.46; 1.34) for 2-deoxystreptamine, respectively. Neamine was more potent than 2-deoxystreptamine in the incisional and neuropathic pain models, but they had similar potency in the tail-flick test. Tetra-azidoneamine, a neamine derivative in which free amino groups are replaced with azido groups, did not change the incisional mechanical allodynia. The reduction of incisional allodynia by neamine and 2-deoxystreptamine was transitorily antagonized by intrathecal administration of calcium chloride. Conclusions The intraspinal administration of neamine and 2-deoxystreptamine is antinociceptive in rats. The presence of amino groups in the structure of these derivatives is fundamental to their antinociceptive effect, which may be due to a calcium antagonist activity. |
| Databáze: | OpenAIRE |
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