Analgesic Properties of Opioid/NK1 Multitarget Ligands with Distinct in Vitro Profiles in Naive and Chronic Constriction Injury Mice.
Model: Chronic constriction injury of the sciatic nerve after Bennett and Xie: three 4/0 silk ligatures placed around the nerve distal to the sciatic notch at 1 mm spacing under isoflurane anaesthesia
In naive mice the pure opioid parents gave near 100 per cent maximum possible effect on tail-flick whereas hybrids reached only about 60 to 70 per cent. Under neuropathic conditions the opioid parents largely lost efficacy while the best hybrid produced close to 100 per cent maximum possible effect…
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