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A Modified Inflammatory Pain Model to Study the Analgesic Effect in Mice
Published on: November 15, 2024
[Comparative analysis of analgesic activities of dermorphin, [DPro6]-dermorphin, and their C-terminal tripeptides]
Abstract:
Analgesic activities of dermorphin (DM), [DPro6]-DM, and their C-terminal tripeptides were comparatively studied. Analgesic activity was evaluated in tail flick, hot plate, tail pinch, formalin, and acetic acid writhing tests describing different levels of organization of pain sensitivity. Intraperitoneal administration of the peptides decreased the pain threshold in all these tests. The C-terminal tripeptides DM(5-7) and [DPro6]-DM(5-7) demonstrated analgesics activity comparable or sometimes higher than that of the full-length molecules. The effect of DM, [DPro6]-DM, and C-terminals fragments DM(5-7) and [DPro6]-DM(5-7) decreased after co-administration with naloxone, which points to the opioid nature of analgesic activity of the peptides.
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Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...

