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ICI 174864: A highly selective antagonist for the opioid Δ-receptor

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  • Peripheral analgesia: Hitting pain where it hurts

    2011, Biochimica et Biophysica Acta - Molecular Basis of Disease
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    The selective KOR agonist U50488 reduced nociceptor spontaneous activity in acutely inflamed cat knee joints [108] as well as reducing pain behaviour in Freund's complete adjuvant inflamed paws [109]. Confirmation that U50488 was producing antihyperalgesia via KORs was indicated by the blocking effects of the KOR antagonist nor-BNI [110] but not the MOR antagonist CTAP [111] nor the DOR antagonist ICI174864 [112]. The synthetic DOR agonist DPDPE has been found to be antihyperalgesic when injected locally into the inflamed rat hindpaw [109] and when administered around the primary tumour site in an animal model of bone cancer pain [113].

  • Endogenous opioids and feeding behavior: A 30-year historical perspective

    2004, Peptides
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    Whereas BFNA was characterized as a short-term kappa agonist and irreversible mu antagonist [391,475,508], the irreversible though selective antagonist, naloxonazine acted at the high-affinity mu-1 receptor that binds opiates and most enkephalins with similar high affinities [177]. The development of delta antagonists began with ICI174864 that acts as a selective, short-term delta antagonist [105], albeit degrading into a peptide with mu agonist activity [90]. DALCE was then developed as a short-acting delta-1 agonist that covalently binds with the receptor acting long-term as an antagonist [50].

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