The antinociceptive activity of κ- but not δ-opioid receptor agonists is maintained in morphine-tolerant neuropathic rats
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Cited by (24)
Endomorphin analog analgesics with reduced abuse liability, respiratory depression, motor impairment, tolerance, and glial activation relative to morphine
2016, NeuropharmacologyCitation Excerpt :Interestingly, analogs 1, 3 and 4 showed high efficacy delta antagonism at sub-micromolar concentrations. In vivo selectivity was also demonstrated: Fig. 1c shows that antinociceptive effects of all four analogs were significantly blocked by naloxone (1 mg/kg), but not by antagonists for DOR (NTI) or KOR (nor-BNI) at doses (1 mg/kg) known to antagonize selective agonists for those receptors after i.v. injection in the rat (Catheline et al., 1996; Desmeules et al., 1993). The EM analogs showed favorable solubility (40, 20, 20 and 50 mg/ml in water, 15, 15, 12, and 20 mg/ml in saline, and 90, 70, 50, and 50 mg/ml in 20% PEG400/saline for analogs 1–4 respectively), and stable plasma half-life in vitro.
Effects of U-69,593, a κ-opioid receptor agonist, on carrageenin-induced peripheral oedema and Fos expression in the rat spinal cord
1999, European Journal of Pharmacology
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