Regular paperAntinociceptive effects of the selective non-peptidic δ-opioid receptor agonist TAN-67 in diabetic mice
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2022, Bioorganic and Medicinal Chemistry LettersCitation Excerpt :Meanwhile, ligands with selective agonistic activity on DOR or KOR are expected to be used as analgesics without addiction. We previously designed and synthesized the DOR selective agonist, (±)-TAN-67 (1), in the course of the development of addiction-free opioid analgesics.2,3 Unexpectedly, this compound did not show potent analgesic effect in vivo in spite of the potent DOR agonist activity in vitro.4
Zebrafish models relevant to studying central opioid and endocannabinoid systems
2018, Progress in Neuro-Psychopharmacology and Biological PsychiatryInvolvement of delta opioid receptors in alcohol withdrawal-induced mechanical allodynia in male C57BL/6 mice
2016, Drug and Alcohol DependenceDOR<inf>2</inf>-selective but not DOR<inf>1</inf>-selective antagonist abolishes anxiolytic-like effects of the δ opioid receptor agonist KNT-127
2014, NeuropharmacologyCitation Excerpt :These results were consistent with our previous report with mice acetic acid test (Saitoh et al., 2011). In addition, another study also showed that the antinociceptive effects of a selective DOR agonist TAN-67 were abolished by pretreatment with BNTX, but not with NTB in the mice acetic acid writhing test and tail flick test (Kamei et al., 1995). Taken together, these results suggest that BNTX sensitive DOR1 subtype play important roles in the antinociceptive effects of DOR agonists in the inflammatory pain responses.
Novel δ1-receptor agonist KNT-127 increases the release of dopamine and l-glutamate in the striatum, nucleus accumbens and median pre-frontal cortex
2012, NeuropharmacologyCitation Excerpt :Furthermore, no ESR signal was generated from dialysate, even at high KNT-127 concentration (1–100 nM) (data not shown). The δ-receptor is recognized as a novel neurotransmitter system that may be directly involved in neuropsychiatric disorders, i.e., chronic pain, schizophrenia, Parkinson’s disease, anxiety and mood disorders (Broom et al., 2002; Chang et al., 1993; Cryan et al., 2002; Kamei et al., 1995; Saitoh et al., 2011); however, peptide δ-receptor agonists cannot fully penetrate the blood–brain barrier (Nagase et al., 2010). Therefore, a number of small-molecular non-peptide δ-receptor agonists have become available for experimental use; they comprise compounds of different structures, such as the isoquinoline derivatives (TAN-67 and KNT-127) (Nagase et al., 2010, 2001) and the benzhydryl piperazine derivatives (SNC80 and BW373U86) (Bilsky et al., 1995; Chang et al., 1993).