European Journal of Pharmacology: Molecular Pharmacology
Properties of TAN-67, a nonpeptide δ-opioid receptor agonist, at cloned human δ-and μ-opioid receptors
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Activation of peripheral δ<inf>2</inf>-opioid receptor prevents reperfusion heart injury
2021, European Journal of PharmacologyCitation Excerpt :These data were confirmed by other investigators (Zeng et al., 2011), who found that TAN-67 at dose of 10 mg/kg prevents ischemia/reperfusion injury of the heart via opioid δ1-receptor stimulation. The use of such a high dose by both groups of investigators was surprising because TAN-67 exhibits a high affinity for opioid δ-receptor (Knapp et al., 1995; Gross, 2003). We hypothesize that the infarct sparing effect of TAN-67 may involve the activation of central opioid δ1-receptor(s) because of the limited passage through the blood-brain barrier, therefore, such a high dose of the drug was required.
Research and development of κ opioid receptor agonists and δ opioid receptor agonists
2020, Pharmacology and TherapeuticsCitation Excerpt :The (±)-TAN-67 produced an NTI-reversible inhibitory effect on the contraction of mouse vas deferens with an IC50 value of 6.61 nM, suggesting that the (±)-TAN-67 showed agonistic activity via the DOP. The (±)-TAN-67 also showed a robust agonistic activity (EC50 = 1.72 nM) for the inhibition of forskolin-stimulated cAMP accumulation at the human DOP expressed by intact Chinese hamster ovary (CHO) cells, but low potency (EC50 = 1520 nM) at the human MOP receptor expressed by intact B82 mouse fibroblast cells (Knapp et al., 1995). These in vitro results from assays using human DOPs and MOPs showed that the (±)-TAN-67 has a similar binding affinity, selectivity, and potency as DPDPE, a representative prototype peptidic DOP ligand (Knapp et al., 1995).
The delta opioid receptor tool box
2016, NeuroscienceCitation Excerpt :Indeed, no analgesic effects to ARM390 were observed in the lactic acid-induced stretching assay in rats after its intraperitoneal administration (Negus et al., 2012). TAN-67 is a morphinan derivative with high selectivity for the delta opioid receptor (Knapp et al., 1995). Although the racemic (+/−)-TAN-67 showed no analgesic activity, its enantiomer (−)-TAN-67 is highly effective (Nagase et al., 2001).
Kappa and delta opioid receptor signaling is augmented in the failing heart
2009, Journal of Molecular and Cellular CardiologyCitation Excerpt :Fentanyl, concentrations were between 100 pM and 10 μM. Agonist concentrations were based on receptor selectivity [13,14] to assure that drugs would act preferentially at the desired receptor. In addition, preliminary concentration response curves were performed to insure an effective range of concentrations.
Pharmacological profiles of selective non-peptidic δ opioid receptor ligands
2000, Molecular Brain ResearchThe modulatory effect of (+)-TAN-67 on the antinociceptive effects of the nociceptin/orphanin FQ in mice
1999, European Journal of Pharmacology