TAN-67 dihydrobromide

TAN-67 (SB-205607) dihydrobromide is a potent and selective nonpeptidic δ-opioid receptor agonist with a Ki value of 0.647 nM. TAN-67 dihydrobromide has neuroprotective effect. TAN-67 dihydrobromide can be used in research of ischemic stroke.

TAN-67 (SB-205607) dihydrobromide has high potency (EC₅₀=1.72 nM) for the inhibition of forskolin-stimulated cAMP accumulation at human delta-opioid receptors expressed by intact Chinese hamster ovary cells but low potency (EC₅₀=1520 nM) at human mu-opioid receptors expressed by intact B82 mouse fibroblast cells^[1].

TAN-67 (SB-205607; 1.5-4.5 mg/kg; i.v.; once) dihydrobromide reduces infarct volume in I/R-caused brain injury^[2].
TAN-67 (3 mg/kg; i.v.; once) dihydrobromide improves survival and neurobehavioral performance after I/R^[2].
TAN-67 (3 mg/kg; i.v.; once; adult C57BL/6J male mice) dihydrobromide increases both total APP and mature APP (APPm) levels and APP processing at an early time point (6 h)^[2].

References:
[1]. Knapp RJ, et, al. Properties of TAN-67, a nonpeptidic delta-opioid receptor agonist, at cloned human delta- and mu-opioid receptors. Eur J Pharmacol. 1995 Oct 15;291(2):129-34.
[2]. Min JW, et, al. The non-peptidic δ-opioid receptor agonist Tan-67 mediates neuroprotection post-ischemically and is associated with altered amyloid precursor protein expression, maturation and processing in mice. J Neurochem. 2018 Feb;144(3):336-347.