Abstract.
We previously reported that p-synephrine has antidepressant-like activity in the murine models of forced swimming and tail suspension. In the present study, we characterized antidepressant-like effects of p-synephrine stereoisomers in both in vivo and in vitro systems. In the tail suspension test, S-(+)-p-synephrine (3 mg/kg, p.o.) reduced the duration of immobility, while R-(-)-p-synephrine (0.3–3 mg/kg, p.o.) had no effect. S-(+)-p-synephrine (0.3, 1 and 3 mg/kg, p.o.) and R-(-)-p-synephrine (1 mg/kg and 3 mg/kg, p.o.) significantly reversed the reserpine (2.5 mg/kg, i.p.)-induced hypothermia. S-(+)-p-synephrine was more effective than R-(-)-p-synephrine in inhibition of both [3H]noradrenaline uptake in rat cerebral cortical slices (maximal inhibition 85.7±7.8% vs. 59.8±4.3%; EC50 5.8±0.7 µM vs. 13.5±1.2 µM) and [3H]nisoxetine binding (K i 4.5±0.5 µM vs. 8.2±0.7 µM). In contrast, R-(-)-p-synephrine was more effective than S-(+)-p-synephrine in stimulation of [3H]noradrenaline release from rat cerebral cortical slices (maximal stimulation 23.9±1.8% vs. 20.1±1.7%; EC50 8.2±0.6 µM vs. EC50 12.3±0.9 µM). The stimulatory effect of R-(-)-p-synephrine on [3H]noradrenaline release was inhibited by nisoxetine (100 nM), but tetrodotoxin (1 µM) and elimination of extracellular calcium had no effect. It is suggested that S-(+)-p-synephrine has more effective antidepressant-like activity than R-(-)-p-synephrine.
Similar content being viewed by others
Author information
Authors and Affiliations
Additional information
Electronic Publication
Rights and permissions
About this article
Cite this article
Kim, KW., Kim, HD., Jung, JS. et al. Characterization of antidepressant-like effects of p-synephrine stereoisomers. Naunyn-Schmied Arch Pharmacol 364, 21–26 (2001). https://doi.org/10.1007/s002100100416
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/s002100100416