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GREEN ORANGE

Green Orange which is made from the peal of immature common oranges, deliver a mild stimulating effect that enhances response rate and reaction time.

Kim KW, Kim HD, Jung JS, Woo RS, Kim HS, Suh HW, Kim YH, Song DK. Characterization of antidepressant-like effects of p-synephrine stereoisomers. Naunyn Schmiedebergs Arch Pharmacol 2001 Jul;364(1):21-6. Department of Pharmacology, Chonbuk National University Medical School, Institute for Medical Sciences, Chonchu, South Korea. 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 microM vs. 13.5 +/- 1.2 microM) and [3H]nisoxetine binding (Ki 4.5 +/- 0.5 microM vs. 8.2 +/- 0.7 microM). 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 microM vs. EC50 12.3 +/- 0.9 microM). The stimulatory effect of R-(-)-p-synephrine on [3H]noradrenaline release was inhibited by nisoxetine (100 nM), but tetrodotoxin (1 microM) 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.

Suzuki O, Matsumoto T, Oya M, Katsumata Y, Oxidation of synephrine by type A and type B monoamine oxidase. Experientia 1979 Oct 15;35(10):1283-1284. Synephrine (SP) was found to be a substrate for monoamine oxidase (MAO) in rat brain mitochondria, showing the Km and Vmax values of 250 microM and 32.6 nmoles/mg of protein/30 min respectively. The inhibition studies showed that the SP oxidation was carried out by both type A and type B MAO and a major part of the activity was due to type A MAO.

Hengstmann JH, Aulepp H. [Pharmacokinetics and metabolism of 3H-synephrine (author's transl)] [Article in German] Arzneimittelforschung 1978;28(12):2326-31. The physiological disposition of 1-(4-hydroxyphenyl)-2-methylamino-ethanol-tartrate (synephrine, Sympatol) in man had not been investigated to date. Therefore, we studied pharmacokinetics and metabolism of tritiated synephrine in man. Following short i.v. infusion in six patients about 80% of the administered radioactivity was recovered in urine. Two-thirds of the urinary tritium activity consisted of the deaminated p-hydroxymandelic acid. 10% were excreted as unchanged synephrine only. Following oral ingestion in ten patients the total urinary radioactivity was quite comparable to the i.v. experiments. Therefore, complete enteric absorption has to be stated. The amount of unchanged synephrine amounted, however, only to 2.5% of the dose. The resulting bioavailability has to be calculated to 22% only. The pharmacokinetic parameters are quite comparable to the sympathomimetics similar in structure. The biological half-life was about 2 h. After oral ingestion absorption was fast, the peak concentrations were observed between 1 and 2 h after administration.