| Description: |
Syrosingopine has selective depleting effect on brain amines is potentiated by combined treatment with disulfiram or fusaric acid, a dopamine beta-hydroxylase inhibitor. Syrosingopine can sensitize cancer cells to metformin and its more potent derivative phenformin far below the individual toxic threshold of each compound, thus, combining syrosingopine and codrugs is a promising therapeutic strategy for clinical application for the treatment of cancer.Syrosingopine also has hypotensive properties. |
| Targets: |
HCV | Antifection | Androgen Receptor | Histone Methyltransferase | NF-kB | Mdm2 |
| In vitro: |
| Sci. Adv.,2016 Dec; 2(12): e1601756. | | Syrosingopine sensitizes cancer cells to killing by metformin[Pubmed: 28028542] |
METHODS AND RESULTS:
We report that the anticancer activity of the widely used diabetic drug metformin is strongly potentiated by Syrosingopine. Synthetic lethality elicited by combining the two drugs is synergistic and specific to transformed cells. This effect is unrelated to Syrosingopine’s known role as an inhibitor of the vesicular monoamine transporters. Syrosingopine binds to the glycolytic enzyme α-enolase in vitro, and the expression of the γ-enolase isoform correlates with nonresponsiveness to the drug combination. Syrosingopine sensitized cancer cells to metformin and its more potent derivative phenformin far below the individual toxic threshold of each compound.
CONCLUSIONS:
Thus, combining Syrosingopine and codrugs is a promising therapeutic strategy for clinical application for the treatment of cancer. | | C R Seances Soc Biol Fil. 1960;154:55-7. | | Hypertensive action of syrosingopine after ephedrine.[Pubmed: 14443141] |
METHODS AND RESULTS:
Hypertensive action of syrosingopine after ephedrine. |
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| In vivo: |
| Pharmacol Biochem Behav. 1986 May;24(5):1457-9. | | Effects of amnesic doses of reserpine or syrosingopine on mouse brain acetylcholine levels.[Pubmed: 2873591] |
The effects of reserpine and syrosingopine on mouse whole brain acetylcholine levels were examined.
METHODS AND RESULTS:
At 2 or 24 hr following injection, the brains were removed and analyzed by mass spectrometry. No differences were found between drug-treated and control mice in the acetylcholine content of the brain at either time interval.
CONCLUSIONS:
The results suggest that whole brain acetylcholine levels do not predict the amnesic effects of either reserpine or syrosingopine. | | Behav Neural Biol. 1983 May;38(1):120-6. | | The effect of reserpine, syrosingopine, and guanethidine on the retention of discriminated escape reversal: peripherally administered catecholamines cannot reverse the reserpine amnesia in this situation.[Pubmed: 6138025] |
METHODS AND RESULTS:
In a series of experiments, the effects of reserpine, syrosingopine, and guanethidine on retention of a discriminated escape reversal training were investigated in mice. The peripherally and centrally acting reserpine produced amnesia while the primarily peripherally acting compounds, syrosingopine or guanethidine, did not produce amnesia even when given in high dosages or when training was given with low footshock.
CONCLUSIONS:
Unlike in the passive avoidance situation, peripherally administered norepinephrine or dopamine was not able to attenuate the reserpine-induced amnesia. The results were discussed in terms of the role of biogenic amines in memory formation. |
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