Hiperforina

Hiperforina Uses, Dosage, Side Effects, Food Interaction and all others data.

Hiperforina is a phytochemical generated by the plants of the Hypericum family. One of the most important members of this family, due to its medical properties, is Hypericum perforatum, also known as St John's wort.

Hiperforina is believed to be the primary active constituent responsible for the antidepressant and anxiolytic properties of the extracts of St. John's wort. It acts as a reuptake inhibitor of monoamines, including serotonin, norepinephrine, dopamine, and of GABA and glutamate, with IC50 values of 0.05-0.10 mcg/ml for all compounds, with the exception of glutamate, which is in the 0.5 mcg/ml range. It appears to exert these effects by activating the transient receptor potential ion channel TRPC6. Activation of TRPC6 induces the entry of sodium and calcium into the cell which causes inhibition of monoamine reuptake. Hiperforina is also thought to be responsible for the induction of the cytochrome P450 enzymes CYP3A4 and CYP2C9 by binding to and activating the pregnane X receptor (PXR).

Trade Name Hiperforina
Generic Hyperforin
Hyperforin Other Names Hiperforina, Hyperforine
Type
Formula C35H52O4
Weight Average: 536.797
Monoisotopic: 536.386560154
Groups Nutraceutical
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Hiperforina
Hiperforina

How Hiperforina works

Hiperforina is believed to be the primary active constituent responsible for the antidepressant and anxiolytic properties of the extracts of St. John's wort. It acts as a reuptake inhibitor of monoamines, including serotonin, norepinephrine, dopamine, and of GABA and glutamate, with IC50 values of 0.05-0.10 mcg/ml for all compounds, with the exception of glutamate, which is in the 0.5 mcg/ml range. It appears to exert these effects by activating the transient receptor potential ion channel TRPC6. Activation of TRPC6 induces the entry of sodium and calcium into the cell which causes inhibition of monoamine reuptake.

Toxicity

Oral LD50 (rat):5628 mg/kg; Skin LD50 (rabbit): 15800 mg/kg; Subcutaneous LD50 (mouse):9800 mg/kg; Intraperitoneal LD50 (rabbit):1826 mg/kg

Half Life

9 hours

Innovators Monograph

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*** Taking medicines without doctor's advice can cause long-term problems.
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