Sea foraminifen is the active ingredient of St. John's Wort. It has been used in studies of depression, is known to indirectly inhibit serotonin and norepinephrine reuptake at synapses, and has recently been found to work through direct activation of TRPC6. TRPC6 is a member of the typical transient receptor potential (TRPC) ion channel family. DAG is an endogenous activator of this pathway, and Hyperperforin is the only known selective activator of TRPC6. Although it is widely used, its chemical properties are unstable. Efforts to find a stable but pharmacologically similar activator of TRPC6 resulted in the discovery of a simplified phloroglucinol derivative Hyp9. Like hypericin, hypericin 9 inhibits serotonin reuptake and induces neurite growth. It increases the entry of calcium ions into the cell, selectively increasing the current through the TRPC6 channel.
Molecular Weight | 322.4 |
Formula | C18H26O5 |
CAS Number | 3118-34-1 |
Solubility (25°C) | DMSO: ≥20 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[5] Dominique Yang, et al. Molecular mechanisms involved in LH release by the ovine pituitary cells
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