Forskolin

A diterpene compound from the Coleus forskohlii plant that directly activates adenylate cyclase, increasing intracellular cAMP levels. cAMP is a critical second messenger in neuronal signaling — elevated cAMP enhances long-term potentiation, supports memory consolidation, and increases the sensitivity of neurotransmitter receptors. Also used for thyroid support and body composition.

Dosage

Standard: 250 mg Coleus forskohlii extract (standardized to 10% forskolin = 25 mg forskolin) twice daily. Higher forskolin concentrations (20%) available. Take with food. May cause blood pressure reduction — start low if hypotension-prone.

Dosages shown are for research reference only. Always consult a qualified healthcare provider.

Half-Life

4-6 hours

Administration

Oral (capsules). Coleus forskohlii extract standardized to 10-20% forskolin.

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Mechanism of Action

Forskolin directly activates all nine isoforms of membrane-bound adenylate cyclase (AC1-9), the enzyme that converts ATP to cyclic AMP (cAMP), bypassing G-protein-coupled receptor activation. Elevated cAMP activates protein kinase A (PKA), which phosphorylates CREB (cAMP response element-binding protein) at Ser133 — a transcription factor essential for long-term memory formation that induces expression of BDNF, c-fos, and other plasticity-related genes. This is the same signaling cascade used by dopamine (D1), norepinephrine (beta-adrenergic), and serotonin (5-HT4/7) receptors, but forskolin activates it directly at the effector level. Elevated cAMP also increases neurotransmitter receptor sensitivity (e.g., beta-adrenergic receptor phosphorylation), enhances synaptic plasticity via PKA-mediated GluA1 phosphorylation, and potentiates L-type calcium channels. Forskolin may also activate TRPV channels.

Regulatory Status

Dietary supplement. Available OTC worldwide. Not FDA-approved for any medical condition.

Risks & Safety

Common

Diarrhea, low blood pressure, increased heart rate, headache.

Serious

Significant blood pressure reduction — avoid with hypotension or blood pressure medications.

Rare

Tremor, restlessness, bleeding risk.

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Research Papers

10
Forskolin: upcoming antiglaucoma molecule.

Published: October 1, 2012

AI Summary

Recently, its Ophthalmic inserts and in situ gels for sustained and delayed-release drug delivery systems were tested in New Zealand Albino Rabbits for its antiglaucoma efficacy. This drug review explains Forskolin as a drug, its antiglaucoma potential and recent findings of forskolin as an antiglaucoma agent.

Progress in heterologous biosynthesis of forskolin.

Published: April 29, 2021

AI Summary

Forskolin, a class of labdane-type diterpenoid, has significant medicinal value in anticancer, antiasthmatic, antihypertensive, and heart-strengthening treatments. In recent years, the construction of microbial cell factories to produce medicinal natural products via synthetic biological methods has effectively solved the current problems and is...

Forskolin alleviates cisplatin-induced acute renal toxicity in rats.

Published: July 14, 2022

AI Summary

Renal toxicity correlated with cisplatin administration curbs its clinical application. Accordingly, the identification of novel protective agents is important.

Forskolin: a unique diterpene activator of cyclic AMP-generating systems.

Published: December 31, 1980

AI Summary

Activation of adenylate cyclase by forskolin results in marked increases in levels of intracellular cyclic AMP in a variety of eukaryotic cells. Low concentrations of forskolin which alone elicit small increases in intracellular cyclic AMP greatly potentiate hormonal activation of adenylate cyclase in a number of intact cells.

Forskolin: a specific stimulator of adenylyl cyclase or a diterpene with multiple sites of action?

Published: October 31, 1989

AI Summary

More recently, forskolin has been shown to inhibit a number of membrane transport proteins and channel proteins through a mechanism that does not involve the production of cAMP. Many of these channel proteins are predicted to have similar topographies in the membrane bilayer and it is tempting to speculate that forskolin may be binding at struct...

Forskolin Induces Endocrine Disturbance in Human JEG-3 Placental Cells.

Published: June 29, 2022

AI Summary

We observed that forskolin activated P2X7 receptors and disturbed estradiol, progesterone, hPL and hyperglycosylated hCG secretion in human placental JEG-Tox cells. To the best of our knowledge, we highlighted, for the first time, that forskolin induced endocrine disturbance in placental cells.

Forskolin effects on the cAMP system and steroidogenesis in the immature rat ovary.

Published: October 31, 1983

AI Summary

The diterpene forskolin was found to activate the adenylate cyclase system in intact tissue and membrane preparations of the immature rat ovary. The presence of 8-bromo-cAMP (brcAMP) in the preincubation medium reduced the subsequent hormone response.

Forskolin, adenylate cyclase, and cell physiology: an overview.

Published: December 31, 1983

AI Summary

Its use has revealed further subtleties to the control of cyclic AMP generation by adenylate cyclase in both solubilized and membrane preparations and in intact cells. Clinical applications of forskolin as a hypotensive, spasmolytic, lipolytic, or antithrombotic agents or for the treatment of glaucoma or cardiac insufficiency remain other challe...

[Recent advances in biosynthesis of forskolin].

Published: August 6, 2020

AI Summary

In this paper, the structure, activity, biosynthetic pathway and the heterologous biosynthesis of forskolin were reviewed. The problems and solutions in the heterologous biosynthesis of forskolin were also discussed and summarized, which will provide references for the construction of high-yielding forskolin engineering strains.

Forskolin Improves Male Reproductive Complications Caused by Hyperglycemia in Type 2 Diabetic Rats.

Published: August 6, 2023

AI Summary

In many diabetic patients, spermatogenesis complications are frequent causing infertility problems. This study aimed to demonstrate the effect of Forskolin on male reproductive dysfunction caused by type 2 diabetes.

Frequently Asked Questions

What is Forskolin used for?

A diterpene compound from the Coleus forskohlii plant that directly activates adenylate cyclase, increasing intracellular cAMP levels. cAMP is a critical second messenger in neuronal signaling — elevated cAMP enhances long-term potentiation, supports memory consolidation, and increases the sensitivity of neurotransmitter receptors. Also used for thyroid support and body composition.

What are the side effects of Forskolin?

Common: Diarrhea, low blood pressure, increased heart rate, headache. Serious: Significant blood pressure reduction — avoid with hypotension or blood pressure medications. Rare: Tremor, restlessness, bleeding risk.

How is Forskolin administered?

Forskolin is administered via oral (capsules). coleus forskohlii extract standardized to 10-20% forskolin..

What is the half-life of Forskolin?

The half-life of Forskolin is 4-6 hours.

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