Forskolin-dosage

Forskolin

David Tomen
Author:
David Tomen
12 minute read
Forskolin has been shown to boost memory and learning, improve motivation and mood, and stimulate cerebral circulation

Forskolin (Coleus forskohlii) is the only known supplement to naturally boost cAMP (Cyclic Adenosine Monophosphate) in your brain. cAMP is important for neural signaling within brain cells.

As a secondary messenger in neurons, cAMP produces proteins needed for neuron and synapse growth. This process is called Long-Term Potentiation (LTP).

LTP is the process where synaptic connections get stronger in response to electrical stimulation in the brain. This process happens naturally through life experience. It’s a critical part of synaptic plasticity. And how experience is recorded through learning and memory.

Forskolin is a chemical compound extracted from Coleus forskohlii (Plectranthus barbatus), a perennial plant native to India, Burma and Thailand.

Coleus forskohlii by Dick Culbert (own work) via Wikimedia Commons
Coleus forskohlii by Dick Culbert (own work) [CC BY-SA 4.0], via Wikimedia Commons
Forskohlii has been used for millennia in traditional Ayurvedic medicine to treat heart disease, convulsions, spasms and painful urination.[i]

Forskolin is used in Western homeopathic medicine to treat allergies, skin conditions, obesity, PMS, irritable bower syndrome, urinary tract infections, bladder infections, cancer, blood clots, male infertility, insomnia and convulsions.

Some healthcare providers even use Forskolin intravenously (IV) for heart failure.

Here we’re going to explore how Forskolin benefits your brain.

Forskolin helps:

  • Neural signaling: Forskolin activates the enzyme adenylate cyclase which increases cAMP (Cyclic Adenosine Monophosphate) levels in brain cells. cAMP is a signal carrier required for intracellular communication. Increasing cAMP levels helps boost cognition, long-term memory, and alertness.
  • Cerebral Circulation: Forskolin works as a vasodilator which increases blood flow in your brain. Improved blood flow increases nutrient and oxygen delivery to brain cells.
  • Brain-Derived Neurotrophic Factor (BDNF): Forskolin stimulates the TRKb receptor which helps potentiate BDNF. Both cAMP and BDNF can activate mitogen-activated protein kinase (MAPK/ERK) which plays a role in long-term potentiation (LTP).[ii] LTP helps create long-term memory.

Overview

Forskolin is a chemical compound found in the Coleus forskohlii plant, a member of the mint family which grows as a perennial on the plains of India and lower Himalayas.

Forskolin
Forskolin

Coleus forskohlii was used in traditional Ayurvedic medicine to improve mood and for general health and wellness. As folk medicine, the herb was used to treat central nervous system disorders, problems of the heart, lung function, skin and gastrointestinal issues.

Researchers and holistic medical practitioners use the extract Forskolin to boost cerebral blood flow, lower blood pressure, treat hypertension, asthma and congestive heart failure.

As a nootropic, Forskolin is the only known supplement to naturally raise cAMP levels. Forskolin activates the enzyme adenylate cyclase which increases intracellular levels of cAMP (Cyclic Adenosine Monophosphate).[iii]

cAMP was discovered in 1956 and its production is now known to be the final common pathway for many hormones and transmitter agents.

To put this in practical perspective, hormones and neurotransmitters do not enter the cell. Instead, they activate a receptor on the cell membrane that is part of the adenylate cyclase enzyme complex.

The production of cAMP in a cell is catalyzed by this complex. The cyclic AMP (cAMP) then activates cAMP dependent protein kinase (PKA), which results in changes in the cell’s function.[iv] Based on input from the relevant hormone or neurotransmitter.

The elevation of cAMP along with PKA is required for long-term potentiation (LTP). This increase in neuroplasticity is how long-term memories are formed and encoded in your brain.

Researchers have found that increases in cAMP rapidly activates the Brain-Derived Neurotrophic Factor (BDNF) receptor TrkB and induces BDNF-dependent long-term potentiation at the Schaffer collateral-CA1 synapse in the hippocampus.[v]

In simpler terms, Forskolin boosts cAMP levels which affects long-term potentiation (LTP). LTP is an integral part of the process in developing and encoding long-term memories.

Forskolin-increases-memory

How does Forskolin work in the Brain?

Forskolin boosts brain health and function in several ways. But two in particular stand out.

  1. Forskolin enhances memory. Forskolin as a nootropic has the unique ability to activate the enzyme adenylate cyclase (AC). The activated AC enzyme then converts to cAMP (Cyclic Adenosine Monophosphate), a secondary messenger used for intracellular communication.[vi]

cAMP helps stimulate the production of CREB (cAMP response element-binding protein). An increase in CREB enhances Long-Term Potentiation (LTP).

LTP is the connection between brain synapses. Strengthening in response to stimulation by neurons on either side. A major component in both learning and memory.

Memories are stored at a cellular level. And retrieved at a cellular level. This well-travelled pathway is strengthened by boosting cAMP with Forskolin.[vii]

  1. Forskolin increases cerebral circulation. Coleus forskohlii has traditionally been used to treat hypertension (high blood pressure), congestive heart failure and angina (reduced blood flow to the heart).

Forskolin is very effective in lowering blood pressure. And scientists believe this ability to boost blood flow is related to Forskolin’s cAMP-elevating ability.

Researchers recruited 7 patients with dilated cardiomyopathy (DCM). DCM is a condition in which the heart’s ability to pump blood is decreased due to the left heart ventricle being enlarged and weakened. Forskolin administration dramatically improved left ventricle function. And increased overall cardiovascular performance.[viii]

Another group of scientists set out to study the effects of Forskolin on cerebral circulation. In this study, rabbits were anesthetized and measuring devices were attached to blood vessels entering and coming out of the brain.

The study found that Forskolin was an effective cerebral vasodilator. Enlarging blood vessels in the brain boosted blood flow. Allowing for more efficient delivery of nutrients and oxygen to brain cells.[ix]

How things go bad

Environmental factors like the food we eat, exposure to toxins, polluted air, ADHD, illness, stress and aging changes our brain chemistry.

Mood and motivation declines

Memory and recall decline

Long-term memory fades

All of these changes are contributing factors to poor quality of life. And as they progress, to neurodegenerative diseases like Alzheimer’s, dementia and Parkinson’s.

Forskolin benefits

Research from hundreds of studies, and feedback from neurohackers have shown that Forskolin can:Forskolin boosts dopamine

Forskolin is fat-soluble and quickly enters your brain after you take it. Once in your brain, it boosts cAMP activity. cAMP is involved in the Long-Term Potentiation process of preserving memories.

Forskolin combined with Artichoke extract is even more effective. Forskolin effectively boosts cAMP levels but also increases PDE4 in the brain. PDE4 is a cAMP inhibitor and will counteract increases by Forskolin if left unchecked.

Inhibiting PDE4 with Artichoke Extract, and boosting cAMP with Forskolin also potentiates dopamine release in the brain. Boosting processes in this stream of chemical reactions in the brain increases learning and memory.[x] Without the side effects of stimulating dopamine production through the use of drugs like Adderall or Ritalin.

How does Forskolin feel?

Many neurohackers report that Forskolin with Artichoke Extract improves mood. It motivates you to want to learn, and to get things done. Some say it works as good as Modafinil.Forskolin-helps-you-lose-weight-2

The general consensus is:

  • Improved long-term memory
  • Increased ability to retain information
  • Increased ability to study
  • Improved mood and motivation

Forskolin Clinical Research

Forskolin as a nootropic

cAMP responsive element binding protein (CREB) is a protein that modulates the transcription of genes. Increases in cAMP triggers the activation of CREB.

And this transcription factor is a big part of intracellular signaling. It regulates everything from the production of new sperm cells in men (spermatogenesis), to the circadian rhythms that control your sleep and awake cycles, to memory formation.

Forskolin increases cAMP which triggers the activation of CREB. Researchers have found through animal studies that CREB is required for a variety of complex forms of memory, including spatial memory and social learning.[xi]

Forskolin reduces anxiety

Benzodiazepines (Benzos) like Valium are a class of psychoactive drug used to treat anxiety, insomnia, agitation, muscle spasms, alcohol withdrawal and before medical and dental procedures to keep the patient calm.

Benzodiazepines come with a whole host of negative side effects including addiction, cognitive impairment, decreasing effectiveness (tolerance) and nasty withdrawal symptoms.

Scientists have been studying non-GABAergic substances that elevate cAMP, and have anti-anxiety activity. So they took a look at Forskolin.

In one animal study, researchers compared the effects on anxiety of Forskolin compared to diazepam (Valium). And found that Forskolin produced significant anti-anxiety activity in both stressed and unstressed animals.

Diazepam had an anti-anxiety effect on the unstressed animals. But did not work for stressed animals. The researchers noted that the anti-anxiety activity of Forskolin was accompanied by a significant elevation of cAMP levels. There’s cAMP again…

The researchers concluded that Forskolin was a better option for treating anxiety. This non-receptor mediated anti-anxiety action through cAMP elevation was preferable to the adverse reactions people get from using receptor-mediated drugs like Benzos.[xii]

Forskolin as a neuroprotectant in chemical warfare

If you ever find yourself in a warzone, you may want to have a bottle of Forskolin with you.

Acetylcholinesterase (AChE) is the primary cholinesterase in your body. This enzyme catalyzes the breakdown of acetylcholine (ACh) once ACh is used in the synaptic cleft during neurotransmission. This is how it works…

During neurotransmission, ACh is released from the first neuron into the synaptic cleft of the 2nd neuron where it binds to ACh receptors. And does its job of passing on the neural signal.

Once ACh has done its job, AChE which is also located in that synaptic cleft, steps in and breaks down acetylcholine (ACh) by liberating the choline. The liberated choline is taken up again by another neuron, and ACh is synthesized by combining the free recycled choline with Acetyl-CoA through the action of choline acetyltransferase.

Chemical warfare agents like Sarin gas, and insecticides like malathion, act to inhibit AChE. Which means they shut down this recycling process needed for acetylcholine production in the brain.

Researchers have demonstrated that Forskolin is a very effective AChE promoter. Forskolin activates AChE and up-regulates its expression.  Using mouse models, the scientists showed that Forskolin boosted AChE expression outside and inside the affected brain cells.

They concluded that Forskolin can sufficiently upregulate cellular AChE production and protect cells against chemical warfare agents like Sarin.[xiii]

Forskolin works to protect your brain from damage caused by insecticides too. So if your using an insecticide in the house or out in your garden, you may want to protect your brain by dosing with Forskolin first.

Forskolin Recommended Dosage

Recommended dosage for Forskolin is 250 mg of Coleus forskohlii at 10%, or 125 mg of Coleus forskohlii at 25%.

CILTEP Stack - Artichoke Extract + Forskolin + ALCAR + Caffeine
CILTEP Stack – Artichoke Extract + Forskolin + ALCAR + Caffeine

For boosting cAMP in a CILTEP stack: 4 mg Forskolin extract per day along with 900 mg of Artichoke Extract for PDE4 suppression.

NOTE: You will not get the full nootropic benefit of using Forskolin if you dose it on its own. Forskolin has a tendency to boost cAMP and PDE4 levels. And PDE4 suppresses cAMP. Artichoke Extract helps control PDE4.

And don’t worry about measuring out an accurate 4 mg for this CILTEP stack. I’ve been using 250 mg of Forskolin (10% ForsLean®) with 900 mg of Artichoke Extract (6%) with great success.

For counteracting Forskolin’s effect on Acetylcholinesterase: 800 mg Acetyl-L-Carnitine (ALCAR) – (200 mg of ALCAR for every 1 mg of Forskolin) per day.

Many users of this stack report it helpful to supplement with 500 mg Phenylalanine, a B-Vitamin Complex and caffeine (coffee or preferably green tea).

Forskolin Side Effects

Forskolin induces CYP3A gene expression in your liver. Which means, like grapefruit juice, Forskolin needs to be used cautiously as it will amplify the effects of other nootropics in your stack. And prescription meds.[xiv]

Acetylcholinesterase is upregulated by cAMP which makes you sleepy. This means that available Acetylcholine (ACh) in your brain drops. You can counteract this with Acetyl-l-Carnitine (ALCAR), which calms the upregulation of Acetylcholinesterase.

The most common side effect with Forskolin is diarrhea because increased cAMP affects the smooth muscle in your gastrointestinal tract. Things move through your intestines faster with Forskolin. But this side effect usually happens at much higher than recommended doses of Forskolin.

Forskolin reduces blood pressure. So if you’re on high blood pressure meds or have naturally low blood pressure you should avoid using Forskolin.

Type of Forskolin to Buy

Forskolin is usually marked as “Forskolin” or “Coleus forskohlii” on the bottle.

Forskolin typically comes in 125 mg capsules of Coleus Forskohlii (25% Forskolin), or 250 mg capsules of Coleus Forskohlii (10% Forskolin).

Look for a Coleus forskohlii or Forskolin supplement with the percentage of Forskolin extract clearly marked on the label.Forskolin-dosage

ForsLean® by Sabinsa Corporation is a branded and patented form of Coleus forskohlii that’s been used most often in human trials. So we prefer a supplement that uses ForsLean® as their source of Forskolin.

Researchers in India reported that Forskolin concentration can change significantly depending on where the Coleus forskohlii is grown.[xv] And why we prefer a standardized version like ForsLean®.

Nootropics Expert Recommendation

Forskolin Extract 125 – 250 mg per day

Nootropics Expert Tested and ApprovedI recommend using Forskolin as a nootropic supplement.

Your body does not make Forskolin on its own. So to get its benefits you must take it as a standardized supplement.

Forskolin on its own as a supplement for cognition and memory is not very effective because it increases PDE4 (a cAMP reducer) along with boosting cAMP. So the nootropic effects cancel each other out.

But Forskolin is especially helpful when combined with Artichoke Extract. It helps boost memory, increases motivation and the desire to learn. And helps improve mood while controlling anxiety.

We suggest dosing Forskolin 125 – 250 mg per day with 900 mg of Artichoke Extract taken in the morning. Stack this with at least 800 mg of ALCAR to keep your acetylcholine levels up.

We’ve also found that combining this stack with caffeine is helpful. The L-Theanine in green tea comes with the caffeine boost we need. Without the side effects of coffee.

And finally, we are making the effects of normal dopamine function more effective with this stack. It triggers the desirable downstream processes that increase learning and memory.

The chemical dynamics of the dopamine are preserved. And we don’t get the negative side effects of using a stimulant like Adderall or Ritalin.

This Forskolin/Artichoke Extract stack increases mental endurance for encoding long-term memories.

As an Amazon Associate I earn from qualifying purchases. This post may also contain other affiliate links and I will be compensated if you make a purchase after clicking on my links.

[i] Dubrey M.P., Srimal R.C., Nityanand S., Dhawan B.N. “Pharmacological studies on coleonol, a hypotensive diterpene from Coleus forskohlii” Journal of Ethnopharmacology Volume 3, Issue 1, January 1981, Pages 1-13 (source)

[ii] Patterson S.L., Pittenger C., Morozov A., Martin K.C., Scanlin H., Drake C., Kandel E.R. “Some forms of cAMP-mediated long-lasting potentiation are associated with release of BDNF and nuclear translocation of phospho-MAP kinase.” Neuron. 2001 Oct 11;32(1):123-40. (source)

[iii] Seamon K.B., Daly J.W. “Forskolin: a unique diterpene activator of cyclic AMP-generating systems.” Journal of Cyclic Nucleotide Research. 1981;7(4):201-24. (source)

[iv] Ding X., Staudinger J.L. “Induction of drug metabolism by forskolin: the role of the pregnane X receptor and the protein kinase a signal transduction pathway.” Journal of Pharmacology and Experimental Therapy. 2005 Feb;312(2):849-56. Epub 2004 Sep 30. (source)

[v] Patterson S.L., Pittenger C., Morozov A., Martin K.C., Scanlin H., Drake C., Kandel E.R. “Some forms of cAMP-mediated long-lasting potentiation are associated with release of BDNF and nuclear translocation of phospho-MAP kinase.” Neuron. 2001 Oct 11;32(1):123-40. (source)

[vi] Huang Y.Y., Li X.C., Kandel E.R. “cAMP contributes to mossy fiber LTP by initiating both a covalently mediated early phase and macromolecular synthesis-dependent late phase.” Cell. 1994 Oct 7;79(1):69-79. (source)

[vii] Cooke S.F., Bliss T.V.P. “Plasticity in the human central nervous system” Journal of Neurology May 2006 (source)

[viii] Kramer W., Thormann J., Kindler M., Schlepper M. “Effects of forskolin on left ventricular function in dilated cardiomyopathy.”Arzneimittelforschung. 1987 Mar;37(3):364-7. (source)

[ix] Wysham D.G., Brotherton A.F., Heistad D.D. “Effects of forskolin on cerebral blood flow: implications for a role of adenylate cyclase.”Stroke. 1986 Nov-Dec;17(6):1299-303. (source)

[x] Almeida L.E., Murray P.D., Zielke H.R., Roby C.D., Kingsbury T.J., Krueger B.K. “Autocrine activation of neuronal NMDA receptors by aspartate mediates dopamine- and cAMP-induced CREB-dependent gene transcription.” Journal of Neuroscience 2009 Oct 7;29(40):12702-10. (source)

[xi] Silva A.J., Kogan J.H., Frankland P.W., Kida S. “CREB and memory.” Annual Review of Neuroscience. 1998;21:127-48 (source)

[xii] Malik R., Gilhotra N. “A NOVEL NON–RECEPTOR AND NON- GABAERGIC ANTIANXIETY-LIKE ACTIVITY OF FORSKOLIN: SYNERGY WITH DIAZEPAM” International Journal of Pharmacy and Pharmaceutical Sciences Vol. 7, Issue 2. 2015 (source)

[xiii] Curtin B.F., Pal N., Gordon R.K., Nambiar M.P. “Forskolin, an inducer of cAMP, up-regulates acetylcholinesterase expression and protects against organophosphate exposure in neuro 2A cells.”Molecular and Cellular Biochemistry. 2006 Oct;290(1-2):23-32 (source)

[xiv] Ding X., Staudinger J.L. “Induction of drug metabolism by forskolin: the role of the pregnane X receptor and the protein kinase a signal transduction pathway.” International Journal of Pharmacology and Experimental Therapy. 2005 Feb;312(2):849-56. Epub 2004 Sep 30. (source)

[xv] Tamboli E.T., Singh M., Kamal Y.T., Garg M., Parveen R., Mujeeb M., Ahmad S. “Metabolic diversity in Coleus forskohlii Briq. of Indian subcontinent.” Natural Product Research. 2013;27(19):1737-42 (source)

Subscribe to the Nootropics Expert newsletter

Keep up to date with the latest developments in the nootropics space.

Head First 2nd Editon

The Award Winning Guide to Healing & Optimizing Your Brain with Nootropic Supplements.

Head First 2nd Edition

NEW! Eliminate Brain Fog, Low Energy, Moodiness, Difficulty Sleeping, Memory Loss or Anxiety. Available on Amazon, Barnes & Noble, Apple Books, Walmart and more...



Where to Buy Nootropics

Wondering where to buy the best nootropic supplements? Well, you’re in the right place. Because here you will find the nootropic supplements that I personally use and recommend. Each supplement has a link to the company store and product that I use. I also include a link to my full review for each supplement here […]

The Definitive Guide to Nootropics

Nootropics can help increase your memory, boost learning ability, improve your mood and assist overall brain function. If you’re new to nootropics, or wonder about the difference between a nootropic and a smart drug, then this page is for you. Here you’ll find the definition of a nootropic, how to pronounce the word “nootropic”, the […]

The Most Comprehensive Nootropics List

This is our big list of the most popular Nootropics in use today. Here you’ll learn what each nootropic is, what it does and suggested dosages. What is this List of Nootropics About? Nootropic supplements are cognitive enhancers aiming to improve brain function. Whether you are looking to treat mild cognitive impairment, improve mental focus, or biohack […]



Free Secrets of the Brain 3rd Edition

Get “Secrets of the Optimized Brain,” 92 nootropics to help you plan your Nootropic Stack when you sign up for my newsletter:

Join The Discussion - 107 comments

Deborah Nelson
November 8, 2020

Thank you so much for the information. I started with 400 mg Aniracetam and 300 mg Alpha GPC to avoid the racetam headache. Added 500 mg L Carnatine, 1000 mg Artichoke Extract and 250 mg (20% standardized) Forskolin and have felt calm focus. It’s been great, but wake up with headache now. Should I not be using L Carnatine with Alpha GPC?

    David Tomen
    November 8, 2020

    Deborah, L-Carnitine cannot cross the blood-brain barrier and that my be your problem. You need Acetyl L-Carnitine (ALCAR) for this stack to work.

Aaron
November 8, 2020

In the article, you refer to ‘Forskolin activates AChE and up-regulates its expression. ‘ but on October 29, 20 you refer to “Or we use an acetylcholinesterase inhibitor such as Forskolin” in one of your replies. Aren’t those contradictory?

I believe that my AChE receptors were damaged after getting ear tubes under general anesthesia as a child. As a result, I developed hyperhidrosis (excessive sweating) and also something called post orgasm illness syndrome which causes irritability, dark circles, mood disorder, allergic type symptoms, etc. after orgasm. Anticholinergic antihistamines seemed to help for awhile, but I went off of the about 6 years ago after 30 years of use. I’ve felt lousy since then and some urine testing shows high levels of organophosphates and other toxins in my system. Even back on the anticholinergics, piracetam and sodium butyrate still haven’t gotten me fully back on track. Will Coleus Forskolli help me to get my ACHe activity up and running to help remove any excess acetylcholine and organophosphate building from my brain and/or repair the AChe receptors? I haven’t tried atropine treatment yet. How bout Galantamine?
Any assistance would be great.

    David Tomen
    November 8, 2020

    Aaron, that was a mistake on my part and I went back and corrected. Not sure how that happened. Likely late in the day and I had no business trying to answer questions! So thank you.

    If you are looking for some way to upregulate acetylcholinesterase rather than inhibit it then Forskolin is a good choice. Galantamine is an acetylcholinesterase inhibitor which I think you are trying to avoid.

    Now I’m confused from re-reading your question. Do you want more or less acetylcholine in your brain?

      Aaron
      April 27, 2021

      Definitely trying to lower acetylcholine in the brain. I have low cholinesterase/pseudocholinesterase (confirmed in Nov ’20) since I was a kid (probably due to general anesthesia for ear tubes) so I’ve had issues with hyperhidrosis and allergies for decades. Was taking chlorpheniramine and glycopyrrolate/oxybutynin for awhile, but was told to stop due to potential dementia risk. I know those drugs/antihistamines were causing issues for me (memory, etc). Given my low AChE, and the fact that I love to eat animal protein, lowering ACh is definitely important. Piracetam seems somewhat effective. Would I be fine with just taking Forskolin or do I need artichoke extract as well? Is there a combo supplement of those two on the market? Thanks!

        David Tomen
        April 30, 2021

        Aaron, all you need is Forskolin.

    Ahern
    March 27, 2021

    Racetam: Deplete ACh
    Forskoli: Upregulate AChE

      Aaron
      April 27, 2021

      Very helpful and concise summary. 🙂

Reese Daniel
October 31, 2020

Forskolin supplements gave me horrible insomnia. I did not use the artichoke supplement with it, was taking if for weight loss not nootropic effect. Gave me the worse insomnia I’ve ever had. None of the good effects of stimulants but all of the bad. Forskolin makes Adderall look like Ambien……..Another horrible nootropic that did the same thing to me is vinpocetine….stay sfay from that stuff. Awful. Even after you stop taking it, it takes about 6 days for the bad effects to go away. Maybe these supplements just affect me differently, I don’t know but they cause my brain to do bizarre and unpleasant things and completely mess up my sleep cycle.

    David Tomen
    October 31, 2020

    Reese, that is a highly unusual reaction to Forskolin. Because if anything it should make you feel sleepy instead of causing insomnia.

    Both Forskolin and Vinpocetine activate cAMP. So you must have something strange going on with cAMP or how glutamate works in your brain to get this type of reaction.

Martin Nordin
October 24, 2020

Hi David
I have another question also, and it concerns caffeine combination

https://www.ncbi.nlm.nih.gov/pubmed/1690138
Caffeine inhibits forskolin-stimulated cyclic AMP accumulation in rat brain

“The most common side effect (which is still relatively rare) is diarrhea, due to its ability to increase the rate at which food moves through your digestive tract.

I should note, though, that this isn’t an issue for most people who are dieting, because restricting calories decreases gut motility. In other words,
dieting cancels out this effect for most people.
Regardless, if you run into this problem, you may want to stop taking forskolin, or at least >stop taking it with caffeine<

How do they mean? caffeine will worse Colleus induced "rate at which food moves through your digestive tract."
And what does dieting mean? (unspecified what diet)

And here is the other possible? issue (1) with my plan to combine Forskolin with Cacao

Theobromine and caffeine (1) the major alkaloids in seeds of Theobroma cacao L
https://www.scielo.br/scielo.php?script=sci_arttext&pid=S0101-20612015000200279&lng=en&nrm=iso

since Theobroma cacao L also are suppose to activate cAMP
(one condition might be that it is a PDE-inhibitor) and at the same time cacao contains caffein (1)but stil activates cAMP in mice, im getting unsure wheter caffeine will really deactivate cAMP in Colleus?

I see 3 potential scenarios If combining Colleus and Cacao in the same drink

1: Either the caffein in Cacao might deactivate Both colleus and its own cAMP enchanting properties?
2: Or it will synergy boost cAMP to new levels
3: Or it will deactive Colleus cAMP activation but add its own cAMP activation

What do you believe?

    David Tomen
    October 26, 2020

    Martin, the first study says, “Caffeine potently inhibited forskolin-stimulated cyclic AMP accumulation in “slices of rat cerebral cortex”.” What makes you think it’ll do the same in a human whole brain that is alive and working?

    I do not spend any time trying to dissect studies like these because most of the time they are completely irrelevant to the main mechanisms of action in the human brain which is demonstrated in dozens of studies.

      Martin Nordin
      October 27, 2020

      Thats a good point

      But also the study about upregulation cholinesterase you
      are refering to?
      https://pubmed.ncbi.nlm.nih.gov/16924422/
      are
      “N2a cells are a fast-growing mouse neuroblastoma cell line”

      However i believe its true and i hope its true in living human brains, but i think it may happen only in diseases that mimics pesticid attacks, both neuroblastoma and dementia might do that?

      And i did today find a secondary rat-study that supports the upregulation they call it “anticholinergic”
      https://pubmed.ncbi.nlm.nih.gov/16924422/

      And as i told you i have found several downregulation mouse studies also

        David Tomen
        October 28, 2020

        Martin, I understand your concern regarding these studies. But the thing is they are done with mice and rats and often just using a cell line in a petri dish.

        I’ve found the “rubber hits the road” when you try this with real people (i.e. humans). And see what happens.

        The thing is these supplements are generally safe and non-toxic when used at recommended dosages. And if they’re not contraindicated with any meds you happen to be using.

        It’s safe to try these supplements just to see if they work like the studies and reports by neurohackers say they do.

        And if all goes well you try them daily for a week or two. And then you’ll know if anything is upregulated or downregulated depending on how you feel.

        Martin Nordin
        October 29, 2020

        Im not worried for Colleus being toxic,
        i want to increase cholinesterase

        And what where the signs in human of healthy increased cholinesterase? whas it feeling more sleepy? or something more to?

        David Tomen
        October 29, 2020

        Martin, Cholinesterase is a family of enzymes that are involved in the synthesis of acetylcholine. We don’t attempt to increase the enzyme cholinesterase with nootropics. We use nootropics to either increase acetylcholine directly. With supplements such as Alpha GPC or CDP-Choline along with the necessary cofactors like ALCAR and the B-Vitamins.

        Or we use an acetylcholinesterase inhibitor such as Huperzine-A which inhibits this enzyme directly. When you inhibit acetylcholinesterase it forces more acetylcholine to be available.

        Too much or too little acetylcholine can make you feel sleepy.

Benjamin David Steele
September 28, 2020

You write that, “Many users of this stack report it helpful to supplement with 500 mg Phenylalanine, a B-Vitamin Complex and caffeine (coffee or preferably green tea).” Why do they find that helpful? What do each of those contribute?

    David Tomen
    September 29, 2020

    Benjamin, because Forskolin boosts the catecholamines like dopamine and Phenylalanine is a precursor to the synthesis of dopamine. And some of the B-Vitamins are a cofactor in the synthesis of dopamine. As for caffeine, I’m not sure why some people find it helpful with Forskolin.

Arnold
August 30, 2020

Hi David. Do you cycle Forskolin? There are a lot of sites suggesting to cycle nootropics, but I feel good taking them and dont want to stop taking them. Whats your opinion on this.
Thank you!

    David Tomen
    August 31, 2020

    Arnold, if that’s what the “other sites” are saying I’m happy that you made it here. Because I can’t think of a single reason why you’d want to cycle Forskolin.

    If what you’re doing works for you then keep on doing it. And forget about what others are saying.

Denise Gorlich
July 18, 2020

I’m a 59-yr old woman who has not been able to sleep through the night as long as I can remember. I’ve never had a problem falling asleep but most nights I wake up around 1 or 2:00 am and can’t fall back asleep. I worked a rotating schedule for 25 years so I had always blamed my poor sleep on that but found that once I retired 10 years ago it got no better. I tried everything to get a good nights sleep: sleep studies, meds, supplements… Finally, last year I decided to do a DNA test specifically for sleep and the results of the test suggested, among other things, that I take a Forskolin supplement in the morning. I researched the product and found out that it’s used to lose weight and there was nothing about it helping with sleep. Long story short, I’ve been taking it for at least 6 months and the stuff works for sleep issues. I haven’t lost weight but I sleep through the night. I’ve experimented with the product by going off of it for a few days and find that I wake up during the night and can’t fall asleep. As soon as I go back on the supplement I sleep through the night again. I can find nothing on the internet about Forskolin being used as a sleep aid. Is sleeping through the night a common experience when taking Forskolin?

    David Tomen
    July 18, 2020

    Denise, you just hit on something that could help a lot of people visiting Nootropics Expert. So thank you. Forskolin is not promoted as a “sleep supplement”. But maybe it should be. For a couple of reasons.

    1. cAMP responsive element binding protein (CREB) is a protein that modulates the transcription of genes. Increases in cAMP triggers the activation of CREB.

    And this transcription factor is a big part of intracellular signaling. It regulates everything from the production of new sperm cells in men (spermatogenesis), to “the circadian rhythms that control your sleep and awake cycles”, to memory formation.

    Forskolin increases cAMP which triggers the activation of CREB. Did you get that? Forskolin activates a gene transcription factor that helps to regulate circadian rhythms.

    2. Research shows Forskolin is effective for anxiety. Scroll up to “The Research” section called “Forskolin reduces anxiety”. Its effectiveness was compared to the benzo Xanax. But instead of attempting to reduce anxiety by working on the GABAa receptor like Xanax does (and the way Ambien works), Forskolin provides a similar benefit by affecting cAMP instead. This works because studies show that “sleep deprivation impairs cAMP signaling (https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2783639/). Forskolin helps reverse this process by activating cAMP.

      Karen
      September 26, 2020

      If you have high acetylcholine, wouldn’t using forskolin have a positive affect on sleep similar to an anticholergenic?

        David Tomen
        September 28, 2020

        Karen, I suppose it’s possible although Forskolin is not known as a sleep aid. Acetylcholinesterase is upregulated by cAMP courtesy Forskolin which makes you sleepy. So it may work.

Christian
May 31, 2020

Hello David,

I have been a silent reader of your site for quite a while and want to give you a big THANK YOU for doing all the work and putting out all this well founded and detailled information! THANKS A LOT!

I have discovered Forskolin lately and it seems that this is a substance which holds far more dose dependend effects than known so far; therefore I have included a few links you might want to check out; e.g. Forskolin seems to act as a Inhibitor of Nicotinic Acetylcholine Receptors, and that cAMP incresed by it seems to have positive and negative on the immune response, and that Forskolin seems to be NOT the only know substance to raise cAMP…

Sorry if the information is outdated or you know already, I tried to be precise. Anyway, here it is:

https://pubmed.ncbi.nlm.nih.gov/2425358/
Forskolin Increases the Rate of Acetylcholine Receptor Desensitization at Rat Soleus Endplates

https://pubmed.ncbi.nlm.nih.gov/1588923/
Forskolin Acts as a Noncompetitive Inhibitor of Nicotinic Acetylcholine Receptors

https://link.springer.com/article/10.1007/BF02986022
Effects of forskolin on endogenous dopamine and acetylcholine release

https://www.sciencedirect.com/science/article/abs/pii/030439409090575T
effect of forskolin on the response of acetylcholine receptors in frog sartorius endplate

https://www.sciencedirect.com/science/article/abs/pii/S0006291X85710996
Cyclic AMP Is an Essential Factor in Immune Responses

https://pubmed.ncbi.nlm.nih.gov/15790999/
N-coumaroyldopamine and N-caffeoyldopamine Increase cAMP via Beta 2-adrenoceptors

Hope to have contributed to your work, I just wanted to give a little bit back (and complete the knowledge, that’s a thing of mine…).

Many greetings from Germany!

All the best & God + Jesus bless,

Christian

    David Tomen
    June 1, 2020

    Christian, it’s been awhile since I wrote this review. So thank you for the time you’ve put into this research.

    I’ve taken note of everything and will go back and make adjustments to this review if they’re warranted.

    I very much appreciate when those in our community point out improvements to what I’ve done so far. Thank you.

Leave a Reply to David Tomen Cancel reply

Your email address will not be published. Required fields are marked *

This site uses Akismet to reduce spam. Learn how your comment data is processed.