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Enhancing sleep schedule and/or quality with icariin (a PDE5 inhibitor).

icariin pde5 pde5 inhibitor sleep circadian rythm clock

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#1 EachLastDay

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Posted 01 March 2015 - 06:22 PM


I think this is the right place to post this (first thread).

This study shows that pde5 inhibitors enhance phase advances (waking up earlier and going to sleep earlier) in response to morning ligh exposure.
http://journals.plos...al.pone.0037121

 

I ordered some icariin to try this out. Unwanted erections could be an embarassing side effect, depending on the dose taken.

 

My current understanding is that evening cGMP (induced by pde5 inhibitors) does not have a negative effects on sleep. It is also my understanding that cAMP (induced by forskolin or pde4 inhibitors) enhances/induces melatonin production. Here is an interesting study regarding melatonin and forskolin.

http://onlinelibrary...250411/abstract

 

Additionaly, melatonin inhibits cAMP.
http://www.ncbi.nlm....pubmed/19215498

 

I would like help understanding the relationship between cGMP, cAMP, and sleep. Based on my current understanding, increasing cGMP in the morning should drasticaly enhance sleep schedule and//or quality. Avoiding evening light is also good, but not very practical in this modern age (for me at least).


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#2 xls

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Posted 01 March 2015 - 07:14 PM

Excellent post! Thanks for this information. Keep us updated how it works.

 

edit: just like to mentioned you should wear blue-blocker glasses at night if you're worried about light exposure.

 

 

 

double edit: If this were true though wouldn't viagra be known for enhancing sleep? A side effect of viagra is restlessness...but maybe there's some other mechanism that's causing this besides PDE5 inhibition.


Edited by xls, 01 March 2015 - 07:19 PM.


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#3 EachLastDay

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Posted 01 March 2015 - 07:54 PM

Excellent post! Thanks for this information. Keep us updated how it works.

 

edit: just like to mentioned you should wear blue-blocker glasses at night if you're worried about light exposure.

Thanks. I have blue blocking glasses, I just find them really  anoying to wear. What I have been doing, though, is redshifting my computer moniter in the evening.

 

double edit: If this were true though wouldn't viagra be known for enhancing sleep? A side effect of viagra is restlessness...but maybe there's some other mechanism that's causing this besides PDE5 inhibition.

Viagra is usualy taken in the evening/night. If taken in the morning, just after waking up, it should help to phase advance your circadian rythm. It does this by enhancing the effects of blue light, which is good in the morning and bad in the evening. It may even work by increasing cGMP in the eye itself.

http://en.wikipedia....e_monophosphate

I did not know that viagra causes restlessness. There are many possible reasons for this.I have much more to learn about these complicated topics.

 



#4 Area-1255

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Posted 03 March 2015 - 12:22 AM

Nitric Oxide has a ton of neurological effects; some mediated by cGMP, some not so much. 

When nitric oxide triggers it's second messenger cGMP, it has the ability to activate/cross-activate exclusively the serotonin 5-HT(4) receptor; this causes bowel contraction when excited and thus is something very well associated with excess defacations. 

Additionally, the activation of 5-HT4 leads to excitation - as it is one of the most - if not most stimulatory serotonin receptor subtypes.

 

This may also be a part of why N.O enhances memory, however....so again, don't be surprised if PDE-5 inhibitors ; like ICARIIN, Viagra etc give you the shits as well..

 

Nitric Oxide also acts as a DAT; dopamine transporter inhibitor - therefore, it enhances dopamine activitiy and allows it to remain in the synapse longer and be more efficient.

 

You should expect mainly dopaminergic enhancement as you raise nitric oxide...whereas it's second messenger cGMP tends to have cross-roads effects - modulating/activating serotonin and also possibly increasing glutamate to an extent...

 

Cyclic AMP (cAMP) on the other hand is more tied into cortisol and stress hormones, as well as endogenous endorphin/opioid peptide related systems..but is also needed for testosterone production, thyroid hormone production and is essential for memory function - especially in the PREFRONTAL CORTEXT (executive functions, common sense etc)

 

It's also needed for spatial memory (where you put your keys etc).

 

Agents increasing cyclic GMP amplify 5-HT4-elicited positive inotropic response in failing rat cardiac ventricle.

 

Catecholamine stimulation of testosterone production via cyclic AMP in mouse Leydig cells in monolayer culture.

 

SEROTONIN-CGMP-GASTROINTESTINAL INTERACTIONS

 

http://onlinelibrary.wiley.com/doi/10.1038/sj.bjp.0701463/pdf


Edited by Area-1255, 03 March 2015 - 12:22 AM.


#5 VastEmptiness

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Posted 03 March 2015 - 06:18 PM

 

I ordered some icariin to try this out. Unwanted erections could be an embarassing side effect, depending on the dose taken.

Is it just me that learned all kinds of skills in puberty to hide wild boners that appear randomly during class? xD

However, on the more serious side: Very interesting, keep us updated on your experience.


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#6 EachLastDay

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Posted 05 March 2015 - 12:25 AM

Nitric Oxide has a ton of neurological effects; some mediated by cGMP, some not so much. 

When nitric oxide triggers it's second messenger cGMP, it has the ability to activate/cross-activate exclusively the serotonin 5-HT(4) receptor; this causes bowel contraction when excited and thus is something very well associated with excess defacations. 

Additionally, the activation of 5-HT4 leads to excitation - as it is one of the most - if not most stimulatory serotonin receptor subtypes.

 

This may also be a part of why N.O enhances memory, however....so again, don't be surprised if PDE-5 inhibitors ; like ICARIIN, Viagra etc give you the shits as well..

 

Nitric Oxide also acts as a DAT; dopamine transporter inhibitor - therefore, it enhances dopamine activitiy and allows it to remain in the synapse longer and be more efficient.

 

You should expect mainly dopaminergic enhancement as you raise nitric oxide...whereas it's second messenger cGMP tends to have cross-roads effects - modulating/activating serotonin and also possibly increasing glutamate to an extent...

 

Cyclic AMP (cAMP) on the other hand is more tied into cortisol and stress hormones, as well as endogenous endorphin/opioid peptide related systems..but is also needed for testosterone production, thyroid hormone production and is essential for memory function - especially in the PREFRONTAL CORTEXT (executive functions, common sense etc)

 

It's also needed for spatial memory (where you put your keys etc).

 

Agents increasing cyclic GMP amplify 5-HT4-elicited positive inotropic response in failing rat cardiac ventricle.

 

Catecholamine stimulation of testosterone production via cyclic AMP in mouse Leydig cells in monolayer culture.

 

SEROTONIN-CGMP-GASTROINTESTINAL INTERACTIONS

 

http://onlinelibrary.wiley.com/doi/10.1038/sj.bjp.0701463/pdf

Thank you. This is very helpful, and gives me a few more things to research if I wish.

Here is some more information relevent to this topic. Melatonin increases cGMP

http://joe.endocrino.../3/457.full.pdf

This makes a lot of sense. This should mean thar cGMP levels rise throughout the night, thus cGMP levels would be highest in the (subjective) early morning.

They did record an anomolous rise in cAMP for a moment, but appear to discount this due to the contradicting studies. It could have something to dowith the time of day they were administering it (i.e. 1pm).

 

 

 

I ordered some icariin to try this out. Unwanted erections could be an embarassing side effect, depending on the dose taken.

Is it just me that learned all kinds of skills in puberty to hide wild boners that appear randomly during class? xD

However, on the more serious side: Very interesting, keep us updated on your experience.

 

Hahah. I've never really had this problem, so I've not learnt any techniques. I'm sure google is chalk full of ideas.

 

I'm a bit of a penny pincher, so the free shipping on my icariin estimates it will arive on the 10th :( . It looks promising enough that I probably should have paid for better shipping. Oh well, several days wait won't kill me.

 

One thing I'd really like to know is if more cGMP can create phase advances with afternoon light exposure, rather than phase delays. Could cGMP be a major player in the circadian response to light?

 

On a related topic; I wonder how much of the positive effects reported with the CILTEP stack are actualy related to cGMP and not cAMP?

 

P.S. Is there a way I can edit my original post, so as to include some of this extra information?


Edited by EachLastDay, 05 March 2015 - 12:35 AM.


#7 EachLastDay

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Posted 11 March 2015 - 11:32 PM

I took my first dose of icariin this morning. It's now 4pm and I am more tired than I would have suspected. I think it's because of the icariin, but can't be sure because of daylight saving time. I thought I was buying a 10% extract, but the bottle says "min 3%". I took 3 750mg capsules which, based on 3% icarin, yields over 65mg of icariin. I've seen some people suggest that 250-400mg should be an effective dose for erections.

I just read this in-vitro study which shows that the circadian response to cAMP and cGMP are completely out of phase, just as I suspeced. cGMP massively advanced the clock during subjective midnight (i.e. mid-dark). This is the active phase for rats. I think this means that cGMP would have greatest effects for humans around noon. I could be wrong, though.
http://www.pnas.org/...7/6812.full.pdf



#8 EachLastDay

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Posted 18 March 2015 - 03:25 AM

Update: I have been taking the horny goat weed everday since it arrived, but I've been playing with the times. I've been taking 3 tablets at a time with a fatty food(just in case). This amounts to 65-70mg of icariin. This is definitely the low end of dosing. I might try more, but this bottle will run out fast.

Taking it in the early morning doesn't seem to help. It seemed like it made me tired all day.

Taking it in the late afternoon might help.

Yesterday, around 6pm, I took it with 300-400 micrograms of melatonin to enhance to cGMP, producing effects of melatonin in humans. I also wore my blue-blocking glasses. This seemed to work. I went to bed much earlier than normal. Interestingly I woke up in the middle of the night, then went back to sleep. This is actually my end goal. I want to try the natural biphasal sleep rythm.

I took icariin again with melatonin a couple of hours ago, 6pm, but am not wearing my blue-blocking glasses. I'll try to report back in a few days or so when I have more difinitive data. Looks promising so far, especially since I've only done low dose.



#9 Logic

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Posted 18 March 2015 - 12:20 PM

If you surf the net and do computer stuff at night inverting screen colours helps.

ie: a black background with white text.

 

[left Shift]+[Alt]+{Print Screen] does this for the whole OS.

 

I use Hacker vision, a Google chrome extension to get Longecity to look like it should IMHO.

ie:  Dark background with light text and oranges in stead of blues, or red shifted without the glasses.

 

https://chrome.googl...hhhkmoekeicedej

 

I attached a screen shot.

Attached File  Inverted.jpg   33.7KB   8 downloads



#10 bocor

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Posted 06 December 2015 - 09:24 PM

I've been taking 60 percent icarrin for 3 weeks now 1000 mg per day so 600 mg of icariin I have noticed a host of positive changes I'm sleeping deeper waking feeling refreshed sex drive is up think about sex much more now anxiety is better feel more confident especially socially mind you I'm also taking it with 200 mg of suprabio tocotrienols I also smoke a high cbd strain Cannatonic at night so could be combination I started mainly taking icariin for stem cell activation and testosterone benefits to help heal back injury
I should also add my thinking is quicker sharper creativity is way up

#11 chrisp2

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Posted 07 December 2015 - 12:41 PM

I've been taking 60 percent icarrin for 3 weeks now 1000 mg per day so 600 mg of icariin I have

 

What product are you taking?

 

It seems Icariin is not Icariin...  In that some don't list the standardization amount (although claiming standardized)...  Others say "Icariins" which is different than the singular form, from what I can tell.



#12 bocor

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Posted 07 December 2015 - 08:21 PM

from abs research



#13 chrisp2

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Posted 08 December 2015 - 12:11 AM

from abs research

 

This:

 

http://worldabs.com/products/icariin60

 

?

 

You're taking 2 per day?



#14 tunt01

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Posted 08 December 2015 - 01:11 AM

I've been taking 60 percent icarrin for 3 weeks now 1000 mg per day so 600 mg of icariin I have noticed a host of positive changes I'm sleeping deeper waking feeling refreshed sex drive is up think about sex much more now anxiety is better feel more confident especially socially mind you I'm also taking it with 200 mg of suprabio tocotrienols I also smoke a high cbd strain Cannatonic at night so could be combination I started mainly taking icariin for stem cell activation and testosterone benefits to help heal back injury
I should also add my thinking is quicker sharper creativity is way up

 

Doesn't surprise me.  It's got numerous positive effects, beyond just being a PDE-5 inhibitor.  It activates SIRT6, which is known to extend lifespan.

 

I have a pile of it sitting on my desk, but I've not been taking it lately.  I'm pretty sure it's the primary (or one of the primary) active ingredients in the Sierra Sciences Product B.



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#15 bocor

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Posted 08 December 2015 - 10:37 PM

Yes that's the same
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Also tagged with one or more of these keywords: icariin, pde5, pde5 inhibitor, sleep, circadian rythm, clock

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