Psycho-Babble Medication Thread 1080700

Shown: posts 1 to 16 of 16. This is the beginning of the thread.

 

PDE4 inhibitors?

Posted by SLS on July 22, 2015, at 9:06:22

Does anyone know of a drug available in the USA that inhibits PDE4?

I just read something suggesting that increasing cAMP levels effectively treats depression. A PDE4 inhibitor would do this. The only PDE4 inhibitor that I know of is a Japanese antidepressant by the name of rolipram. I don't think that it is a very effective drug by itself, but might make a good adjunct. If it were available in the USA, I would try it.

Theophylline?


- Scott

 

Re: PDE4 inhibitors?

Posted by linkadge on July 22, 2015, at 19:40:13

In reply to PDE4 inhibitors?, posted by SLS on July 22, 2015, at 9:06:22

Doesn't caffeine, to some extent, inhibit PDE4?

Linkadge

 

Re: PDE4 inhibitors?

Posted by hello123 on July 22, 2015, at 19:50:30

In reply to PDE4 inhibitors?, posted by SLS on July 22, 2015, at 9:06:22

Valium
http://www.ncbi.nlm.nih.gov/pubmed/9559885

and according to wikipedia, theobromine in chocolate is a non-selective PDE inhibitor.

 

Re: PDE4 inhibitors? » hello123

Posted by SLS on July 22, 2015, at 20:10:05

In reply to Re: PDE4 inhibitors?, posted by hello123 on July 22, 2015, at 19:50:30

> Valium
> http://www.ncbi.nlm.nih.gov/pubmed/9559885
>
> and according to wikipedia, theobromine in chocolate is a non-selective PDE inhibitor.

Very interesting. Thanks.


- Scott

 

Re: PDE4 inhibitors? » linkadge

Posted by SLS on July 22, 2015, at 20:14:53

In reply to Re: PDE4 inhibitors?, posted by linkadge on July 22, 2015, at 19:40:13

> Doesn't caffeine, to some extent, inhibit PDE4?
>
> Linkadge

I didn't consider caffeine. I'll look into it. Thanks.

I wish rolipram were available here. I was following the development of this drug for several years in the 1980s. It disappeared off the R&D map in the USA, only to reappear in Japan. Maybe it is available elsewhere, I don't know.


- Scott

 

Re: PDE4 inhibitors?

Posted by linkadge on July 23, 2015, at 16:49:56

In reply to Re: PDE4 inhibitors? » linkadge, posted by SLS on July 22, 2015, at 20:14:53

Caffeine consumption is inversely associated with suicide...

Linkadge

 

Re: PDE4 inhibitors?

Posted by Uncouth on July 24, 2015, at 12:03:25

In reply to Re: PDE4 inhibitors?, posted by linkadge on July 23, 2015, at 16:49:56

Scott et al,

Check out IBUDILAST

Only available in Japan as PINATOS

CHeck out this great article my buddy who owns this blog wrote about it. I've been trying it at 40-90mg a day. Can't say it's totally working but I definitely feel better in terms of general level of inflammation. This article is talking about its effects on glial-related inflammation and addictive behaviors and depression, rather than straight up cAMP increase, though combined with Forskolin it would potentaly increase cAMP, just like the well known "CILTEP" stack used by some people on longecity (I believe artichoke extract, as well as sceletium (kanna) are also effective PDE4 inhibitors. Luteloin might be as well but there are bioavailability questions).

Forskolin reliably increases cAMP independently of PDE4 inhibition but the combination probably is the best.

http://www.metabolicalchemy.com/ibudilast-kicks-inflammation-in-the-*ss/

 

Re: PDE4 inhibitors?

Posted by Hugh on July 24, 2015, at 13:02:18

In reply to PDE4 inhibitors?, posted by SLS on July 22, 2015, at 9:06:22

Resveratrol elevates cAMP levels.

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3431801/

 

Re: PDE4 inhibitors? » Hugh

Posted by SLS on July 24, 2015, at 14:21:30

In reply to Re: PDE4 inhibitors?, posted by Hugh on July 24, 2015, at 13:02:18

> Resveratrol elevates cAMP levels.
>
> http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3431801/

Thanks!

This seems like a good way to go.

As per the article:

"
Because PDE4 makes up most of the PDE activity in myotubes, we treated myotubes with the PDE4 inhibitor rolipram and found that rolipram increased cAMP to levels similar to those induced by resveratrol in myotubes
"


- Scott

 

Re: PDE4 inhibitors?

Posted by SLS on July 24, 2015, at 14:28:46

In reply to Re: PDE4 inhibitors?, posted by Uncouth on July 24, 2015, at 12:03:25

> Scott et al,
>
> Check out IBUDILAST
>
> Only available in Japan as PINATOS
>
> CHeck out this great article my buddy who owns this blog wrote about it. I've been trying it at 40-90mg a day. Can't say it's totally working but I definitely feel better in terms of general level of inflammation. This article is talking about its effects on glial-related inflammation and addictive behaviors and depression, rather than straight up cAMP increase, though combined with Forskolin it would potentaly increase cAMP, just like the well known "CILTEP" stack used by some people on longecity (I believe artichoke extract, as well as sceletium (kanna) are also effective PDE4 inhibitors. Luteloin might be as well but there are bioavailability questions).
>
> Forskolin reliably increases cAMP independently of PDE4 inhibition but the combination probably is the best.
>
> http://www.metabolicalchemy.com/ibudilast-kicks-inflammation-in-the-*ss/

Thanks. Nice article. It took me awhile to figure out that I had to change the "*" to an "a". :-)


- Scott

 

Re: PDE4 inhibitors? » Uncouth

Posted by SLS on July 24, 2015, at 14:29:47

In reply to Re: PDE4 inhibitors?, posted by Uncouth on July 24, 2015, at 12:03:25

> Scott et al,
>
> Check out IBUDILAST
>
> Only available in Japan as PINATOS
>
> CHeck out this great article my buddy who owns this blog wrote about it. I've been trying it at 40-90mg a day. Can't say it's totally working but I definitely feel better in terms of general level of inflammation. This article is talking about its effects on glial-related inflammation and addictive behaviors and depression, rather than straight up cAMP increase, though combined with Forskolin it would potentaly increase cAMP, just like the well known "CILTEP" stack used by some people on longecity (I believe artichoke extract, as well as sceletium (kanna) are also effective PDE4 inhibitors. Luteloin might be as well but there are bioavailability questions).
>
> Forskolin reliably increases cAMP independently of PDE4 inhibition but the combination probably is the best.
>
> http://www.metabolicalchemy.com/ibudilast-kicks-inflammation-in-the-*ss/

Thanks. Nice article. It took me awhile to figure out that I had to change the "*" to an "a". :-)


- Scott

 

Re: PDE4 inhibitors?

Posted by Lamdage22 on July 27, 2015, at 4:54:48

In reply to Re: PDE4 inhibitors?, posted by Uncouth on July 24, 2015, at 12:03:25

caffeine helps me. So does nicotine.

 

Re: PDE4 inhibitors? » Lamdage22

Posted by SLS on July 27, 2015, at 6:50:45

In reply to Re: PDE4 inhibitors?, posted by Lamdage22 on July 27, 2015, at 4:54:48

The problem with using caffeine on a regular basis is that it loses its positive effect and has me bouncing up and down. I don't know - maybe caffeine's main property, adenosine receptor antagonism, is counterproductive for me. I would rather have a selective PDE4 inhibitor. I am now looking at resveratrol as per someone's suggestion.

Thanks for you input.


- Scott

 

Re: PDE4 inhibitors? » SLS

Posted by phidippus on August 5, 2015, at 10:58:46

In reply to PDE4 inhibitors?, posted by SLS on July 22, 2015, at 9:06:22


Mesembrine, an alkaloid from the herb Sceletium tortuosum
Rolipram, used as investigative tool in pharmacological research
Ibudilast, a neuroprotective and bronchodilator drug used mainly in the treatment of asthma and stroke. It inhibits PDE4 to the greatest extent, but also shows significant inhibition of other PDE subtypes, and so acts as a selective PDE4 inhibitor or a non-selective phosphodiesterase inhibitor, depending on the dose.
Piclamilast, a more potent inhibitor than rolipram.[24]
Luteolin, supplement extracted from peanuts that also possesses IGF-1 properties.[25]
Drotaverine, used to alleviate renal colic pain, also to hasten cervical dilatation in labor
Roflumilast, indicated for people with severe COPD to prevent symptoms such as coughing and excess mucus from worsening[26]
Apremilast, used to treat psoriasis and psoriatic arthritis.

Eric

 

Re: PDE4 inhibitors? » phidippus

Posted by Uncouth on August 5, 2015, at 12:06:51

In reply to Re: PDE4 inhibitors? » SLS, posted by phidippus on August 5, 2015, at 10:58:46

I'd add the sceletium (kanna) is available in an effective standardized form called Zembrin. Source Naturals makes it though it seems to be hard to find, but you can get it online. I actually just took some this morning.

Note that it while it is a PDE4 inhibitor, it also possesses some mild SRI properties. I've taken it with an MAOI (starting at half a tablet, then a full tablet) though with no issues.

Some reports online say people feel instant effects, but I don't think I did. Perhaps slightly anxiolytic.

 

Re: PDE4 inhibitors? » Uncouth

Posted by former poster on August 6, 2015, at 18:46:47

In reply to Re: PDE4 inhibitors? » phidippus, posted by Uncouth on August 5, 2015, at 12:06:51

What MAOI are you taking it with? I gave sceletium a trial. It was effective but headache, nausea and ataxia were big issues. Still thinking about Zembrin. Hope the combo works for you. Keep us posted.


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