Re: Annybody believes in 5HT1A antagonists?

[Guest guest]

This email was found in my spam folder. may be thats why there's no response from folks, here? Anyway, this sounds very promising. Almost too good to be true!!Subject: Annybody believes in 5HT1A antagonists?To: SSRIsex Date: Wednesday, December 8, 2010, 3:56 PM

As I read on wikipedia (http://en.wikipedia.org/wiki/Post-SSRI_sexual_dysfunction) ssri's downregulate 5HT1A receptors.

Further research indicated that the use of 5HT1A antagonists are capable of upregulating these receptors.

(http://eurekamag.com/research/036/007/up-regulation-5-ht1a-receptor-special-antagonist-way-100635-adult-rat-hippocampus.php)

With further researching I came across this medicin: Lecozotan (http://en.wikipedia.org/wiki/Lecozotan) wich is in Phase III clinical trails)

I've read this:

Lecozotan is a competitive, selective 5-HT1A receptor antagonist[3] which enhances the potassium-stimulated release of acetylcholine and glutamate.[4]

This reminded me of something i've read here about glutamate and sexual behavior.

Is this a possible treatment? Will upregulation of this receptor give any relief?

[Guest guest]

Any idea when this thing will hit the market? I curiosity is peaked.

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> Subject: Annybody believes in 5HT1A antagonists?

> To: SSRIsex

> Date: Wednesday, December 8, 2010, 3:56 PM

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> As I read on wikipedia

(http://en.wikipedia.org/wiki/Post-SSRI_sexual_dysfunction) ssri's downregulate

5HT1A receptors.

>

> Further research indicated that the use of 5HT1A antagonists are capable of

upregulating these receptors.

>

>

(http://eurekamag.com/research/036/007/up-regulation-5-ht1a-receptor-special-ant\

agonist-way-100635-adult-rat-hippocampus.php)

>

>

>

> With further researching I came across this medicin: Lecozotan

(http://en.wikipedia.org/wiki/Lecozotan) wich is in Phase III clinical trails)

>

>

>

> I've read this:

>

>

>

> Lecozotan is a competitive, selective 5-HT1A receptor antagonist[3] which

enhances the potassium-stimulated release of acetylcholine and glutamate.[4]

>

>

>

> This reminded me of something i've read here about glutamate and sexual

behavior.

>

> Is this a possible treatment? Will upregulation of this receptor give any

relief?

>

[Guest guest]

Isn't buspar a 5HT1A antagonist?

>

> As I read on wikipedia

(http://en.wikipedia.org/wiki/Post-SSRI_sexual_dysfunction) ssri's downregulate

5HT1A receptors.

> Further research indicated that the use of 5HT1A antagonists are capable of

upregulating these receptors.

>

(http://eurekamag.com/research/036/007/up-regulation-5-ht1a-receptor-special-ant\

agonist-way-100635-adult-rat-hippocampus.php)

>

> With further researching I came across this medicin: Lecozotan

(http://en.wikipedia.org/wiki/Lecozotan) wich is in Phase III clinical trails)

>

> I've read this:

>

> Lecozotan is a competitive, selective 5-HT1A receptor antagonist[3] which

enhances the potassium-stimulated release of acetylcholine and glutamate.[4]

>

> This reminded me of something i've read here about glutamate and sexual

behavior.

> Is this a possible treatment? Will upregulation of this receptor give any

relief?

>

[Guest guest]

Buspar is an agonist. From wikipedia below:Buspirone functions as a serotonin 5-HT1A receptor partial agonist.[6] It is this action that is thought to mediate its anxiolytic and antidepressant effects. Additionally, it functions as a dopamine D2, as well as α1, and α2-adrenergic receptor antagonist

to a lesser degree, though these properties are generally undesirable in an anxiolytic and likely only contribute to side effects.Subject: Re: Annybody believes in 5HT1A antagonists?To: SSRIsex Date: Saturday, December 11, 2010, 12:23 AM

Isn't buspar a 5HT1A antagonist?

>

> As I read on wikipedia (http://en.wikipedia.org/wiki/Post-SSRI_sexual_dysfunction) ssri's downregulate 5HT1A receptors.

> Further research indicated that the use of 5HT1A antagonists are capable of upregulating these receptors.

> (http://eurekamag.com/research/036/007/up-regulation-5-ht1a-receptor-special-antagonist-way-100635-adult-rat-hippocampus.php)

>

> With further researching I came across this medicin: Lecozotan (http://en.wikipedia.org/wiki/Lecozotan) wich is in Phase III clinical trails)

>

> I've read this:

>

> Lecozotan is a competitive, selective 5-HT1A receptor antagonist[3] which enhances the potassium-stimulated release of acetylcholine and glutamate.[4]

>

> This reminded me of something i've read here about glutamate and sexual behavior.

> Is this a possible treatment? Will upregulation of this receptor give any relief?

>

[Guest guest]

From what I understand, if you're off SSRI's, and you have PSSD, taking 5HT(xx) (I don't remember which one -- each type does different things) can get more serotonin running around in your brain and body (not sure about the latter - I think that's made by the intestines) to add to the serotonin that makes it out of the axon into the synapse. But then it would be as if you were taking an SSRI again, as least as far as having extra serotonin in your brain.

If you're still on an SSRI, it adds too much and you might get that thing that hangs over all our heads -- serotonin syndrome, which can be fatal.

In any case, I haven't read anything saying that 5HT(xx) can upregulate (raise fro the dead) the axon's reuptake receptors. And I do mean axon -- the nerve that carried the serotonin to the synapse (actually nerves don't carry chemicals other than sodium and potassium ions, which exchange places -- inside and outside the neuron, and this exchange ripples down the neuron, acting as a signal to the nerve ending to do its job, in this case make serotonin & excrete it to the synapse). Too much inhibition of reuptake cells (the function of reuptake is to keep you from having too much serotonin going around in your brain) by SSRI's may cause "downregulation" of the reuptake cells (read: paralysis, giving up its job since it doesn't seem to be needed, disuse, and possibly, cell death).

It would be better to put someone who's chronically depressed (and not situationally -- nobody with situational depression should be given meds for it) on the right 5HT molecule than to put them on SSRIs.

I posted something about this earlier today.

Ann

> >> > As I read on wikipedia (http://en.wikipedia.org/wiki/Post-SSRI_sexual_dysfunction) ssri's downregulate 5HT1A receptors. > > Further research indicated that the use of 5HT1A antagonists are capable of upregulating these receptors.> > (http://eurekamag.com/research/036/007/up-regulation-5-ht1a-receptor-special-antagonist-way-100635-adult-rat-hippocampus.php)> > > > With further researching I came across this medicin: Lecozotan (http://en.wikipedia.org/wiki/Lecozotan) wich is in Phase III clinical trails)> > > > I've read this:> > > > Lecozotan is a competitive, selective 5-HT1A receptor antagonist[3] which enhances the potassium-stimulated release of acetylcholine and glutamate.[4]> > > > This reminded me of something i've read here about glutamate and sexual behavior.> > Is this a possible treatment? Will upregulation of this receptor give any relief?> >>

[Guest guest]

Are we talking about receptors on the next dendrite or reuptake receptors on the axon whence the original serotonin came? If it stimulates the reuptake receptors, it'll only work if the receptors haven't been "downregulated" to zero, i.e. they no longer can function. If there are some live, albeit sluggish reuptake receptors, then Buspar might be able to bring them back to full or partial function and hopefully this will cause the axon to make more fully functional receptors and nobody will ever inhibit them again.

Ann

> > >> > > As I read on wikipedia (http://en.wikipedia.org/wiki/Post-SSRI_sexual_dysfunction) ssri's downregulate 5HT1A receptors. > > > Further research indicated that the use of 5HT1A antagonists are capable of upregulating these receptors.> > > (http://eurekamag.com/research/036/007/up-regulation-5-ht1a-receptor-special-antagonist-way-100635-adult-rat-hippocampus.php)> > > > > > With further researching I came across this medicin: Lecozotan (http://en.wikipedia.org/wiki/Lecozotan) wich is in Phase III clinical trails)> > > > > > I've read this:> > > > > > Lecozotan is a competitive, selective 5-HT1A receptor antagonist[3] which enhances the potassium-stimulated release of acetylcholine and glutamate.[4]> > > > > > This reminded me of something i've read here about glutamate and sexual behavior.> > > Is this a possible treatment? Will upregulation of this receptor give any relief?> > >>

[Guest guest]

I think 5HT(xx) refers to the receptors, but the thing you would take to increase serotonin is 5htp, a precursor to serotonin that is able to pass the blood-brain barrier.I think the theory with 5HT1A antagonists is that they simulate low levels of serotonin and hopefully cause the receptors to upregulate, in the opposite way that having too much serotonin available when on SSRI may have caused downregulation.---It is 5htp that you shoudl be careful taking in conjunction with SSRIs.

http://en.wikipedia.org/wiki/5-Hydroxytryptophan

Yes, 5htp, makes more serotonin available to the brain but is this effectively the same as taking SSRI? I like to think not!The way I see it is a crude river analogy:SSRI is building a dam and 5htp is putting in a bit more water upstream. (Sorry! just the way I think about it.)Both end up with a more water available but the dam has the biggest impact on the environment!My opinions are amateur, and I am aware that other posters have had negative experiences with 5htp. my point is just that I dont think because ultimately 5htp and SSRI end up with more serotonin that they will necessarily both be damaging in the same way.From: ruby2zdy

To: SSRIsex Sent: Sat, 11 December, 2010 6:46:05Subject: Re: Annybody believes in 5HT1A antagonists?

From what I understand, if you're off SSRI's, and you have PSSD, taking 5HT(xx) (I don't remember which one -- each type does different things) can get more serotonin running around in your brain and body (not sure about the latter - I think that's made by the intestines) to add to the serotonin that makes it out of the axon into the synapse. But then it would be as if you were taking an SSRI again, as least as far as having extra serotonin in your brain.

If you're still on an SSRI, it adds too much and you might get that thing that hangs over all our heads -- serotonin syndrome, which can be fatal.

In any case, I haven't read anything saying that 5HT(xx) can upregulate (raise fro the dead) the axon's reuptake receptors. And I do mean axon -- the nerve that carried the serotonin to the synapse (actually nerves don't carry chemicals other than sodium and potassium ions, which exchange places -- inside and outside the neuron, and this exchange ripples down the neuron, acting as a signal to the nerve ending to do its job, in this case make serotonin & excrete it to the synapse). Too much inhibition of reuptake cells (the function of reuptake is to keep you from having too much serotonin going around in your brain) by SSRI's may cause "downregulation" of the reuptake cells (read: paralysis, giving up its job since it doesn't seem to be needed, disuse, and possibly, cell death).

It would be better to put someone who's chronically depressed (and not situationally -- nobody with situational depression should be given meds for it) on the right 5HT molecule than to put them on SSRIs.

I posted something about this earlier today.

Ann

> >> > As I read on wikipedia (http://en.wikipedia.org/wiki/Post-SSRI_sexual_dysfunction) ssri's downregulate 5HT1A receptors. > > Further research indicated that the use of 5HT1A antagonists are capable of upregulating these receptors.> > (http://eurekamag.com/research/036/007/up-regulation-5-ht1a-receptor-special-antagonist-way-100635-adult-rat-hippocampus.php)> > > > With further researching I came across this medicin:

Lecozotan (http://en.wikipedia.org/wiki/Lecozotan) wich is in Phase III clinical trails)> > > > I've read this:> > > > Lecozotan is a competitive, selective 5-HT1A receptor antagonist[3] which enhances the potassium-stimulated release of acetylcholine and glutamate.[4]> > > > This reminded me of something i've read here about glutamate and sexual behavior.> > Is this a possible treatment? Will upregulation of this receptor give any relief?> >>

[Guest guest]

Is this based on fact or theory? Just curious where you got this info? Is

there anywhere this is documented?

> >

> > >

> >

> > > As I read on wikipedia

> (http://en.wikipedia.org/wiki/Post-SSRI_sexual_dysfunction) ssri's

> downregulate 5HT1A receptors.

> >

> > > Further research indicated that the use of 5HT1A antagonists are

> capable of upregulating these receptors.

> >

> > >

> (http://eurekamag.com/research/036/007/up-regulation-5-ht1a-receptor-spe\

> cial-antagonist-way-100635-adult-rat-hippocampus.php)

> >

> > >

> >

> > > With further researching I came across this medicin: Lecozotan

> (http://en.wikipedia.org/wiki/Lecozotan) wich is in Phase III clinical

> trails)

> >

> > >

> >

> > > I've read this:

> >

> > >

> >

> > > Lecozotan is a competitive, selective 5-HT1A receptor antagonist[3]

> which enhances the potassium-stimulated release of acetylcholine and

> glutamate.[4]

> >

> > >

> >

> > > This reminded me of something i've read here about glutamate and

> sexual behavior.

> >

> > > Is this a possible treatment? Will upregulation of this receptor

> give any relief?

> >

> > >

> >

>

[Guest guest]

I hope i'm not dissapointing annybody, but this is all a theorie, based up what

I've read on wikipedia, what guesses the cause of pssd.

For the record, a 5HTXX agonist/antagonist can't do annything with the reuptake

ports.

But I've read somewhere, that a monkey was given XTC for about 4 days straight,

and then they axamined his serotonin system. Before there were all beautifull

white stripes, and afterwards the picture was all black. After 7 years, less

then half of the white returned.

Somebody claims 5HT neurons are NOT killed in the process, but the radio-active

tracer they use, binds to the reuptake ports. Now if XTC 'killed' these reuptake

ports, it's like the whole serotonin system is destroid. But in fact it's still

there. This gives hope.

Possible there are some axons lost, but they can regrow.

Now..

This 5HT1A antagonist binds to the receptors, inhibiting there action. This will

cause to upregulate these receptors, become more sensitive, to return natural

balance. Hoping that 5HT1A downregulation plays a mayor role in PSSD,

upregulation of these receptors can give some relief.

But I belief that PSSD is a whole complex thing, possible more complex then

explained on wikipedia. Why do most people DON'T get PSSD? They must have

downregulated postsynaptic 5HT1A neurons too, but no sexual side effects.

>

> As I read on wikipedia

(http://en.wikipedia.org/wiki/Post-SSRI_sexual_dysfunction) ssri's downregulate

5HT1A receptors.

> Further research indicated that the use of 5HT1A antagonists are capable of

upregulating these receptors.

>

(http://eurekamag.com/research/036/007/up-regulation-5-ht1a-receptor-special-ant\

agonist-way-100635-adult-rat-hippocampus.php)

>

> With further researching I came across this medicin: Lecozotan

(http://en.wikipedia.org/wiki/Lecozotan) wich is in Phase III clinical trails)

>

> I've read this:

>

> Lecozotan is a competitive, selective 5-HT1A receptor antagonist[3] which

enhances the potassium-stimulated release of acetylcholine and glutamate.[4]

>

> This reminded me of something i've read here about glutamate and sexual

behavior.

> Is this a possible treatment? Will upregulation of this receptor give any

relief?

>