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Way 100635 does resensitize 5ht1a

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1 Way 100635 does resensitize 5ht1a on Thu Apr 28, 2016 4:16 am

Austria


hello,

my name is geri from austria.

have you seen the following study?


Antagonist-induced increase in 5-HT1A-receptor expression in adult rat hippocampus and cortex.

Abbas SY1, Nogueira MI, Azmitia EC.
Author information

Abstract

Many receptor antagonists function as reverse agonists on the signaling transduction pathway, but little is known about the action of these drugs on the regulation of receptor expression. Serotonin 1A (5-HT1A) receptor expression in 5-HT and serum-free fetal hippocampal cultures is increased in the presence of a specific 5-HT1A-receptor antagonist N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl) cyclohexane carboxamide (WAY 100635). To study the plasticity of postsynaptic 5-HT1A receptors in the presence of antagonist in vivo, adult Sprague Dawley rats were injected i.p. either once or twice daily with a dose of WAY 100635 (3 mg/kg) over a period of 3 days. The 5-HT1A receptor expression was detected by immunocytochemistry and light microscopy, and the receptor immunoreactivity (IR) in hippocampus subregions was quantitatively assessed by using a comparative computer-assisted morphometric analysis. Following the daily injections of WAY 100635, a significant increase in 5-HT1A receptor labeling in hippocampal neurons was recorded. This marked increase in 5-HT1A receptor expression, which occurred within 4 h after a single injection of WAY 100635, is evident on the somata membrane and dendritic processes of hippocampal and cortex layer V neurons. By contrast, no increase in 5-HT1A receptor-IR was observed after multiple daily injections at a low dose (1 mg/kg) of WAY 100635. Our study shows that a single or multiple daily injections of WAY 100635 can result in an increase in 5-HT1A receptor-IR. This increase in labeling is consistent with an enhanced expression of the receptor protein. The action of this "inverse agonist" may have clinical importance in disorders such as depression, epilepsy, and Alzheimer's disease in which 5-HT1A receptor levels are deficient.




For me it looks like that WAY 100635 does reverse desensitization of 5ht1a receptors... the used dosage is 3mg/kg...
means for me 240mg (at 80 kg)


and it does this within 3 days ...

can someone tell me if somebody has ever used WAY 100635?
i can't find anything.

Anyway I am going to try it, I will buy from the source that you gave us.

It costs 450 Dollars for 1g

I would need 240mg a day, so my cycle would last 4 days.

please tell me what you think, could this help us?

I have 2 more questions:

Is there a difference between rat-dosage and human-dosage?

how is it administraded? subcutan or intramuscular?

thank you very much

2 Re: Way 100635 does resensitize 5ht1a on Fri Apr 29, 2016 11:39 am

Area-1255

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Admin / Head Writer
No, DO NOT use that much WAY. You have to convert the rat to human dose using a specific conversion method, we do not use the same amount that rats use because of body surface area differences.
The WAY dosage would be about 18-25 mg . Maximum of 50-60 mg, no more than that under ANY CIRCUMSTANCES!
It can be administered subcutaneous or intramuscular.
http://www.ergo-log.com/calculatethehumandosage.html
http://www.fda.gov/downloads/Drugs/.../Guidances/UCM078932.pdf
https://www.researchgate.net/post/How_to_convert_human_dose_to_rat_dose

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3 Re: Way 100635 does resensitize 5ht1a on Fri Apr 29, 2016 11:43 am

Area-1255

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Admin / Head Writer
Also, it should be used with ketanserin for optimal efficiency.

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4 Re: Way 100635 does resensitize 5ht1a on Fri Apr 29, 2016 7:53 pm

Austria


Alright i see, thank you, then my cycle could last longer! and did you try it area?

Should i inject with nacl solution? If yes with how much?

5 Re: Way 100635 does resensitize 5ht1a on Mon May 02, 2016 6:42 pm

Area-1255

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Austria wrote:Alright i see, thank you,  then my cycle could last longer! and did you try it area?

Should i inject with nacl solution? If yes with how much?
No. I haven't tried it because THT hasn't contacted me back yet. I will eventually though. Saline isn't really necessary. Not for that compound in particular.

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6 Re: Way 100635 does resensitize 5ht1a on Mon Mar 20, 2017 6:42 pm

Area-1255

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Updating this Article.

Correct dosage of WAY 100 635 for HUMANS for Cognitive Enhancement / PSSD.
- 2.5 mg per day for Safety, then work up to a MAXIMUM of 10-15 mg of WAY.
- Administration would be ideally by Injection, for maximum absorption.
- Works best with Ritanserin.

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