Psycho-Babble Medication Thread 1121215

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Mice lacking 5-ht2c unlearn fear faster

Posted by linkadge on December 5, 2022, at 14:04:27

https://medicalxpress.com/news/2022-12-mouse-fearlessness.html

 

Re: Mice lacking 5-ht2c unlearn fear faster

Posted by Jay2112 on December 5, 2022, at 17:05:24

In reply to Mice lacking 5-ht2c unlearn fear faster, posted by linkadge on December 5, 2022, at 14:04:27

The 5-ht2c receptor is the most activating serotonin receptor. It is implicated in everything from autism to bipolar disorder. Serzone (nefadezone) blocked this receptor, and was considered one of the most unique antidepressants on the market. Trazodone is a similar drug, but way more side effects.

I think many on here would respond to nefadezone. Risperidone and clozapine are the two most powerful 5ht2c antipsychotic blockers.

Jay

 

Re: Mice lacking 5-ht2c unlearn fear faster

Posted by iforgotmypassword on December 7, 2022, at 15:57:19

In reply to Mice lacking 5-ht2c unlearn fear faster, posted by linkadge on December 5, 2022, at 14:04:27

What i recall from reading abt this recently given 5-ht2c seems to b the disaster receptor responsibile for ssri akathisia, bruxism etc that chokes DA efflux from VTA:

-forget risperidoneits actually pretty weak. U need higher 2c affinity than 2a to get significant occupancy at 2c receptors, and saturation with inverse agonism seems to b required to get the pro-DA anti-EPS effect you see in animal models; risperidone is also one of the harshest antipsychotics ive ever taken on movement

-this leaves clozapine, mirtazapine, and maybe asenapine and sertindole but i doubt they are as gentle on movement as clozapine

 

Re: Mice lacking 5-ht2c unlearn fear faster » iforgotmypassword

Posted by SLS on December 7, 2022, at 20:26:07

In reply to Re: Mice lacking 5-ht2c unlearn fear faster, posted by iforgotmypassword on December 7, 2022, at 15:57:19

Hi.

> What i recall from reading abt this recently given 5-ht2c seems to b the disaster receptor responsibile for ssri akathisia, bruxism etc that chokes DA efflux from VTA:


> U need higher 2c affinity than 2a to get significant occupancy at 2c receptors, and saturation with inverse agonism seems to b required to get the pro-DA anti-EPS effect you see in animal models

> Inverse agonism at 5-HT2a? So, merely blocking 5-HT2a is not sufficient to allow the stimulation of 5-HT2c?


Wow.


I'm not clear about how it works that 5-HT2c agonism should produce anti-dopaminergic effects. Can you describe how that happens? I don't think I really appreciated the ability of SSRIs to reduce DA function to the point of producing EPS. Is this due to 5-HT2c agonism? What about the ability of SSRIs to produce amotivation and "emotional numbing"? Is this the result of the same mechanisms?


; risperidone is also one of the harshest antipsychotics ive ever taken on movement


I think risperidone is considered an atypical AP because it blocks 5-HT2c receptors. However, I think its binding affinity to D2 receptors leaves risperidone hanging somewhere between typical and atypical APs. I was given risperidone to treat a moderate manic reaction to a drug treatment. I was not well. My father and brother eventually convinced me to swallow a risperidone pill. They had been working with my doctor. I went from a sort of dysphoric mania to a very slowed-down depression within 30 minutes. I felt like I was dying inside. It's not for everybody.


> -this leaves clozapine, mirtazapine, and maybe asenapine and sertindole but i doubt they are as gentle on movement as clozapine


It's interesting that you didn't include olanzapine. I had the impression that olanzapine was the AP closest to clozapine with respect to clinical effects, including the incidence of EPS, but I haven't kept current.

Olanzapine was often used to remediate the EPS caused by other APs - as is clozapine.

Did you know that immediately upon its approval, olanzapine was reported as triggering mania? I haven't looked to see if this concern still exists.


- Scott

 

Re: Mice lacking 5-ht2c unlearn fear faster » SLS

Posted by iforgotmypassword on December 7, 2022, at 22:23:00

In reply to Re: Mice lacking 5-ht2c unlearn fear faster » iforgotmypassword, posted by SLS on December 7, 2022, at 20:26:07

Hi! Ill brb in a bit. I couldnt read all of this just yet. But here are some articles i quickly googled that seem to agree with what ive been reading in general before i forget

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1939890/

https://www.nature.com/articles/s41380-018-0227-x

 

Thanks. :-) (nm) » iforgotmypassword

Posted by SLS on December 8, 2022, at 0:18:44

In reply to Re: Mice lacking 5-ht2c unlearn fear faster » SLS, posted by iforgotmypassword on December 7, 2022, at 22:23:00

 

CAPTODIAMINE in canada or US

Posted by iforgotmypassword on December 8, 2022, at 15:17:11

In reply to Mice lacking 5-ht2c unlearn fear faster, posted by linkadge on December 5, 2022, at 14:04:27

It's weird but has unique effects in benzo withdrawal that look like the 5-ht2c antagonism is serious. Very old antihistamine.

Is legal Canada as a prescription drug again since 2013. Not currently made my generic or brand companies. 2 compounding pharmacies say they can't make it as they can't get the raw ingredient.

Do any compounding pharmacies make the compound themselves? There are instructions that make it sound like with the right reagents, it can b made professionally.

But it's also sold in France and Pakistan.

Really want to try it for my akathisia and tension, that tends to b worsened by benzos.

 

Re: Mice lacking 5-ht2c unlearn fear faster » iforgotmypassword

Posted by SLS on December 8, 2022, at 17:53:09

In reply to Re: Mice lacking 5-ht2c unlearn fear faster, posted by iforgotmypassword on December 7, 2022, at 15:57:19

Ritanserin

A great drug without an indication.

Check it out.


- Scott

 

Re: Mice lacking 5-ht2c unlearn fear faster

Posted by Jay2112 on December 16, 2022, at 18:39:43

In reply to Re: Mice lacking 5-ht2c unlearn fear faster » iforgotmypassword, posted by SLS on December 8, 2022, at 17:53:09

How serotonin activates adrenaline:

Serotonin activates the hypothalamic-pituitary-adrenal axis via serotonin 2C receptor stimulation

https://pubmed.ncbi.nlm.nih.gov/17596444/

5-ht2c is also implicated in autism. NOT a 'nice' receptor. :/

Jay


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