Psycho-Babble Medication Thread 1060890

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Serotonin 5-HT7 receptor antagonism and depression

Posted by SLS on February 19, 2014, at 23:15:39

There is an increasing focus on the serotonin 5-HT7 receptor and its involvement in the etiology and treatment of depression. Among the drugs that act as antagonists at this receptor are lurasidone (Latuda), asenapine (Saphris), aripiprazole (Abilify), vortioxetine (Brintellix), levomilnacipran (Fetzima), and amisulpride (Solian). I think it is worth investigating this subject further.


Other 5-HT7 antagonists according to Wiki:

Amisulpride
Amitriptyline
Amoxapine
Clomipramine
Clozapine
Cyproheptadine
EGIS-12233
Fluphenazine
Fluperlapine
ICI 169,369
Imipramine
Ketanserin
Loxapine
Lurasidone
LY-215,840
Maprotiline
Mesulergine
Methysergide
Mianserin
Olanzapine
Ritanserin
SB-258,719[24][25][26]
SB-258,741[26]
SB-269,970 (highly 5-HT7 selective)[27]
SB-656,104-A[28]
SB-691,673[24]
Sertindole
Spiperone
Sulpiride
Tenilapine
TFMPP
Vortioxetine
Trifluoperazine
Ziprasidone
Zotepine


- Scott

 

Re: Serotonin 5-HT7 receptor antagonism and depression » SLS

Posted by Phillipa on February 20, 2014, at 9:17:51

In reply to Serotonin 5-HT7 receptor antagonism and depression, posted by SLS on February 19, 2014, at 23:15:39

How come so many atypical antipsychotics? And TCA's pretty heavy duty meds? PJ

 

Re: Serotonin 5-HT7 receptor antagonism and depression » Phillipa

Posted by SLS on February 20, 2014, at 11:34:46

In reply to Re: Serotonin 5-HT7 receptor antagonism and depression » SLS, posted by Phillipa on February 20, 2014, at 9:17:51

> How come so many atypical antipsychotics? And TCA's pretty heavy duty meds? PJ

I don't know how to answer your question. Drug chemicals don't know what it is they are supposed to be. They just are.

As more data emerges regarding 5-HT7 receptors and depression, I'm sure there will be some pleasant surprises.


- Scott

 

Re: Serotonin 5-HT7 receptor antagonism and depression

Posted by jono_in_adelaide on February 22, 2014, at 7:08:31

In reply to Serotonin 5-HT7 receptor antagonism and depression, posted by SLS on February 19, 2014, at 23:15:39

I think risperidone is also a 5HT7 antagonist, no?

I found 1mg at night very helpfull in depression and anxiety

 

Re: Serotonin 5-HT7 receptor antagonism and depression » jono_in_adelaide

Posted by SLS on February 22, 2014, at 16:31:22

In reply to Re: Serotonin 5-HT7 receptor antagonism and depression, posted by jono_in_adelaide on February 22, 2014, at 7:08:31

> I think risperidone is also a 5HT7 antagonist, no?

Yes. So much so, that it is actually an irreversible inverse agonist. An inverse agonist not only blocks the receptor from doing its job, it fools it into doing the *opposite* of what it was designed to do. For example, if a receptor normally depolarizes the cell membrane when stimulated, an inverse agonist will cause the receptor to hyperpolarize the cell membrane.

> I found 1mg at night very helpfull in depression and anxiety

That's great!

Do you experience an improvement in depression and anxiety throughout the day?


- Scott

 

Re: Serotonin 5-HT7 receptor antagonism and depression

Posted by bleauberry on February 22, 2014, at 16:34:41

In reply to Serotonin 5-HT7 receptor antagonism and depression, posted by SLS on February 19, 2014, at 23:15:39

Amisulpride and zyprexa both helped me, and both have 5-HT7 mechanisms.

 

Re: Serotonin 5-HT7 receptor antagonism and depression

Posted by jono_in_adelaide on February 22, 2014, at 18:05:49

In reply to Re: Serotonin 5-HT7 receptor antagonism and depression » jono_in_adelaide, posted by SLS on February 22, 2014, at 16:31:22

Scott, yes, sure do - less depression, less anxiety, and less intrusive thoghts ("it'd be better if you just killed your self" etc)

Side effects were limited to a little drowsiness for the first 2 days, you could probably avoid this by starting at 0.5mg at night then increasing to 1mg and so on

 

Important correction:

Posted by SLS on February 23, 2014, at 15:02:38

In reply to Serotonin 5-HT7 receptor antagonism and depression, posted by SLS on February 19, 2014, at 23:15:39

Levomilnacipran (Fetzima) is NOT a 5-HT7 antagonist.

Sorry.


- Scott


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