Psycho-Babble Medication Thread 1094216

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Are there any 5ht1a Inverse Agonists?

Posted by Hello321 on July 25, 2017, at 23:17:34

Been some time now ive been trying different meds hoping to find relief for some intense anhedonia. Lately ive gotten interested in the 5ht1a receptors effects on brain function/mood. And i had at one point tried buspar and it had a very strong, negative effect on my anhedonia from the first dose. And so now im thinking the opposite of an agonist/inverse agonist at the 1a receptors might be beneficial for me. Ive taken a few non selective 5ht1a antagonists with no benefit. But an antagonist isnt quite the opposite of an agonist like buspar. An inverse agonist would be needed to get the opposite effect. But are there any 5ht1a inverse agonists?

 

Re: Are there any 5ht1a Inverse Agonists? Hello321

Posted by SLS on July 26, 2017, at 2:17:42

In reply to Are there any 5ht1a Inverse Agonists?, posted by Hello321 on July 25, 2017, at 23:17:34

> Been some time now ive been trying different meds hoping to find relief for some intense anhedonia. Lately ive gotten interested in the 5ht1a receptors effects on brain function/mood. And i had at one point tried buspar and it had a very strong, negative effect on my anhedonia from the first dose. And so now im thinking the opposite of an agonist/inverse agonist at the 1a receptors might be beneficial for me. Ive taken a few non selective 5ht1a antagonists with no benefit. But an antagonist isnt quite the opposite of an agonist like buspar. An inverse agonist would be needed to get the opposite effect. But are there any 5ht1a inverse agonists?

You might take a look at Trintellix. It is a full agonist at 5-HT1a receptors.


- Scott

 

Re: Are there any 5ht1a Inverse Agonists?

Posted by Hello321 on July 26, 2017, at 14:57:02

In reply to Re: Are there any 5ht1a Inverse Agonists? Hello321, posted by SLS on July 26, 2017, at 2:17:42

Inverse agonist. It has the exact opposite effect of an agonist at a receptor. Instead os simply blocking a receptor like an antagonist, it inhibits the effects the receptor itself has in the brain. I think Spiperone is an Inverse Agonist at the the 5ht1a receptor, but its not available in America. Tho i may see if theres a way to obtain it online.

 

Re: Are there any 5ht1a Inverse Agonists? Hello321

Posted by SLS on July 26, 2017, at 19:51:35

In reply to Re: Are there any 5ht1a Inverse Agonists?, posted by Hello321 on July 26, 2017, at 14:57:02

> Inverse agonist. It has the exact opposite effect of an agonist at a receptor. Instead os simply blocking a receptor like an antagonist, it inhibits the effects the receptor itself has in the brain. I think Spiperone is an Inverse Agonist at the the 5ht1a receptor, but its not available in America. Tho i may see if theres a way to obtain it online.

My apologies. You are right, of course. I had thought you meant partial agonist. I didn't read closely enough.


- Scott

 

Re: Are there any 5ht1a Inverse Agonists?

Posted by linkadge on July 28, 2017, at 10:43:22

In reply to Re: Are there any 5ht1a Inverse Agonists? Hello321, posted by SLS on July 26, 2017, at 19:51:35

No, there really are no selective inverse agonists / antagonists at 5-ht1a. I assume you've tried propranolol / pindolol, as they (supposedly) have some antagonist activity.

Transcranial magnetic stimulation supposedly down regulates 5-ht1a, which would have the same net effect as an antagonist.

Linkadge

 

Re: Are there any 5ht1a Inverse Agonists?

Posted by porkpiehat on August 2, 2017, at 10:03:04

In reply to Re: Are there any 5ht1a Inverse Agonists?, posted by linkadge on July 28, 2017, at 10:43:22

> No, there really are no selective inverse agonists / antagonists at 5-ht1a. I assume you've tried propranolol / pindolol, as they (supposedly) have some antagonist activity.
>
I have found propranolol is helpful when I get the kind of irritability and agitation I experience similar to buspar.

 

Re: Are there any 5ht1a Inverse Agonists? porkpiehat

Posted by linkadge on August 11, 2017, at 11:16:46

In reply to Re: Are there any 5ht1a Inverse Agonists?, posted by porkpiehat on August 2, 2017, at 10:03:04

I have tried propranolol, but not pindolol.

I don't know to what degree the 5-ht1a action is involved, as these two drugs are much stronger beta blockers.

Another thing to note is that propranolol may have activity at 5-ht1b receptors too (like lithium).

 

Re: Are there any 5ht1a Inverse Agonists?

Posted by Lamdage22 on August 13, 2017, at 9:09:34

In reply to Re: Are there any 5ht1a Inverse Agonists? porkpiehat, posted by linkadge on August 11, 2017, at 11:16:46

just because buspar made ypu worse doesnt automatically mean that the opposite mechanism of action will make you better.

 

Re: Are there any 5ht1a Inverse Agonists? Lamdage22

Posted by linkadge on August 14, 2017, at 10:56:46

In reply to Re: Are there any 5ht1a Inverse Agonists?, posted by Lamdage22 on August 13, 2017, at 9:09:34

Good point. Also, buspar is not a selective 5-ht1a agonist, unfortunately.


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