![[dr. bob]](/dr-bob-sm.gif)
Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 4 of 4. This is the beginning of the thread.
Posted by SLS on August 18, 2020, at 22:25:18
Someone asked me if I knew of any glutamate release inhibitors. The first drug to pop into my head was lamotrigine. However, the new "antipsychotic", Caplyta (lumateperone), works to lower glutamate activity secondary to its agonism of D1 receptors. Lumateperone is also a potent 5-HT2a receptor antagonist, but has low affintiy for D2 receptors.
Glutamatergic neurotransmission isn't the easiest to figure out. Sometimes it makes more sense to look at what brain structures or neural tracts are activated or inhibited by exposure to a drug. It might be a good idea to follow lumateperone to see if it has any utility in unipolar or bipolar disorders.
The reason I put "antipsychotic" in quotes is because a chemical compound doesn't always know what it's supposed to be.
- Scott
Posted by linkadge on August 19, 2020, at 12:42:32
In reply to Caplyta (lumateperone) - Reduces glutamate., posted by SLS on August 18, 2020, at 22:25:18
Looking at the wikipedia article, it almost seems to be a selective 5-ht2a antagonist:
5-HT2A0.54
Dopamine receptor D141
Serotonin transporter33
Dopamine receptor D232
Dopamine receptor D4<100
Alpha-1A adrenergic receptor<100
Alpha-1B adrenergic receptor<100
There was another selective 5-ht2 antagonist (pimavanserin) released recently for Parkinson's releated hallucinations. Interestingly blocking 5-ht2a produces downstream effects on GSK3, which then in turn modulates D2 receptor sensitivity. In some models selective 5-ht2a antagonists are antipsychotic.Linkadge
Posted by undopaminergic on August 20, 2020, at 2:55:33
In reply to Re: Caplyta (lumateperone) - Reduces glutamate., posted by linkadge on August 19, 2020, at 12:42:32
> Looking at the wikipedia article, it almost seems to be a selective 5-ht2a antagonist:
>
> 5-HT2A0.54
> Dopamine receptor D141
> Serotonin transporter33
> Dopamine receptor D232
> Dopamine receptor D4<100
> Alpha-1A adrenergic receptor<100
> Alpha-1B adrenergic receptor<100
>I wonder if they might mean >100.
-undopaminergic
Posted by linkadge on August 20, 2020, at 9:02:41
In reply to Re: Caplyta (lumateperone) - Reduces glutamate., posted by undopaminergic on August 20, 2020, at 2:55:33
Yeah. Probably.
Linkadge
This is the end of the thread.
Psycho-Babble Medication | Extras | FAQ
Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.org
Script revised: February 4, 2008
URL: http://www.dr-bob.org/cgi-bin/pb/mget.pl
Copyright 2006-17 Robert Hsiung.
Owned and operated by Dr. Bob LLC and not the University of Chicago.