Nagelfar
Bluelight Crew
Vortioxetine is a SARI & SPARI (serotonin antagonist and reuptake inhibitor & serotonin partial agonist & reuptake inhibitor)
This drug is quite interesting, it is a:
quasi-full-agonist of the 5-HT1A serotonin receptor
& a partial agonist to the 5-HT1B receptor
Which both mediate anti-depressant effects.
While other serotonin receptors which actually inhibit anti-depressant effects:
the receptors:
5-HT1D, 5-HT3A & 5-HT7
...are all antagonized.
While inhibiting the reuptake of serotonin at SERT (the serotonin transporter) & norepinephrine at NET.
Most anti-depressants are SSRIs, which selectively inhibit serotonin in favor of the other monoamines: norepinephrine (NE) and dopamine (DA), but this effects *all* of the serotonin receptors by flooding the synapses with a serotonin efflux which agonizes (activates) them all, even the receptors which have been shown to *increase* depressive mood instability rather than correct it (however on a broad spectrum, the number of receptors which do good for depression outweigh those that do bad). However, this drug, not only directly stimulates the receptors that do good for ones mood as a direct agonist itself (which most anti-depressants do not do) it also blocks, or 'antagonizes' the receptors which cause negative influences to ones emotional state: effectively blocking the serotonin that it is responsible in mediating the increase in from working on the receptors which diminish the efficacy of its purpose as an anti-depressant.
It's neither a pro-drug nor does it have active metabolites and has a half life of 66 hours. It has been shown to enhance memory in rats; which means it is also potentially a nootropic drug.
...
Also the same drug company that makes it, Lundbeck, is in phase 2 clinical trials of Tedatioxetine; a drug which is only a methyl & a nitrogen away from Vortioxetine, but has some major differences (as most such minor changes in QSAR similarly alter affinity in drastic ways & measures). Tedatioxetine is additionally a dopamine reuptake inhibitor at DAT while continuing to inhibit both SERT & NET, but it is not an agonist of any receptor, but rather only an antagonist at 5-HT2A, 5-HT2C & 5-HT3 serotonin receptors.
Tedatioxetine:
I think this kind of multi-functional serotonin "modulator" is the future of anti-depressants; and it's trials have been great for effectiveness. There will be no generic for some time since the brand name Brintellix for Vortioxetine was only approved in 2013, but I'd love to be able to get on this to treat my own major depression, though my government insurance hinders me from non-generics.
Now all they need to add is true 'positive allosteric modulation' of the differing monoamine transporters, such as SoRI-20041. SoRIs & SARIs.
This drug is quite interesting, it is a:
quasi-full-agonist of the 5-HT1A serotonin receptor
& a partial agonist to the 5-HT1B receptor
Which both mediate anti-depressant effects.
While other serotonin receptors which actually inhibit anti-depressant effects:
the receptors:
5-HT1D, 5-HT3A & 5-HT7
...are all antagonized.
While inhibiting the reuptake of serotonin at SERT (the serotonin transporter) & norepinephrine at NET.
Most anti-depressants are SSRIs, which selectively inhibit serotonin in favor of the other monoamines: norepinephrine (NE) and dopamine (DA), but this effects *all* of the serotonin receptors by flooding the synapses with a serotonin efflux which agonizes (activates) them all, even the receptors which have been shown to *increase* depressive mood instability rather than correct it (however on a broad spectrum, the number of receptors which do good for depression outweigh those that do bad). However, this drug, not only directly stimulates the receptors that do good for ones mood as a direct agonist itself (which most anti-depressants do not do) it also blocks, or 'antagonizes' the receptors which cause negative influences to ones emotional state: effectively blocking the serotonin that it is responsible in mediating the increase in from working on the receptors which diminish the efficacy of its purpose as an anti-depressant.
It's neither a pro-drug nor does it have active metabolites and has a half life of 66 hours. It has been shown to enhance memory in rats; which means it is also potentially a nootropic drug.
...
Also the same drug company that makes it, Lundbeck, is in phase 2 clinical trials of Tedatioxetine; a drug which is only a methyl & a nitrogen away from Vortioxetine, but has some major differences (as most such minor changes in QSAR similarly alter affinity in drastic ways & measures). Tedatioxetine is additionally a dopamine reuptake inhibitor at DAT while continuing to inhibit both SERT & NET, but it is not an agonist of any receptor, but rather only an antagonist at 5-HT2A, 5-HT2C & 5-HT3 serotonin receptors.
Tedatioxetine:
I think this kind of multi-functional serotonin "modulator" is the future of anti-depressants; and it's trials have been great for effectiveness. There will be no generic for some time since the brand name Brintellix for Vortioxetine was only approved in 2013, but I'd love to be able to get on this to treat my own major depression, though my government insurance hinders me from non-generics.
Now all they need to add is true 'positive allosteric modulation' of the differing monoamine transporters, such as SoRI-20041. SoRIs & SARIs.
