idontknow-78
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Amineptine methyl ester pharmacodynamics
Hello everyone, I wanted to know from those who are more experienced, if anyone knows the pharmacodynamics of amineptine methyl ester. on this site:
https://www.benchchem.com/product/b565756
They talk in detail about its antidepressant, anxiolytic and pain-relieving properties, but unfortunately no scientific article is cited as a
reference, so I don't know where this information was taken from, nor whether it is reliable. I personally couldn't find anything on Pubmed. can
someone help me? also, does this methyl refer to methane or methanol? Thank you
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paulll
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Neither methane nor methanol. I hope I'm not being overly presumptuous here but, if you look at the structural model on the site you linked, there's a
line sticking off the O at the bottom. This denotes a carbon single-bonded to the oxygen, and that all the other valence spots on said carbon are
taken up by a hydrogen. 4 spots, one occupied by the bond with the oxygen, leaving -CH3, a methyl group. The fact that that methyl group is
single-bonded onto that oxygen is the difference between, "amineptine methyl ester," and amineptine.
Kinetically, I'd be astonished to find that this molecule doesn't readily hydrolise in vivo, yielding amineptine, and actually yes, there's your
methanol. So it's a effectively a prodrug for amineptine, and a shitty one at that; amineptine didn't get traction partly because it's a bit of a
blunt instrument but also because it has potentially wild hepatotoxicity.
Dynamically, it would appear to be a potentially more hepatoxic version of amineptine, nothing more. I see scepticism in your post and I think that's
barking up the right tree; the link says it's a serotonin agonist whereas amineptine has a very, very low affinity for 5HT receptors.
It's a bullshit molecule.
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CouchHatter
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I would also be skeptical of any drug with 'inept' in the name.
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idontknow-78
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Quote: Originally posted by paulll  | Neither methane nor methanol. I hope I'm not being overly presumptuous here but, if you look at the structural model on the site you linked, there's a
line sticking off the O at the bottom. This denotes a carbon single-bonded to the oxygen, and that all the other valence spots on said carbon are
taken up by a hydrogen. 4 spots, one occupied by the bond with the oxygen, leaving -CH3, a methyl group. The fact that that methyl group is
single-bonded onto that oxygen is the difference between, "amineptine methyl ester," and amineptine.
Kinetically, I'd be astonished to find that this molecule doesn't readily hydrolise in vivo, yielding amineptine, and actually yes, there's your
methanol. So it's a effectively a prodrug for amineptine, and a shitty one at that; amineptine didn't get traction partly because it's a bit of a
blunt instrument but also because it has potentially wild hepatotoxicity.
Dynamically, it would appear to be a potentially more hepatoxic version of amineptine, nothing more. I see scepticism in your post and I think that's
barking up the right tree; the link says it's a serotonin agonist whereas amineptine has a very, very low affinity for 5HT receptors.
It's a bullshit molecule. |
https://www.smolecule.com/products/s986877
Here on this site, however, there is an even longer and more detailed description of the first site, while in the first site they talk about action on
serotonin, here they talk about action on dopamine, all obviously without citing even the slightest scientific article as a reference .
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idontknow-78
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| Quote: Originally posted by paulll | Neither methane nor methanol. I hope I'm not being overly presumptuous here but, if you look at the structural model on the site you linked, there's a
line sticking off the O at the bottom. This denotes a carbon single-bonded to the oxygen, and that all the other valence spots on said carbon are
taken up by a hydrogen. 4 spots, one occupied by the bond with the oxygen, leaving -CH3, a methyl group. The fact that that methyl group is
single-bonded onto that oxygen is the difference between, "amineptine methyl ester," and amineptine.
Kinetically, I'd be astonished to find that this molecule doesn't readily hydrolise in vivo, yielding amineptine, and actually yes, there's your
methanol. So it's a effectively a prodrug for amineptine, and a shitty one at that; amineptine didn't get traction partly because it's a bit of a
blunt instrument but also because it has potentially wild hepatotoxicity.
Dynamically, it would appear to be a potentially more hepatoxic version of amineptine, nothing more. I see scepticism in your post and I think that's
barking up the right tree; the link says it's a serotonin agonist whereas amineptine has a very, very low affinity for 5HT receptors.
It's a bullshit molecule. |
What makes you think that it could have more hepatotoxicity than amineptine hcl?
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paulll
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Because its hydrolysis will give methanol. A trivial amount, realistically, but still.
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idontknow-78
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| Quote: Originally posted by paulll | Neither methane nor methanol. I hope I'm not being overly presumptuous here but, if you look at the structural model on the site you linked, there's a
line sticking off the O at the bottom. This denotes a carbon single-bonded to the oxygen, and that all the other valence spots on said carbon are
taken up by a hydrogen. 4 spots, one occupied by the bond with the oxygen, leaving -CH3, a methyl group. The fact that that methyl group is
single-bonded onto that oxygen is the difference between, "amineptine methyl ester," and amineptine.
Kinetically, I'd be astonished to find that this molecule doesn't readily hydrolise in vivo, yielding amineptine, and actually yes, there's your
methanol. So it's a effectively a prodrug for amineptine, and a shitty one at that; amineptine didn't get traction partly because it's a bit of a
blunt instrument but also because it has potentially wild hepatotoxicity.
Dynamically, it would appear to be a potentially more hepatoxic version of amineptine, nothing more. I see scepticism in your post and I think that's
barking up the right tree; the link says it's a serotonin agonist whereas amineptine has a very, very low affinity for 5HT receptors.
It's a bullshit molecule. |
When you talked about hydrolosis, did you mean that once ingested, this molecule would be metabolized and/or split into amineptine hcl? correct me if
I'm wrong. if this were the case, what would have been the point of marketing amineptine hcl, it would have been enough to sell this reagent
directly. also, forgive me my ignorance, but in general aren't the methylated forms simply more absorbable? for example, methylcobalamin is more
absorbable than cyanocobalamin. could it be the same for amineptine or is that a very simplistic way of looking at it? Thanks
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idontknow-78
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Methyl ester pharmacodynamic?
Hello everyone, I wanted to know if it is true that the methylated esters of a molecule, once ingested, are "freed/transformed" into the basic
molecule and that this process occurs either in the stomach, thanks to its acidic environment or in the intestine thanks to its basic environment.
also, can this process happen in reverse? that is, after ingesting a molecule, during digestion/metabolism, can it be released/transformed into its
methyl ester form? Thank you
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Texium
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Yes, most ingested esters will undergo acid hydrolysis in the stomach or be cleaved by esterase enzymes. I am not aware of any human metabolic route
that results in forming a methyl ester, though I am not a medicinal chemist. My understanding is that carboxylic acids are often excreted unchanged,
or conjugated to other molecules like glycine (see hippuric acid). Fatty acids, possibly including the one I assume you're referring to, can also be
oxidized and sliced up by enzymes to make acetyl-CoA for the Krebs cycle.
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Texium
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Threads Merged
10-11-2023 at 11:28 |
idontknow-78
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I'm referring to amineptine methyl ester behaviour
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Texium
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Yes, that was rather obvious since it seems to be your obsession for some reason.
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idontknow-78
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It's not an obsession, it's a health problem. I finally managed to obtain a synthesis of amineptine hcl, but a small percentage of this methyl ester
is present. no one can tell me clearly and unequivocally whether this ester is released as active ingredient in the stomach or a way to purify it .
some say yes, others no, but no one has shown me scientific documentation to support one hypothesis or another. even those who sell this ester
declare different pharmavodynamics / kinetics without showing any documentation. For example :
https://www.smolecule.com/products/s986877
https://www.benchchem.com/product/b565756
[Edited on 14-11-2023 by idontknow-78]
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Texium
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A health problem that you're trying to self-medicate? In your
first post you said you work in an analytical lab, implying that it was needed as an analytical sample. It's sounding more and more like you want to
ingest it. Per the forum guidelines: | Quote: | | Reported syntheses must be carried out on a small scale and be clearly motivated by intellectual interest, not commercial aspirations or a
desire to ingest the resulting substance. |
We are not qualified to give medical advice. If you have a health problem that may require medication you need to talk to a doctor, not an amateur
chemistry forum. I am locking this thread now and I suggest you seek medical advice from a more appropriate source.
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Texium
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Thread Closed
14-11-2023 at 10:58 |
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