[HN Gopher] Small molecule cognitive enhancer reverses age-relat...
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       Small molecule cognitive enhancer reverses age-related memory
       decline in mice
        
       Author : clockworksoul
       Score  : 100 points
       Date   : 2022-10-15 15:20 UTC (7 hours ago)
        
 (HTM) web link (pubmed.ncbi.nlm.nih.gov)
 (TXT) w3m dump (pubmed.ncbi.nlm.nih.gov)
        
       | IndigoIncognito wrote:
       | I need this, I just caught covid recently and I struggled to read
       | the title
        
         | [deleted]
        
         | mrtesthah wrote:
         | Your microglial cells are overly reactive.
         | https://www.sciencedirect.com/science/article/pii/S009286742...
         | 
         | Try NAC, CBD, PEA (Palmitoylethanolamide;
         | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9406356/), DHA/EPA
         | (fish oil) and other things to reduce brain inflammation.
         | 
         | But trans-ISRIB looks exactly on point in its particular
         | mechanism.
         | 
         | You can already import it in bulk from manufacturers like
         | nutrabiotechchem.com.
        
           | jokowueu wrote:
           | Never heard of netrabio before and I'm generally knowledgable
           | about such sites
           | 
           | Also Are you currently on any discord servers ?
        
           | derefr wrote:
           | How about cerebrolysin? A friend of mine who suffered a
           | traumatic brain injury swears by it.
        
       | norwalkbear wrote:
       | Just a reminder mouse physiology is not human. This is a great
       | start but hacking biology is not the same as pcs.
       | 
       | I add this warning because I'm seeing a lot of younger software
       | engineers try out custom peptides to boost their iq, memory, and
       | work ability.
        
         | [deleted]
        
         | Avicebron wrote:
         | Also laboratory mice are not necessarily comparable to the
         | diversity in genetics of even wild mice (or the genetic
         | diversity of the human population if we want to extrapolate).
        
         | causi wrote:
         | _I add this warning because I 'm seeing a lot of younger
         | software engineers try out custom peptides to boost their iq,
         | memory, and work ability._
         | 
         | Eh, I say let 'em. People need to stop pretending aging isn't a
         | tragedy just because it's our natural state. We should be as
         | bold with treatments for it as we are with treatments for other
         | fatal diseases.
        
           | generalizations wrote:
           | Just get them to write down their results somewhere. Enough
           | anecdotes might turn into anecdata.
        
             | bglazer wrote:
             | Me and every one of my friends have seen this horse named
             | Hans, very clever, that could understand everything its
             | trainer said. He could do arithmetic too! I don't
             | understand why big psychology won't take our data seriously
             | and finally accept that horses are capable of long
             | division.
        
             | treeman79 wrote:
             | Did this a lot when I was having severe dementia problems.
             | Would track results on various medications to see what
             | worked.
             | 
             | 95% made a bad situation much worse. Memantine Had a
             | moderate boost.
             | 
             | Went on a Blood thinner and everything resolved.
        
               | mota7 wrote:
               | Do you know why the blood thinners helped? (I'm assuming
               | there was some underlying condition that this treated?)
        
           | tsol wrote:
           | >People need to stop pretending aging isn't a tragedy just
           | because it's our natural state. We should be as bold with
           | treatments for it as we are with treatments for other fatal
           | diseases.
           | 
           | We don't encourage people to experiment with self medicating
           | themselves for cancer and multiple sclerosis, because it's
           | dangerous and most people have no idea what they're doing.
           | It's pretty much the same thing here. I know it'll happen
           | either way, but I wouldn't recommend it to the average
           | person.
        
             | causi wrote:
             | _I know it 'll happen either way, but I wouldn't recommend
             | it to the average person._
             | 
             | Hence "let them", not "encourage them". The average person
             | doesn't have the slightest idea what a "custom peptide" is.
        
               | whatshisface wrote:
               | But you're responding to a warning with "let them," not a
               | bill in congress.
        
       | pfisherman wrote:
       | If you are looking for a cognitive enhancer then caffeine and
       | modafinil / provigil have been proven to enhance focus. I believe
       | that latter of those is used extensively by fighter pilots and
       | other military to stay alert; and the former is used by pretty
       | much everybody for the same purpose.
       | 
       | I know drink a cup of coffee is probably not the answer a lot of
       | the nootropic heads are looking for; but I don't think there are
       | any silver bullets here.
        
         | x86x87 wrote:
         | On top of that coffee also contains chlorogenic acid which
         | allegedly is good for longevity
        
           | stjohnswarts wrote:
           | This is one of the reasons I switched to fine mesh coffee
           | filter (metal) a while back, instead of paper filters, hoping
           | to get more of the goodness of coffee in me. Although it does
           | let cafestol through as well, but that doesn't seem like much
           | of a big deal if you don't have any cholesterol issues.
        
             | giardini wrote:
             | Try a Vietnamese coffee maker: they're little more than a
             | stainless steel filter and cost only a few bucks. The
             | coffee is _strong_ :
             | 
             | https://www.wikihow.com/Make-Vietnamese-Coffee
             | 
             | Oh, the usual coffee is "Cafe Du Monde" (in the orange
             | can).
        
         | giardini wrote:
         | A cup of coffee beats provigil's side-effects:
         | 
         |  _skin rash or hives, blisters or peeling, mouth sores, trouble
         | breathing or swallowing, fever, swelling in your legs, dark
         | urine, yellowing of your skin or eyes, or swelling in your
         | face_!? And there 's more: https://www.drugs.com/provigil.html
         | 
         | Modafinil/provigil might be worse than crack!
        
           | HyperSane wrote:
           | I have used provigil and had zero side effects. All it does
           | is allow me to code for many hours.
        
         | zoklet-enjoyer wrote:
         | I've taken adrafinil off and on over the years and it doesn't
         | do much of anything for me. Not sure if I'm expecting too much
         | or what's going on with that.
        
       | csdvrx wrote:
       | As usual, I fear comments will focus on the "in mice" part,
       | forgetting that for most base circuits (ex: brain, nerves ...)
       | and physiology (scarring, aging, inflammation ...) they are
       | extremely close.
       | 
       | Also, other "cognitive enhancers" have usually found effects in
       | both rodents and primates.
        
         | stjohnswarts wrote:
         | then why do 98% of these "promising" results turn out to be
         | ineffectual in humans if we're that close biologically?
        
         | [deleted]
        
         | BoorishBears wrote:
         | And instead as usual, any useful commentary will be drowned out
         | by people rushing over themselves to point out that humans
         | aren't mice.
        
           | glenstein wrote:
           | Exactly. I feel like it's the equivalent of the Onion article
           | that pokes fun at that type of behavior:
           | 
           | >Learned Sage Points Out That Powerball Not As Much After
           | Taxes https://www.theonion.com/learned-sage-points-out-that-
           | powerb...
           | 
           | Whether it's mice or powerball, the lowest hanging fruit is
           | the Learned Sage comment, noting that things aren't quite as
           | they seem.
        
         | mtlmtlmtlmtl wrote:
         | It's not just a question of efficacy, but also safety, which
         | can depend on more than just the systems relevant to efficacy.
        
         | civilized wrote:
         | And then someone will come in and tell you that most things
         | tried in mice don't work out in humans, and we will issue a
         | collective shrug as we don't know what to believe.
        
           | ethanbond wrote:
           | The nice thing is that you don't need to decide what to
           | believe. You just keep doing experiments and, if well
           | designed, they'll tell you what's true anyway. These animal
           | model experiments are not intended to prove applicability to
           | humans, they're intended to prove that you can take the next
           | (tiny) step along the (extremely long) road to human
           | applicability.
        
             | glenstein wrote:
             | Which in and of itself is sufficient to proceed with "huh,
             | cool! keep up this line of research!"
        
           | gfodor wrote:
           | Mice shedding
        
           | csdvrx wrote:
           | What doesn't work in mice is typically for mouse-models of
           | diseases: we try to replicate a disease based on what we
           | think causes it, then try to cure it.
           | 
           | That's typical for cancer, Alzheimer etc. No wonder the
           | things tried in the toy problem don't work out when faced
           | with the real problem!
           | 
           | The problem isn't so much the mice being so different, but
           | the disease itself being very different from the toy problem.
        
             | civilized wrote:
             | So how is the enhancer mouse research different from the
             | disease mouse research that you acknowledge often doesn't
             | work?
        
               | csdvrx wrote:
               | It isn't tried on a disease model, but on a core
               | mechanism: aging.
        
               | Avicebron wrote:
               | spherical mice.
        
               | civilized wrote:
               | This all hinges on the idea that, while disease is too
               | different between species for insights to transfer well,
               | aging isn't like that?
        
               | glenstein wrote:
               | Right. Their first comment was about the similarity of,
               | in their words, base circuits and physiology.
        
               | civilized wrote:
               | I just don't know if it's obvious that aging is a matter
               | of base circuits and physiology and disease is less so.
        
       | strangattractor wrote:
       | I was just getting use to calling whatchamcallit thingamabob:)
        
       | SnowHill9902 wrote:
       | What's the catch? It's usually less plasticity.
        
       | michaelangerman wrote:
       | Eventually we will figure out how these chemicals work to combat
       | a disease that is currently not well understood. Great news !
        
         | csdvrx wrote:
         | It says in the first line "The integrated stress response (ISR)
         | is activated during aging"
         | 
         | Odds are the same basic mechanism is activated by many other
         | things, including some inflammation process.
        
           | galangalalgol wrote:
           | Yeah, I am considering purchasing ISRB "for research". Some
           | people I love suffer with chronic inflammation due to various
           | autoimmune diseases. I know plenty of amateur body builders
           | buy chemicals "for research" but use them as supplements.
           | They keep tabular and video artifacts like most body builders
           | do, so I wonder to what degree the activities are illegal?
        
             | voldacar wrote:
             | The problem with ISRIB is that it isn't water soluble. I'm
             | not convinced that people who take it (usually subcutaneous
             | injection or snorting it) aren't just experiencing placebo.
             | I don't know of any way of actually getting the molecule to
             | your body's cells in a consistent manner.
        
               | galangalalgol wrote:
               | The study dissolved it in DMSO, then that in polysorbate
               | 80, then that in polyethylene glycol. Then injected that
               | intraperitoneally. That seems doable.
        
               | voldacar wrote:
               | Intraperitoneal injection isn't really done in humans,
               | the closest equivalent would be subcutaneous or maybe
               | intramuscular injection. I don't know about the safety of
               | injecting DMSO into humans but it's probably not too bad
               | since it seems perfectly safe when used for transdermal
               | drug delivery. The bigger problem is that you're
               | injecting a water-insoluble compound mixed in a small
               | amount of solvent into what is essentially a big bag of
               | water. Once that DMSO/PEG/whatever is injected, it will
               | just mix with the water in your body, so the ISRIB will
               | just precipitate out of solution since it is now
               | surrounded by 99% water molecules. So it will never get
               | distributed to all your organs, which is the goal.
        
               | whatshisface wrote:
               | I could be missing something, but since your cells are
               | separated by water, it doesn't matter how many steps you
               | take to get it in your body.
        
               | galangalalgol wrote:
               | DMSO is soluble in both polar and non polar solvents. I
               | assume the insolubility in water is precisely what they
               | used it to solve. Im any case, their delivery mechanism
               | worked in mice, so it would work in people. The part that
               | might not carry over to people is the effect once in the
               | cell.
        
             | csdvrx wrote:
             | No idea, but unless it's on a restricted list (classified
             | by the DEA), I think "not at all".
        
       | derefr wrote:
       | For what it's worth, just as an amateur chemist staring hard at
       | the molecule, it looks like the ligand (the outer bit that plugs
       | into receptor binding sites) consists of a monochlorinated
       | benzene ring. Which would likely put this in the same drug class
       | as https://en.wikipedia.org/wiki/Bromantane, whose ligand is a
       | _monobrominated_ benzene ring -- and which is also a  "cognitive
       | enhancer" nootropic with a thusfar not well understood mechanism-
       | of-action.
       | 
       | The naive assumption some people make is that bromantane (and so
       | probably also ISRIB) would have an at least partially similar MoA
       | to amphetamine, given that amphetamine has a plain old benzene
       | ring hanging off of one end of it; but IIRC that is incorrect,
       | as, in amphetamine, the benzene is not the ligand -- rather, the
       | amide group on the other end is.
        
         | toddm wrote:
         | Computational chemist here, working at the moment on small
         | molecule ligands in the context of drug discovery.
         | 
         | The small molecule itself is the ligand. There is interaction
         | of the ligand with the binding site amino acids via hydrogen
         | bonds to several locations on the ligand.
         | 
         | Have a look at the RCSB PDB entry for 6EZO - ISRIB bound to
         | eIF2B (the 3D view is https://www.rcsb.org/3d-view/6EZO), turn
         | on Dynamic Bonds and click on the ligand.
         | 
         | While this static shot does not reveal all the interactions
         | (such as those that are longer-range, cation-pi, water-
         | mediated, and so on) that one would see in a molecular dynamics
         | simulation or by docking, it's very useful.
         | 
         | Finally, when benzene is attached to something, it's a phenyl
         | group; amphetamine is the ligand; and the functional group is
         | amine, not amide.
        
           | derefr wrote:
           | Thanks for that.
           | 
           | Is there a term for a part of a molecule that takes part in
           | "medium range" interactions -- making the molecule
           | electrostatically attracted toward/repulsed away from
           | specific macromolecule binding sites, like is happening with
           | the hydrogen bonds here -- but which don't then take part in
           | any kind of redox or polymerization reaction once the
           | molecule reaches close enough for such to take place? Because
           | that's what I meant here by trying to distinguish which part
           | of these molecules is the ligand: which part is getting
           | directly chemically reacted with / away (triggering the state
           | change in the receptor), vs. the part being interacted with
           | only indirectly in the sense of "a key that fits into a
           | molecular lock vs. a key that doesn't".
           | 
           | What I've been told is that the phenyl group in amphetamine
           | isn't reacted with / reacted away by a DA receptor binding
           | site, but rather just gives it its binding affinity by being
           | the right shape to fit into (and the right charge + mass to
           | be attracted by) DAR and DATR binding sites without the
           | indirect forces of the "walls" of these receptors repulsing
           | it.
           | 
           | Under this logic (if it's sound, which you seem to be saying
           | it's not), a brominated phenyl group would really just be a
           | bromide ion in direct reaction terms -- it'd theoretically
           | attach to any chloride channel. The phenyl group it's riding
           | on, would -- along with the rest of the molecule -- serve to
           | ensure that the bromide ion only gets to come into contact
           | with chloride channels inside receptors that allow a phenyl
           | group inside them, rather than repulsing phenyl groups, or
           | not being the right shape to accept phenyl groups.
           | 
           | (This logic -- again, if sound -- would also suggest that
           | chlorhexidine would have a similar nootropic effect if it
           | could cross the blood-brain barrier.)
        
       | dzink wrote:
       | Mice will take over the world. We've fixed aging, cancer, and a
       | lot of other issues in Mice, so now they will outlive us.
        
         | Stupulous wrote:
         | I would love to see a project to raise optimized mice using the
         | tremendous amount of research on them. Is anyone doing that
         | already?
        
           | stjohnswarts wrote:
           | That would be pretty good, apply the best cancer prevention,
           | longevity producing, cancer protecting treatments available
           | to 100 mice, compared to the diet of a typical American in
           | 100 other mice (not very ethical I know) and see what
           | happens.
        
         | [deleted]
        
         | Silverback_VII wrote:
         | I for one do not understand that we do not share our
         | discoveries with nature. After all these animal
         | experimentations we have big debt. It would only be decent to
         | give something back. I think we already made stronger and
         | smarter(with human brain cells) mice. What if make every wild
         | animal smarter in the same fashion? Can we also improve
         | photosynthesis?
        
         | sinenomine wrote:
         | Of course translational research is necessary with such
         | results. Explicit goal of developing cognitive enhancing
         | therapies set by NIH would greatly help motivate such research.
        
       | ProjectArcturis wrote:
       | I'll offer 100-1 odds that this never turns into a human
       | treatment.
        
         | minifridge wrote:
         | ISRIB has toxic effects on the liver, afaik from presentations
         | i have seen. So yeah, unlikely it is going to pass any clinical
         | trial
        
         | computerphage wrote:
         | I'll take the bet. I pay you when it "never" does, and you pay
         | me if it ever does. How does $1 and $100 sound?
        
           | ProjectArcturis wrote:
           | Engineers are the worst.
        
             | qart wrote:
             | The bet might work in your favor. Lots of candiate drugs
             | are discarded for reasons like... having harmful side-
             | effects, being found useless, etc.
        
           | RichardCNormos wrote:
           | I, too, keep my specifics in the pedantry.
        
         | [deleted]
        
         | dang wrote:
         | " _Please don 't post shallow dismissals, especially of other
         | people's work. A good critical comment teaches us something._"
         | 
         | https://news.ycombinator.com/newsguidelines.html
        
         | [deleted]
        
         | gthippo wrote:
         | ISRIB is licensed by Calico which recently initiated phase I
         | trials for its use in ALS
         | (https://www.massgeneral.org/news/press-
         | release/investigation...)
        
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