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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 12 of 12. This is the beginning of the thread.
Posted by Farshad on February 5, 2018, at 19:29:12
Does adderall block DAT?right now im looking at sertraline apparantly it blocks dat. Before you say wellbutrin its effects are weak on Dat not enough to produce an effect recent studies showed.
Posted by Farshad on February 5, 2018, at 19:30:17
In reply to whats a drug that blocks DAT(dopamind transporter), posted by Farshad on February 5, 2018, at 19:29:12
> Does adderall block DAT?right now im looking at sertraline apparantly it blocks dat. Before you say wellbutrin its effects are weak on Dat not enough to produce an effect recent studies showed.
ops I messed the title up meant dopamine transporter
Posted by Farshad on February 5, 2018, at 19:43:59
In reply to Re: whats a drug that blocks DAT(dopamind transporter), posted by Farshad on February 5, 2018, at 19:30:17
> > Does adderall block DAT?right now im looking at sertraline apparantly it blocks dat. Before you say wellbutrin its effects are weak on Dat not enough to produce an effect recent studies showed.
>
> ops I messed the title up meant dopamine transporter
hmm If I took both sertraline and wellbutrin would that be enough to block DAT And increase dopamine???
Posted by SLS on February 6, 2018, at 2:29:14
In reply to Re: whats a drug that blocks DAT(dopamind transporter), posted by Farshad on February 5, 2018, at 19:43:59
Methylphenidate
(Ritalin, Concerta, Focalin)
Generally, these are not good antidepressants.
In my experience, DAT inhibition (dopamine reuptake inhibition) is not sufficient to effect antidepressant effects.
Sertraline? I thought you wanted to avoid a SRI.
Intestigational dopamine/norepinephrine reuptake inhibitor:
Solriamfetol (jzp-110) DNRI: NDA submitted December, 2017
Indicated for Excessive Sleepiness Associated with Narcolepsy and Obstructive Sleep Apnea. Parkinsons?
- Scott
Posted by farshad on February 6, 2018, at 6:23:05
In reply to Re: whats a drug that blocks DAT(dopamind transporter) » Farshad, posted by SLS on February 6, 2018, at 2:29:14
> Methylphenidate
>
> (Ritalin, Concerta, Focalin)
>
> Generally, these are not good antidepressants.
>
> In my experience, DAT inhibition (dopamine reuptake inhibition) is not sufficient to effect antidepressant effects.
>
> Sertraline? I thought you wanted to avoid a SRI.
>
> Intestigational dopamine/norepinephrine reuptake inhibitor:
>
> Solriamfetol (jzp-110) DNRI: NDA submitted December, 2017
> Indicated for Excessive Sleepiness Associated with Narcolepsy and Obstructive Sleep Apnea. Parkinsons?
>
>
> - ScottMy SERT is already pretty slow so SSRI(sertraline in this case) wont make a difference for me for serotonin.
But do you know if combining wellbutrin and sertraline together will block DAT enough to increase dopamine ?
It says sertraline is stronger in blocking DAT than wellbutrin on wiki .. So wellbutrin blocks DAT 27% , Sertraline say blocks 35% , thats enough for an effect right.. they say you need to block atleast 50% to produce an anti depressant effect or somth. thats why this combo is so common too.
Posted by SLS on February 6, 2018, at 9:11:02
In reply to Re: whats a drug that blocks DAT(dopamind transporter), posted by farshad on February 6, 2018, at 6:23:05
> > Methylphenidate
> >
> > (Ritalin, Concerta, Focalin)
> >
> > Generally, these are not good antidepressants.
> >
> > In my experience, DAT inhibition (dopamine reuptake inhibition) is not sufficient to effect antidepressant effects.
> >
> > Sertraline? I thought you wanted to avoid a SRI.
> >
> > Intestigational dopamine/norepinephrine reuptake inhibitor:
> >
> > Solriamfetol (jzp-110) DNRI: NDA submitted December, 2017
> > Indicated for Excessive Sleepiness Associated with Narcolepsy and Obstructive Sleep Apnea. Parkinsons?
> >
> >
> > - Scott
>
> My SERT is already pretty slow soYou don't know that.
> SSRI(sertraline in this case) wont make a difference for me for serotonin.
You don't know that. Your statement here is in conflict with statements you have made previously.
> But do you know if combining wellbutrin and sertraline together will block DAT enough to increase dopamine ?
>
> It says sertraline is stronger in blocking DAT than wellbutrin on wikiI looked up Ki on PDSP. Sertraline is a mild DAT inhibitor, which is stronger than bupropion.
> .. So wellbutrin blocks DAT 27% , Sertraline say blocks 35% , thats enough for an effect right.
Where did you get these numbers from? Do they provide values for other drugs? I question that bupropion is 27%. That sounds rather high to me. How do you know that the effects are simply additive? Perhaps the antidepressant effect is the result of some synergistism for other reasons.
> They say you need to block atleast 50% to produce an anti depressant effect
I would be interested to know where you found that.
> thats why this combo is so common too.
My *guess* is that adding bupropion to any SRI can work. My friend needs to take bupropion in combination with desvenlafaxine in order to achieve full remission.
If you decide to commit to pro-dopamine mechanisms, you might try a combination of aripiprazole, lamotrigine, and buproprion.
- Scott
Posted by farshad on February 6, 2018, at 10:42:38
In reply to Re: whats a drug that blocks DAT(dopamind transporter), posted by SLS on February 6, 2018, at 9:11:02
> > > Methylphenidate
> > >
> > > (Ritalin, Concerta, Focalin)
> > >
> > > Generally, these are not good antidepressants.
> > >
> > > In my experience, DAT inhibition (dopamine reuptake inhibition) is not sufficient to effect antidepressant effects.
> > >
> > > Sertraline? I thought you wanted to avoid a SRI.
> > >
> > > Intestigational dopamine/norepinephrine reuptake inhibitor:
> > >
> > > Solriamfetol (jzp-110) DNRI: NDA submitted December, 2017
> > > Indicated for Excessive Sleepiness Associated with Narcolepsy and Obstructive Sleep Apnea. Parkinsons?
> > >
> > >
> > > - Scott
> >
> > My SERT is already pretty slow so
>
> You don't know that.
>
> > SSRI(sertraline in this case) wont make a difference for me for serotonin.
>
> You don't know that. Your statement here is in conflict with statements you have made previously.
>
> > But do you know if combining wellbutrin and sertraline together will block DAT enough to increase dopamine ?
> >
> > It says sertraline is stronger in blocking DAT than wellbutrin on wiki
>
> I looked up Ki on PDSP. Sertraline is a mild DAT inhibitor, which is stronger than bupropion.
>
> > .. So wellbutrin blocks DAT 27% , Sertraline say blocks 35% , thats enough for an effect right.
>
> Where did you get these numbers from? Do they provide values for other drugs? I question that bupropion is 27%. That sounds rather high to me. How do you know that the effects are simply additive? Perhaps the antidepressant effect is the result of some synergistism for other reasons.
>
> > They say you need to block atleast 50% to produce an anti depressant effect
>
> I would be interested to know where you found that.
>
> > thats why this combo is so common too.
>
> My *guess* is that adding bupropion to any SRI can work. My friend needs to take bupropion in combination with desvenlafaxine in order to achieve full remission.
>
> If you decide to commit to pro-dopamine mechanisms, you might try a combination of aripiprazole, lamotrigine, and buproprion.
>
>
> - Scott
The occupancy of dopamine transporter (DAT) sites by bupropion and its metabolites in the human brain as measured by positron emission tomography was 26% according to GlaxoSmithKline researchers .in any case, the above findings suggest that, although weak DAT occupation may occur, oral bupropion at clinically-used doses does not have the actual capacity to elevate dopamine levels in the human brain.[14] In accordance with this finding, based on analogy with serotonin reuptake inhibitors, higher than 50% inhibition of DAT would be needed for the dopamine reuptake mechanism to be a significant mechanism of the drug's action. Moreover, 65%75% DAT occupancy is necessary for euphoria and abuse potential.[82]
Tatsumi et al. (1997) found Ki values of sertraline at the human SERT, DAT, and NET of 0.29, 25, and 420 nM, respectively.[93] The selectivity of sertraline for the SERT over the DAT was 86-fold.[93] In any case, of the wide assortment of antidepressants assessed in the study, sertraline showed the highest affinity of them all for the DAT, even higher than the norepinephrinedopamine reuptake inhibitors (NDRIs) nomifensine (Ki = 56 nM) and BUPROPION (Ki = 520 nM).[93][104] Sertraline also has similar affinity for the DAT as the NDRI methylphenidate (Ki = 24 nM).[93][104] Tametraline (CP-24,441), a very close analogue of sertraline and the compound from which sertraline was originally derived, is an NDRI that was never marketed.[109]
So if wellbutrin alone is 27% and sertraline has higher affinity for dat than wellbutrin it should equal more than 50% if taken together thus produce an effect.
Posted by Christ_empowered on February 6, 2018, at 11:28:55
In reply to Re: whats a drug that blocks DAT(dopamind transporter), posted by farshad on February 6, 2018, at 10:42:38
ask your doctor for provigil, nuvigil, maybe ritalin or focalin. zoloft is one of the most numbing, apathy-inducing ssri drugs out there, especially as the dose goes up.
some doctors are using mirapex, off label, for psychiatric stuff. maybe that'd be a good option?
Posted by farshad on February 6, 2018, at 11:44:00
In reply to Re: whats a drug that blocks DAT(dopamind transporter), posted by Christ_empowered on February 6, 2018, at 11:28:55
> ask your doctor for provigil, nuvigil, maybe ritalin or focalin. zoloft is one of the most numbing, apathy-inducing ssri drugs out there, especially as the dose goes up.
>
> some doctors are using mirapex, off label, for psychiatric stuff. maybe that'd be a good option?modafinil is very weak dont think it blocks DAT look here:
https://en.wikipedia.org/wiki/Dopamine_reuptake_inhibitor
I want one blocks dopamine transporter thus increasing dopamine neurotransmission all over the brain.Sertraline and wellbutrin seem to be the only option taken together. Wellbutrin can also off set some of the side effects from sertraline.
hmm ritalin I guess could work...... can you take that everyday?
ritalin half life is short so that why sertraline still makes more sense , sertraline half life is 26 hours.
if you can find a drug that blocks DAT and has a long half life let me know.
Posted by Christ_empowered on February 6, 2018, at 12:58:50
In reply to Re: whats a drug that blocks DAT(dopamind transporter), posted by farshad on February 6, 2018, at 11:44:00
there are a number of long acting ritalin and focalin preparations on the market. zoloft+wellbutrin can be effective for some forms of depression, but I wouldn't say that adding wellbutrin off sets "side effects." adding wellbutrin to ongoing ssri further alters brain chemistry, which may or may not be a good thing.
Posted by SLS on February 6, 2018, at 15:03:25
In reply to Re: whats a drug that blocks DAT(dopamind transporter), posted by farshad on February 6, 2018, at 10:42:38
I hope you didn't depend on a cherry-picked post located on a public forum. Bupropion is also quoted as occupying only 14% of DAT in the original article to be found here:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC514842/
Even the 14% is not a reliable value as is described in the article.
Modafinil is often cited as being a DAT inhibitor.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2696807/
Again, DAT inhibition is not sufficient for a compound to produce an antidepressant effect.
Where did you find the numbers regarding DAT occupancy as it relates to antidepressant and euphoric effects?
What drugs are you considering tying given the information you have compiled?
- Scott
Posted by farshad on February 6, 2018, at 15:13:53
In reply to Re: whats a drug that blocks DAT(dopamind transporter) » farshad, posted by SLS on February 6, 2018, at 15:03:25
> I hope you didn't depend on a cherry-picked post located on a public forum. Bupropion is also quoted as occupying only 14% of DAT in the original article to be found here:
>
> https://www.ncbi.nlm.nih.gov/pmc/articles/PMC514842/
>
> Even the 14% is not a reliable value as is described in the article.
>
> Modafinil is often cited as being a DAT inhibitor.
>
> https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2696807/
>
> Again, DAT inhibition is not sufficient for a compound to produce an antidepressant effect.
>
> Where did you find the numbers regarding DAT occupancy as it relates to antidepressant and euphoric effects?
>
> What drugs are you considering tying given the information you have compiled?
>
>
> - Scottwell the creators of wellbutrin said its at 27% -
https://drugs-forum.com/threads/bupropion-doesnt-actually-increase-dopamine-new-info.263168/
Wellbutrin inhibits at 27% , sertraline is a stronger inhibitor of DAT than wellbutrin so it has to be more than 27% so the 2 together 50% DAT inhibition = anti depressant effect
The DAT occupancy was just based of SERT , Since serotonin transporter inhibition needs to be over 50% to produce an anti depressant effect, Thus I assumed same for The Dopamine transporter but I could be wrong
This is the end of the thread.
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