379 replies to this topic

[FrankMH]

Count me in please. Much appreciated.

[DorianGray]

Depending on the price and from where the IDRA-21 would be shipped from (I am from Germany), I would be in.

[Patrick Sylvester]

please count me in.
and i hope this ends the cross pollination

Really, if this ..... doesnt work out I dont know what will.

prl/nsi/cx ###/org26576/s18986/pepa/dihexia/isoxazole9/glyx13/c16
i don't imagine your done just yet.

[FrankMH]

Has it been confirmed that benzo withdrawal isn't a potential issue with this compound?

[Reformed-Redan]

Has it been confirmed that benzo withdrawal isn't a potential issue with this compound?

I have never head of any such thing. The benzene ring is just there to bind to the AMPA receptors. The fact that benzos bind to GABA a&b receptors and that this compound has a benzine ring is no cause for alarm.

I read some studies that there were no issues with repeated dosing and loss of activity on AMPA receptors. Will look for it later.

Edited by yadayada, 16 May 2013 - 07:42 PM.

[megatron]

I'm in as usual :P

[Psionic]

Please count me in too. More details needed

[gamesguru]

In.

[Artificiality]

Any news on the price, ScienceGuy?

Count me in as long as the price isn't outrageous.

[Reformed-Redan]

So, who's it going to be? Synthex will be our supplier for this as they have a good track-record, unless someone known anyone else. I'll ask for some quotes.

[SUB-Rx]

I'd like to participate as well.

[ScienceGuy]

Any news on the price, ScienceGuy?

Count me in as long as the price isn't outrageous.

This is Yadayada's party, not mine

For a variety of reasons, including IDRA-21's high probability of inducing adverse effects relating to its influence on the GLUTAMATE PATHWAY I am personally going to be acquiring a very small quantity to test on my lab rat prior to escalating to bulk custom synthesis etc. however, don't let this hold you guys back if you want to go ahead with a group buy in parallel with my doing this

Here's my post from earlier in case anyone missed it:

I just found out I can obtain a small quantity of IDRA-21 from a reputable laboratory in the UK, as they have already synthesized it.

Consequently, I am going to acquire a small amount and try it. I will be sure to post my personal experience with it.

[Reformed-Redan]

Any news on the price, ScienceGuy?

Count me in as long as the price isn't outrageous.

This is Yadayada's party, not mine

For a variety of reasons, including IDRA-21's high probability of inducing adverse effects relating to its influence on the GLUTAMATE PATHWAY I am personally going to be acquiring a very small quantity to test on my lab rat prior to escalating to bulk custom synthesis etc. however, don't let this hold you guys back if you want to go ahead with a group buy in parallel with my doing this

Here's my post from earlier in case anyone missed it:

I just found out I can obtain a small quantity of IDRA-21 from a reputable laboratory in the UK, as they have already synthesized it.

Consequently, I am going to acquire a small amount and try it. I will be sure to post my personal experience with it.

I don't hold any priority here. I'd be glad if you can make this group buy happen, ScienceGuy. Also, the broad term "GLUTAMATE PATHWAY" does no good here. Piracetam, adderall and many other compounds work on the glutamate pathway.

IDRA's action is just more specific and potent. Should I bring out all the papers on it? I've gone over them like five times already.

[joostus]

What are your thoughts on AMPA drugs on healty young people, I'm asking because I haven't had much luck with the other ampakines.
As far as I understand this noot works mainly by antagonizing the desentision of the AMPA-specific glutamate receptors, while this may be needed with elderly or when using benzo's of nightshade would this have results in healthy adults?

[ScienceGuy]

What are your thoughts on AMPA drugs on healty young people, I'm asking because I haven't had much luck with the other ampakines.
As far as I understand this noot works mainly by antagonizing the desentision of the AMPA-specific glutamate receptors, while this may be needed with elderly or when using benzo's of nightshade would this have results in healthy adults?

Anything that induces or exacerbates stimulation of the GLUTAMATE receptors and/or POSITIVE MODULATION of the GLUTAMATE PATHWAY is going to have the potential for causing NEUROTOXICITY, which should be a potential concern for HEALTHY INDIVIDUALS considering taking IDRA-21

Unfortunately, this is typically the problem with AMPAKINES in general, including SUNIFIRAM

Of course, the potential for ADVERSE EFFECTS associated with this particular mechanism of action will be DOSAGE DEPENDENT; and so I strongly urge anyone considering testing out IDRA-21 to start at a VERY LOW DOSE, especially given its reported THREE-DAY DURATION OF EFFECT; and to then adjust dosage very gradually according to how one responds to it

Edited by ScienceGuy, 17 May 2013 - 08:01 AM.

[BioFreak]

ScienceGuy, do you know what the actual cause/mechanism for toxicity from glutamate is?

I agree with the dosage - its possible dosage range is so wide, and duration so long, its much smarter to start low.

[empedocles]

A repost of relevant literature might prove beneficial for creating an informed dosing protocol.

[CalMinera]

If it's not too much money, I'd be very interested in joining in. If that's cool and all. This is my first post.

[Daz_Bike]

Count me in for this.

[Werper]

I'll give it a go, if the opportunity is still there....

[Reformed-Redan]

http://www.pnas.org/...94/13/7053.long

In cerebellar granule neurons of neonatal rats micromolar concentrations of 7-chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine S,S-dioxide (IDRA-21) and cyclothiazide, two negative modulators of the spontaneous agonist-dependent rapid desensitization of α-amino-3-hydroxy-5-methylisoxazolepropionic acid (AMPA)-gated ion channels, facilitate AMPA receptor function by increasing the content of free cytosolic Ca²⁺ as measured by single-cell fura-2 acetoxymethyl ester (Fura-2) Ca²⁺-dependent fluorescence and intracellular Na⁺ measured with the sodium-binding bezofuran isophthalate acetoxymethyl ester fluorescence indicator. IDRA-21 increases intracellular Na⁺ transient with a threshold (5 μM) that is ≈10 times higher and has an intrinsic activity significantly lower than that of cyclothiazide. By virtue of its low intrinsic activity, IDRA-21 elicits a free cytosolic Ca²⁺ transient increase that is shorter lasting than that elicited by cyclothiazide even when the drug is left in contact with cultured granule cells for several minutes. Additionally, while dose dependently, 5–25 μM cyclothiazide in the presence of AMPA is highly neurotoxic, IDRA-21 (up to 100 μM) is devoid of neurotoxicity. The neurotoxicity elicited by cyclothiazide persists in the presence of dizocilpine (an antagonist of N-methyl-D-aspartate-selective glutamate receptors) but is blocked by 2,3-dihydroxy-6-nitrosulfamoylbenzo[f]quinoxaline (a competitive AMPA receptor antagonist) and the 1-(aminophenyl)-4-methyl-7,8-methylendioxy-5H-2,3-benzodiazepine (GYKI 52466; a noncompetitive AMPA receptor antagonist). Since the doses of IDRA-21 that enhance cognitive processes in rats and monkeys are several orders of magnitude lower than those required to elicit marginal neurotoxicity in cultured neurons, it can be surmised that IDRA-21 is a potent cognition-enhancing drug virtually devoid of neurotoxic liability because it acts as a partial negative allosteric modulator of AMPA receptor desensitization.

[Neosback]

Count me in, seems like something worth trying.

[OpaqueMind]

If there's room, I'm in too.

[Web]

I'm in if there's room and the price is reasonable.

Edited by Web, 17 May 2013 - 08:01 PM.

[Dashwolf]

As long as the price isn't ridiculous, I'm interested.

[Amorphous]

Indeed very interesting. I'd like to be in too.

[lukem5]

I am a nootropic virgin and I would like to try it in a very small amount as a first nootropic, it sounds too good to be true

[sunshinefrost]

Alright then, i'm in

[Picard]

In. Please keep us informed of details.

Do we also have a rough estimate/expectation of the timeframe?

Edited by Picard, 18 May 2013 - 04:58 PM.

[Reformed-Redan]

I will keep you updated when I get more info.