11 replies to this topic

[Reformed-Redan]

Wow, just stepping back for a second a lot of things have been happening on the forum recently. Got one group buy dine for uridine. PRL-8-53 is in the process of synthesis. NSI-189 will soon be done. Things are moving really fast. Too fast for my wallet for sure.

I'm wondering if we can have a proposal for a couple of interesting compounds that we can organize in a more timely manner. Like every couple of months I can put aside a certain amount for a promising compound. I don't want these group buys to die away after a month or so. We could just organize a group buy when convenient for everyone. I for one don't have unlimited funds; but, there are an unlimited of interesting compounds out there- some of which we will be seeing soon.

So, what are some interesting compounds to look at for any upcoming group buy??

I've got:
IDRA-21 (strong nootropic effects, unseen of)
and
BPAP (The evolution of selegiline, active at 100micrograms)

also of interest are gabaa alpha 5 inverse agonists with strong nootropic effects at low doses and long half lives.
alpha 7 nicotinic positive allosteric modulators are also interesting at normalizing brain function for many neurological disorders and with nootropic effects.

List whatever is of interest.

One last things. Voicing concerns proposed by lenses in another thread. It best not combine too many novel nootropics at once to avoid any interactions and possible damage.

Let's see what we can find here, then maybe vote on.

I'm getting a little high on life. Hehe

[daouda]

Well these are probably too experimental at the moment, but obviously : dihexa, and isoxazole-9

[chung_pao]

I'm probably in on a group buy if you find any of the above.

I'm also interested in this compound http://en.wikipedia....wiki/SKF-38,393.
It's supposed to activate LTP by stimulating D1 and D5 receptors, which activate adenylyl cyclase, leading to cAMP formation.
What's unique about it is that it doesn't affect D2-4 receptors, which inhibit adenylyl cyclase, and thus impair LTP.
There are a few studies in which this compound show a lot of promise.

[kevinseven11]

Longecity is rapidly becoming a very effective nootropic community. There are more to add!

[Patrick Sylvester]

just cross-posting for consolidation sake

Indeloxazine - "cerebral activator" used in Japan.
Teniloxazine - investigated as a neuroprotective and nootropic agent but ultimately developed and approved as an antidepressant in Japan.
Minocycline - antibiotic that has demonstrated neurorestorative as well as neuroprotective properties.
P7C3A20 - "Neurogenesis Enhancer"
Pirisudanol - used in Europe for mild cognitive impairment, fatigue and depression.
Taltirelin - thyrotropin-releasing hormone (TRH) analog with purported nootropic, neuroprotective and analgesic effects.
Linopirdine - purported cognition-enhancing drug.
Leteprinim - hypoxanthine derivative with neuroprotective and nootropic effects.
Bifemelane - used for senile dementia in Japan.
Ispronicline - neural nicotinic acetylcholine receptors partial agonist with antidepressant, nootropic and neuroprotective effects.
S-17092 - selective Prolyl endopeptidase inhibitor producing nootropic effects.
Semax - Russian drug with purported nootropic, neuroprotective and neurorestorative properties.

→ source (external link)

C16 - Protein kinase RNA-activated (PKR) inhibitor

The double-stranded RNA-activated protein kinase (PKR) was originally identified as a sensor of virus infection, but its function in the brain remains unknown. Here, we report that the lack of PKR enhances learning and memory in several behavioral tasks while increasing network excitability.

get a perfect memory but become vulnerable to viral infections

→ source (external link)

... i still want to know more about Intellix even if its just lore.

[Reformed-Redan]

Indeloxazine looks pretty interesting. Anyone from Japan care to send some?

[Reformed-Redan]

Org 26576 looks pretty neat.

[chung_pao]

I'm particularly interested in allosteric modulators. These are drugs, like the ampakines, which don't directly agonise/antagonise receptors, but sensitize/desensitize them.
Allosteric modulators of dopamine, nACh, AMPA and NMDA receptors are of special interest

My beef with direct agonists/antagonists is that I quickly grow tolerant to their effect, irregardless of what receptor it targets.
Allosteric modulators on the other hand are attached to receptors at the site reserved for hormones, among other things. This is what makes ampakines so consistent in their effects. However, this is just my hypothesis, and I'm throwing it out there in case anyone is on the same train of though.

[Patrick Sylvester]

Effects of several cerebroprotective drugs on NMDA channel function: evaluation using Xenopus oocytes and [3H]MK-801 binding.
Kaneko S, Sugimura M, Inoue T, Satoh M.

Department of Pharmacology, Faculty of Pharmaceutical Sciences, Kyoto University, Japan.

The effects of several cerebroprotective and nootropic drugs on the function of excitatory amino acid (EAA) receptor subtypes expressed in Xenopus oocytes after injection of rodent brain poly(A)+ mRNA were investigated. The oocyte response to N-methyl-D-aspartate (NMDA) in the presence of glycine (Gly) was inhibited dose-dependently by bifemelane, indeloxazine, vinpocetine and vincamine while no effect was observed by idebenone, Ca hopantenate, aniracetam or piracetam. Bifemelane, indeloxazine and vinpocetine suppressed the maximum response of NMDA and Gly without affecting their EC50 values. Unlike Mg2+, they did not affect the current-voltage relationship of the NMDA response be low 0mV. On the non-NMDA-type responses o f the injected oocytes to kainate (KA), alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) and quisqualate (QA), no significant effects were observed by these drugs at 100 microM. On the binding of [3H](+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imi ne ( MK-801 ) to brain membranes, the estimated IC50 values were 88 microM for bifemelane, 102 microM for indeloxazine, and 115 microM for vinpocetine. The dissociation rate of [3H] MK-801 was significantly slowed by Zn 2+ and vinpocetine, but not affected by bifemelane or indeloxazine. The Kd value for [3H]MK-801 binding was increased by bifemelane and indeloxazine while Bmax was unchanged. These results suggest that the inhibition of NMDA channels by vinpocetine shows a similarity to the action of Zn2+ which closes the gate of the NMDA channel. In contrast, bifemelane and indeloxazine may affect the phencyclidine (PCP)-site in the open channels and inhibit NMDA function.

PMID: 1652446

stumbled across a Indeloxazine mention in a cerebroprotective study when debating whether to use vinpo.

Edited by Patrick Sylvester, 04 June 2013 - 04:40 AM.

[Reformed-Redan]

So, here is the current list that is being refined depending on how organization goes.
So far,
1. IDRA-21 (might depend on the results of ScienceGuy)
2. Pitolisant.
3. ISRIB potent alternative to C16, potent memory enhancer.
I think I have a trustworthy and honest supplier that can have this all done for us, if there is interest.

[eon]

I believe it was withdrawn in 1998 due to ineffectiveness but it's still sold as research chemical as with anything else no longer sold. Interesting mentioned of BPAP (selegiline part 2? I thought that would be rasagiline?)). I haven't heard much about BPAP but I am looking into selegiline.

 

Amfonelic acid is a compound of interest to me that is very expensive.

 

Indeloxazine looks pretty interesting. Anyone from Japan care to send some?

 

Edited by eon, 21 December 2014 - 01:37 PM.

[Ark]

Indeloxazine count me in