47 replies to this topic

[jackinbox]

Nice post aidanpryde! Very few people are willing to make the effort you made to get the stuff. I know little about chemistry but I guess finding how to synthesis a molecule isn't a piece of cake. You are definitely connected with competent people.

[jackinbox]

1Kg/4000$... anyone wants to be part of a buyer group? I'm pretty sure it's not too hard to find a chinese custom manufacturer willing to make some. Let's say that we get it at this price: If we get 10 person interested, it would cost only 400$ each for 100 grams. I did invest much more than that in nootropics and medications so far.

http://www.asischem.com/customsyn.asp

[stargazer]

1Kg/4000$... anyone wants to be part of a buyer group? I'm pretty sure it's not too hard to find a chinese custom manufacturer willing to make some. Let's say that we get it at this price: If we get 10 person interested, it would cost only 400$ each for 100 grams. I did invest much more than that in nootropics and medications so far.

http://www.asischem.com/customsyn.asp

I'm game, PM me with further details.

[mtriogd]

anyone care to reference the research where Idebenone and Aniracetam are noted to have AMPA effects (agonism) of considerasble enough nature that one can warrant in any way to call them Ampakines as some here have

(obviously this means they would express these parameteres in a solid manner at reasonably normal dosing schemes and thus have ED50 or Ki values to assert such)

TIA

[spacey]

1Kg/4000$... anyone wants to be part of a buyer group? I'm pretty sure it's not too hard to find a chinese custom manufacturer willing to make some. Let's say that we get it at this price: If we get 10 person interested, it would cost only 400$ each for 100 grams. I did invest much more than that in nootropics and medications so far.

http://www.asischem.com/customsyn.asp

I'm game, PM me with further details.

Yeah I'd be willing to spend some money in a buying group as well.

Here is a company that will synthesize not only in bulk
http://www.exchemist...-synthesis.html

Edited by spacey, 05 November 2007 - 05:31 PM.

[mtriogd]

True, as it is an enhancer and thus not simply an agonist which may not be all that good a thing

similar to BPAP/PPAP...talk about perhaps the ultimate stack for wakefulness/motivation/cgnition/focus/well-being!

again i would like to see the studies for IDEB and Aniracteam as i am going on the assumption that they do not have any real effect at any normally used (even high-end) dosing on positive AMPA modulation...that is my speculation offhand, but if there is a study or two to prove me wrong please someone ref them

[jackinbox]

There is interest in the buying group idea! So far, we are 3 interested (one private). If it was not the research part, it wouldn't be too hard to setup a buying group. Convincing people to invest in the development of a compound is harder than than convincing them to buy the actual product.

If we could get someone used to do business with suppliers involved, it would help a lot. Peter? Are you there?

[shamus]

FYI: Bulk Nutrition sells @ ~$80 for 275 grams.

[mtriogd]

^ we are talking about CX516, not Aniracetam which i assume you are referring to

[jackinbox]

Yeah, Bulk Nutrition carry a lot of stuff but but I don't expect them to sell CX516 anytime soon...

[mtriogd]

We are a gruop of italian cellular neurophysiologists involved since years in research on glutamatergic transmission and plasticity. We would be interested in testing the effect of Ampakines in cerebellar preparation in vitro but till now we haven't found a commercial site for purchasing Ampakines.
Could you please help us?
Please contact me at andreflieshigh@tiscali.it

Dipartimento di Scienze Fisologiche Farmacologiche e Molecolari
Univerity of Pavia
www.unipv.it/dsffcm/pagine/labs/dangelo/dangelo.html

If there is ample demand we can supply CX516 to anyone who desires to procure this for research in vitro or in vivo in animal models. We also have the ability to manufacture other Ampakines at best pricings thanks to our synthesis expertise.

We are aware there are many honorable scientists and hobbyist researchers and as long as you assert you will be using for non-human purposes we can make available to parties as below:

50g $325
100g $495
200g $895
500g $1995

We are a professional, repected, well-known research supply cooperative who supplies to both institutions and hobbyists.
Lead time is 4-6 weeks from the point we can assess demand warrants as we would hope to break even and in the interest of science we feel this is a good pursuit.
We also have stocked MitoQ, Pramiracetam, Nefiracetam, Memantine, amongst other items, all of highest quality, just to note.
I assume this is not spam as to the interest expressed in this thread desiring such and that it is not available elsewhere it appears so we hope this is to some degree noted as a community benefit for researchers looking to forward knowledge in this area. As such though I will not post our website here, but note we have never had one unsatisfied researcher and those who inquire will perhaps be aware of our site and stellar reputation which goes back many, many years as we will remit the site to serious inquiries only.
For greater details do not hesitate to contact.
Brgds!

[blazewind]

I found some interesting CX516 studies:


Title: Can ampakines reverse cognitive deficits in healthy adults? Efficacy and safety of a single dose of the Ampakine ® compound, CX516, on measures of sleepiness and performance in sleep-deprived healthy young men
Author: Mishory, A
Add.Author / Editor: Grenesco, E
Anderson, B
Nahas, Z
Horner, MD
Molanr, CE
Johnson, S
Deadwyler, S
Rogers, G
Carney, JM
George, MS
Citation: BIOLOGICAL PSYCHIATRY 55: 189S-189S 677 Suppl. 8 APR 15 2004
Year: 2004
ISSN: 0006-3223
Type: Meeting Abstract
Language: English




677. Can Ampakines Reverse Cognitive Deficits in
Healthy Adults? Efficacy and Safety of a Single
Dose of the Ampakine® Compound, CX516, on
Measures of Sleepiness and Performance in Sleep-
Deprived Healthy Young Men
Alexander Mishory1, Emily Grenesco1, Berry Anderson1,
Ziad Nahas1, Michael D. Horner1, Christine E. Molanr1,
Steven Johnson2, Sam Deadwyler3, Gary Rogers2, John
M. Carney4, Mark S. George1
1Brain Stimulation Laboratory, Institute of Psychiatry, Medical
University of South Carolina, Charleston, SC, 2Cortex
Pharmaceuticals, Cortex Pharmaceuticals, Irvine, CA, 3Pharmacology
Department, Wake Forest University, Winston Salem, NC, 4Defense
Science Office, DARPA, Arlington, VA
Background: Sleep deprivation performance deficits (SDPD) represent a
model of cognitive deficits. Ampakines are a novel class of compounds that
impact cognitive functioning. Research suggests that Ampakine compound,
CX516, as well as a more potent compound, CX717, temporarily reverses
SDPD in non human primates (Hampson RE, 2003). CX516 is currently being
tested in clinical trials.
Methods: We performed 2 serial studies to determine whether CX516 has
effects on human SDPD. In study 1, we studied 11 healthy young men (mean
age 29.8 yrs, 6 SD). Subjects underwent 4 separate 30-hour sleep deprivation
visits, separated by a week of recovery sleep, receiving an oral dose of either
CX516 (900, 1200, 1500mg) or placebo following SD. In study 2, we studied 11
young men receiving either 2100 mg of CX516 or placebo. In both double
blind, randomized, crossover designs, we assessed working memory, motor
skills, error rates and reaction times using the Sternberg Working Memory Task
and Multi-Attribute Task Battery both at baseline and following sleep
deprivation. Quantitative EEG was performed on the last day.
Results: In both studies, CX516 was well-tolerated with no significant side
effects. In the initial study, CX516 showed a dose-dependent improvement in
MATB tracking task accuracy and a reduction in Delta wave activity. At the
higher dose, CX516 resulted in improvement of motor skills and working
memory performance.
Conclusions: CX516 is safe and well-tolerated in this SD model of cognitive
deficits. Further studies with higher doses, as well as with more potent
Ampakine compounds (CX717), appear warranted.

============================================================

Title: Glutamatergic therapy for Alzheimer's disease: Safety, tolerability and preliminary efficacy of CX516
Author: Morris, MJ
Add.Author / Editor: Chase, TN
Johnson, SA
Citation: NEUROBIOLOGY OF AGING 23 (1): 2040 Suppl. 1 JUL-AUG 2002
Year: 2002
ISSN: 0197-4580
Type: Meeting Abstract
Language: English

GLUTAMATERGIC THERAPY FOR ALZHEIMER’S
DISEASE: SAFETY, TOLERABILITY AND
PRELIMINARY EFFICACY OF CX516
Michael J. Morris∗, Thomas N. Chase, National Institute of Health,
Bethesda, MD, USA; Steven A. Johnson, Cortex Pharmaceuticals Inc,
Irvine, CA, USA. Contact e-mail: morrism@ninds.nih.gov
Background: The glutamatergic system is fundamentally involved in learning,
memory and cognition, and is adversely affected in Alzheimer’s disease.
A novel approach to augment CNS glutamatergic transmission is by facilitation
facilitation
of AMPA-type glutamate receptors. Preclinical studies have shown
that the positive AMPA receptor modulator CX516 facilitates memory formation
and retention in young rodents, and improves impaired cognitive
performance of aged rodents to the level of the young animals. We hypothesized
that CX516 might improve memory and cognition in AD patients.
Methods: A randomized, double-blind, placebo-controlled, parallel-group
design was employed. All patients received 1–2 weeks of placebo treatment,
followed by 4 weeks of CX516 or matching placebo treatment, followed
by a final 2–3 week placebo washout period. Dose range (600 mg
bid to 2700 mg tid) was escalated on a weekly basis. Subjects satisfied
NINDS-ADRDA criteria for probable AD and had an MMSE score between
12–26. Primary outcome measures included the ADAS–cog and the
CIBIC+. Results: Fourteen patients (active = 8; placebo = 6) completed
the study. CX516 was well tolerated. There were no drop-outs nor serious
adverse events. Mild headache and nausea were the most common adverse
events. Mean ADAS–cog scores were 2.7 and 3.7 points lower after 4 weeks
of CX516 and at follow-up, respectively, in the CX516 group, compared
with a 0.4 and 1.2 points lower, respectively, for placebo. Within-subject
analysis of the CX516 group by 2-tailed Wilcoxon-paired exact test gave
P = 0.06 after 4 weeks active treatment, and P = 0.03 after 4 weeks active
treatment and 2 weeks placebo washout. CIBIC+ scores were 3.6 and 3.1
for CX516 versus 4.0 and 4.2 for placebo at Week 4 (NS) and follow-up
(P = 0.06), respectively. Conclusions: In this pilot study, CX516 produced
suggestive beneficial effects which appear similar to currently available medications
for AD. A larger and longer study will be conducted to assess more
definitely the safety and efficacy of this novel approach to anti-dementia
therapy.

[mtriogd]

Found this interesting in relating that there appears to not be issues with tolerance and attneuation with CX516

Arai AC, Xia YF, Rogers G, Lynch G, Kessler M.
Benzamide-type AMPA receptor modulators form two subfamilies with distinct modes of action.
J Pharmacol Exp Ther 2002 Dec;303(3):1075-85
"CX516 (BDP-12) and CX546, two first-generation benzamide-type AMPA receptor modulators, were compared with regard to their influence on AMPA receptor-mediated currents, autaptic responses in cultured hippocampal neurons, hippocampal excitatory postsynaptic currents, synaptic field potentials, and agonist binding. The two drugs exhibited comparable potencies in most tests but differed in their efficacy and in their relative impact on various response parameters. CX546 greatly prolonged the duration of synaptic responses, and it slowed 10-fold the deactivation of excised-patch currents following 1-ms pulses of glutamate. The effects of CX516 on those measures were, by comparison, small; however, the drug was equally or more efficacious than CX546 in increasing the amplitude of synaptic responses. This double dissociation suggests that amplitude and duration of synaptic responses are governed by different aspects of receptor kinetics, which are differentially modified by the two drugs. These effects can be reproduced in receptor simulations if one assumes that CX516 preferentially accelerates channel opening while CX546 slows channel closing. In binding tests, CX546 caused an approximately 2-fold increase in the affinity for radiolabeled agonists, whereas CX516 was ineffective. More importantly, even millimolar concentrations of CX516 did not influence the dose-response relation for CX546, suggesting the possibility that they bind to different sites. Taken together, the evidence suggests that benzamide modulators from the Ampakine family form two subgroups with different modes and sites of action. Of these, CX516-type drugs may have the greater therapeutic utility because of their limited efficacy in prolonging synaptic responses and in attenuating receptor desensitization." [Abstract]

[Buonarroti]

I'm wondering if some people involved in the ampakine's development use them themselves. It must be really tempting. It's known that the creator of Deprenyl use it himself but I don't know if he began to use it before or after it has been approved.

There was a husband and wife team, Durk Pearson and Sandy Shaw, who were often guests on the old Merv Griffin Show. They are considered pioneers in the life extention movement. They would go on and describe their ideas and how they personally used their experimental formulas. I Googled up this excerpt from a book from 1999 where the author quoted and observed how they still routinely ingested a list of things mixed in drinks but they did not exercise and ate pretty close to whatever and all that they wanted to eat. He said they looked their ages but showed all signs that they were confident science would have the issue of aging figured out and some form of remedy in time for them to live as long as 2000 years if they avoided non-age related events like accidents. These people seem to have had enough confidence and optimism over the research they were exposed to and have been interested patrons of their own products.

[yatri]

Hi,
Its really nice to read actual experience of the effects of an Ampakine. I have been searching them on the internet wildly. I am aware that Ampalex can be bought from Sigma Aldrich and a Chinese supplier but as everybody knows that the prices are unimaginable. Please reply if I can buy a small quantity from you.

[Rags847]

Hi,
Its really nice to read actual experience of the effects of an Ampakine. I have been searching them on the internet wildly. I am aware that Ampalex can be bought from Sigma Aldrich and a Chinese supplier but as everybody knows that the prices are unimaginable. Please reply if I can buy a small quantity from you.

I think it's a little to early to start taking Ampakines. You should let them work out which version of the Ampakine drug is most effective and safest first, before taking them.

Here is the latest news on Ampikines:
http://www.imminst.o...ews-t20192.html
"The FDA's rejection was based on results of animal toxicology studies that have long plagued the CX717 program. Toxicology concerns resulted in a clinical hold on the program last year, which was lifted by the FDA's Division of Neurology Products so Cortex could begin a trial in Alzheimer's disease. (See BioWorld Today, April 4, 2006, and Oct. 30, 2006.)

But the Division of Psychiatry Products, which oversees ADHD trials, proved harder to convince. Cortex submitted data indicating the animal toxicity issues were due to post-mortem tissue processing and showing that CX717 was well-tolerated in a previous Phase IIa ADHD trial, but the agency refused to approve the Phase IIb plan."

I'm going to stick with Piracetam and it's long track record of effectiveness and safety.

Edited by Rags847, 09 February 2008 - 01:54 PM.

[kassem23]

Any news on the ampakines? Is it possible to procure them from some place?