Buy Ampakines [EXCLUSIVE]

Ampakines or AMPAkines are a subgroup of AMPA receptor positive allosteric modulators with a benzamide or closely related chemical structure.[1][2] They are also known as "CX compounds".[1] Ampakines take their name from the AMPA receptor (AMPAR), a type of ionotropic glutamate receptor with which the ampakines interact and act as positive allosteric modulators (PAMs) of.[1] Although all ampakines are AMPAR PAMs, not all AMPAR PAMs are ampakines.

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More recently developed ampakine compounds are much more potent and selective for the AMPA receptor target, and while none of the newer selective ampakine compounds have yet come onto the market, various ampakines are in clinical trials.[1]

A wide range of ampakines have been developed by RespireRx, which hold patents covering most medical uses of this class of drugs. The best known compounds that have come out of the RespireRx drug development program are CX-516 (Ampalex), CX-546, CX-614, CX-691 (farampator), and CX-717. ORG-26576 was developed by RespireRx but then licensed to Organon for development.

Ampakines are drugs structurally derived from aniracetam that potentiate currents mediated by AMPA type glutamate receptors. These drugs slow deactivation and attenuate desensitization of AMPA receptor currents, increase synaptic responses and enhance long-term potentiation. This review focuses mainly on recent physiological studies and on evidence for two distinct subfamilies. Type I compounds like CX546 are very effective in prolonging synaptic responses while type II compounds like CX516 mainly increase response amplitude. Type I and II drugs do not compete in binding assays and thus presumably act through separate sites. Their differences are likely to have consequences also for synaptic plasticity and behavior. Thus, while all ampakines facilitated long-term potentiation, only CX546 enhanced long-term depression. Further discussed are studies showing that ampakine effects vary substantially between neurons, with increases in EPSCs being larger in CA1 pyramidal cells than in thalamus and in hippocampal interneurons. In behavioral tests, ampakines facilitate learning in many paradigms including odor discrimination, spatial mazes, and conditioning, and they improved short-term memory in a non-matching-to-sample task. Positive results were also obtained in various psychological tests with human subjects. The drugs were effective in correcting behaviors in various animal models of schizophrenia and depression. Lastly, evidence is discussed that ampakines have few adverse effects at therapeutically relevant concentrations and that they protect neurons against neurotoxic insults, in part by mobilizing growth factors like BDNF. Type II drugs like CX516 in particular appear to be inherently safe since their ability to prolong responses is kinetically limited.

One preliminary study on rats shows ampakines enhanced their ability to focus and pay attention. On the other hand, it did show a decrease in object recognition memory.4Zheng Y, et al. Effects of the putative cognitive-enhancing ampakine, CX717, on attention and object recognition memory Curr Alzheimer Res. 2011

There is evidence that ampakines are effective in enhancing synaptic responses, most likely by slowing deactivation. This could be the source of its cognitive enhancement.6Arai AC, et al. Effects of the potent ampakine CX614 on hippocampal and recombinant AMPA receptors: interactions with cyclothiazide and GYKI 52466 Mol Pharmacol. 2000

It seems that ampakines can selectively improve at least some aspects of memory.7Ingvar M, et al. Enhancement by an ampakine of memory encoding in humans Exp Neurol. 19978Lynch G, et al. Evidence that a positive modulator of AMPA-type glutamate receptors improves delayed recall in aged humans Exp Neurol. 1997

Researchers concluded that ampakines could cross the blood-brain barrier and facilitate glutamatergic transmission in a way that enhances the encoding of memory across tasks.13U Staubli, G Rogers, G Lynch. Facilitation of glutamate receptors enhances memory Proc Natl Acad Sci U S A. 1994

The researchers found that the subjects who took ampakines scored twice as well on memory tests, closer to the memory capacity of young subjects.14Lynch G, et al. Evidence that a positive modulator of AMPA-type glutamate receptors improves delayed recall in aged humans Exp Neurol. 1997

Ampakines enhanced the action of typical and atypical antipsychotics like haloperidol and clozapine synergistically. This result suggests that ampakines may be useful as an adjunct therapy with traditional drugs.17Johnson SA, et al. Synergistic interactions between ampakines and antipsychotic drugs J Pharmacol Exp Ther. 1999

The preliminary findings indicate that biarylpropylsulfonamide-type ampakines, exemplified by LY392098, may represent a novel class of antidepressants.20Li X, et al. Antidepressant-like actions of an AMPA receptor potentiator (LY392098) Neuropharmacology. 2001

The authors of this study noted that the rats that took the ampakines displayed less depressive behavior, even more so than the rats on traditional antidepressants.21Knapp RJ, et al. Antidepressant activity of memory-enhancing drugs in the reduction of submissive behavior model Eur J Pharmacol. 2002

Results were evident within 15 minutes of behavioral testing, indicating that ampakines may be particularly fast-acting neuroprotectives.22U.S Hess, et al. Ampakines reduce methamphetamine-driven rotation and activate neocortex in a regionally selective fashion Neuroscience. 2003

Not yet widely used are ampakines, an emerging class of drugs currently studied by the United States military with the aim of increasing alertness in soldiers. Ampakines bind to so-called AMPA receptor molecules in the nervous system and boost the response of nerve cells and strengthening connections between them. Known to improve memory and cognition in rats and healthy human volunteers, ampakines are often considered to be relatively safe potential smart drugs. But they are not without dangers for young people: uncontrolled use of ampakines might over-excite the nervous system, damaging or killing nerve cells, caution the authors.

But research indicates that modafinil could have similar long-term undesired effects as methylphenidate on the developing brain, the study authors said. Not yet widely used are ampakines, an emerging class of drugs currently studied by the US military with the aim of increasing alertness in soldiers.

Ampakines bind to so-called AMPA receptor molecules in the nervous system and boost the response of nerve cells and strengthen connections between them. Known to improve memory and cognition in rats and healthy humans volunteers, ampakines are often considered to be relatively safe potential smart drugs. 041b061a72