314728-85-3 Usage
Description
Sunifiram (DM-235) is a synthetic derivative of piracetam, although due to breaking the pyrrolidone backbone it is no longer in the racetam class of drugs (yet by being derived from them, it is still commonly associated with this class).Sunifiram has mechanisms similar to nefiracetam in the hippocampus, and similar to that drug sunifiram shows anti-amnesiac properties and is potentially a cognitive enhancer. Its anti-amnesiac activity is several orders of magnitude greater than piracetam on a per weight basis, and preliminary evidence suggest it has a similarly low toxicity profile.
Uses
Sunifiram is a potent nootropic agent.
Side effects
While initial research suggests that sunifiram is virtually non-toxic and doesn’t produce any notable side effects, it’s important to note how little research has been conducted on this compound. For this reason, it’s incredibly important that you begin with a low dosage before ramping up to a higher one, and pay close attention to any noted side effects you experience.Based on anecdotal evidence, some sunifiram users have experienced side effects such as:HeadacheHot flashesDifficulty sleepingManic feelingsThese side effects seem only to be mentioned with dosages outside of the 5-10mg range, with higher doses producing more pronounced side effects. If you find that you’re experiencing side effects as you up your dosage, ramp down your dosage to a level where no side effects are present.
Mode of action
Sunifiram enhances NMDA-dependent signaling by increasing PKCα phosphorylation, at a dosage range of 10-100nM. This mechanism of action is dependent on the availability of the glycine binding site and Sunifiram has been shown to act as an antagonist to glycine at a concentration of 300μM.Furthermore, the increased activity of AMPA receptor activation has been associated with increased CAMKII and PKCα phosphorylation. Although studies have confirmed that intracellular proteins like CAMKII and PKCα are activated after Sunifiram administration, other proteins like CaMKIV and ERK remain unaffected.A brief summary of the mechanism of action, as it is currently understood, is that Sunifiram acts on the NMDA receptor’s glycine binding site, which results in increased signaling and activation of CAMKII and PKCα proteins and the subsequent positive regulation of AMPA receptors.Furthermore, animal studies have indicated that a dosage of 0.01mg/kg increases acetylcholine release by up to 200% within one hour of injection, in rat prefrontal cortex. This effect is not seen at a higher dosage of 1mg/kg.
Check Digit Verification of cas no
The CAS Registry Mumber 314728-85-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,1,4,7,2 and 8 respectively; the second part has 2 digits, 8 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 314728-85:
(8*3)+(7*1)+(6*4)+(5*7)+(4*2)+(3*8)+(2*8)+(1*5)=143
143 % 10 = 3
So 314728-85-3 is a valid CAS Registry Number.
314728-85-3Relevant articles and documents
Novel Sunifiram-carbamate hybrids as potential dual acetylcholinesterase inhibitor and NMDAR co-agonist: simulation-guided analogue design and pharmacological screening
Abdel-Aal, Eatedal H.,Abdel-Samii, Zakaria K.,Abo-Dya, Nader E.,Agha, Khalid A.,Agoni, Clement,Ibrahim, Tarek S.,Issahaku, Abdul Rashid,Soliman, Mahmoud E. S.
, p. 1241 - 1256 (2022/05/04)
An efficient method for synthesising NMDAR co-agonist Sunifiram (DM235), in addition to Sunifram-carbamate and anthranilamide hybrids, has been developed in high yields via protecting group-free stepwise unsymmetric diacylation of piperazine using N-acylb
Molecular simplification of 1,4-diazabicyclo[4.3.0]nonan-9-ones gives piperazine derivatives that maintain high nootropic activity
Manetti,Ghelardini,Bartolini,Dei,Galeotti,Gualtieri,Romanelli,Teodori
, p. 4499 - 4507 (2007/10/03)
Several 4-substituted 1-acylpiperazines, obtained by molecular simplification of 4-substituted 1,4-diazabicyclo[4.3.0]nonan-9-ones, have been synthesized and tested in vivo on the mouse passive avoidance test, to evaluate their nootropic activity. The results show that, apparently, an N-acylpiperazine group can mimic the 2-pyrrolidinone ring of 1,4-diazabicyclo[4.3.0]nonan-9-one, as the compounds of the new series maintain high nootropic activity. Moreover molecular simplification produces more clear-cut structure-activity relationships with respect to the parent series. The mechanism of action also appears to be similar in the two series. In fact, although the molecular mechanism remains to be elucidated, the most potent compound of each class (DM232 and 13, DM235) is able to increase acetylcholine release in rat brain. Piperazine derivatives represent a new class of nootropic drugs with an in vivo pharmacological profile very similar to that of piracetam, showing much higher potency with respect to the reference compound. Among the compounds studied, 13 (DM235) shows outstanding potency, being active at a dose of 0.001 mg kg-1 sc.