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Racetam

Racetam

Overview




Racetams are a class of nootropic
Nootropic
Nootropics, also referred to as smart drugs, memory enhancers, and cognitive enhancers, are drugs, supplements, nutraceuticals, and functional foods that are purported to improve mental functions such as cognition, memory, intelligence, motivation, attention, and concentration. The word nootropic...

 drugs
Psychoactive drug
A psychoactive drug, psychopharmaceutical or psychotropic substance is a chemical substance that acts primarily upon the central nervous system where it alters brain function, resulting in changes in perception, mood, consciousness and behavior...

 that share a pyrrolidone
2-Pyrrolidone
2-Pyrrolidone is an organic compound consisting of a five-membered lactam. It is a colorless liquid which is used in industrial settings as a high-boiling non-corrosive polar solvent for a wide variety of applications...

 nucleus.

There is no generally accepted mechanism for racetams. They generally show no affinity for the most important receptors, although modulation of most important central neurotransmitter
Neurotransmitter
Neurotransmitters are endogenous chemicals which relay, amplify, and modulate signals between a neuron and another cell. Neurotransmitters are packaged into synaptic vesicles that cluster beneath the membrane on the presynaptic side of a synapse, and are released into the synaptic cleft, where they...

s, including acetylcholine and glutamate have been reported. Although aniracetam and nebracetam show affinity for muscarinic receptors, only nefiracetam
Nefiracetam
Nefiracetam is a nootropic drug of the racetam family.Nefiracetam’s cytoprotective actions are mediated by enhancement of GABAergic, Cholinergic, and Monoaminergic neuronal systems that give antiamnesia effects to the Alzheimer's type and cerebrovascular type of dementia....

 shows it at the nanomolar range.
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Encyclopedia




Racetams are a class of nootropic
Nootropic
Nootropics, also referred to as smart drugs, memory enhancers, and cognitive enhancers, are drugs, supplements, nutraceuticals, and functional foods that are purported to improve mental functions such as cognition, memory, intelligence, motivation, attention, and concentration. The word nootropic...

 drugs
Psychoactive drug
A psychoactive drug, psychopharmaceutical or psychotropic substance is a chemical substance that acts primarily upon the central nervous system where it alters brain function, resulting in changes in perception, mood, consciousness and behavior...

 that share a pyrrolidone
2-Pyrrolidone
2-Pyrrolidone is an organic compound consisting of a five-membered lactam. It is a colorless liquid which is used in industrial settings as a high-boiling non-corrosive polar solvent for a wide variety of applications...

 nucleus.

Mechanism


There is no generally accepted mechanism for racetams. They generally show no affinity for the most important receptors, although modulation of most important central neurotransmitter
Neurotransmitter
Neurotransmitters are endogenous chemicals which relay, amplify, and modulate signals between a neuron and another cell. Neurotransmitters are packaged into synaptic vesicles that cluster beneath the membrane on the presynaptic side of a synapse, and are released into the synaptic cleft, where they...

s, including acetylcholine and glutamate have been reported. Although aniracetam and nebracetam show affinity for muscarinic receptors, only nefiracetam
Nefiracetam
Nefiracetam is a nootropic drug of the racetam family.Nefiracetam’s cytoprotective actions are mediated by enhancement of GABAergic, Cholinergic, and Monoaminergic neuronal systems that give antiamnesia effects to the Alzheimer's type and cerebrovascular type of dementia....

 shows it at the nanomolar range. Modulation of protein synthesis and protein Kinase C could be a mechanism. Modification of membrane-located
mechanisms of central signal transduction is another hypothesis.

Racetams are understood to work by activating glutamate receptor
Glutamate receptor
Glutamate receptors are transmembrane receptors located on the membranes of neuronal cells. These receptors bind the neurotransmitter glutamate.-Function:...

s that are colocalized with cholinergic receptors, thus increasing the firing of the latter. The racetams consequently increase memory capacity by nearly the same method as the acetylcholinesterase inhibitor
Acetylcholinesterase inhibitor
An acetylcholinesterase inhibitor or anti-cholinesterase is a chemical that inhibits the cholinesterase enzyme from breaking down acetylcholine, increasing both the level and duration of action of the neurotransmitter acetylcholine.- Uses :Acetylcholinesterase inhibitors:* Occur naturally as...

s.

Examples

  • Piracetam
    Piracetam
    Piracetam is a nootropic drug. It appears to enhance cognition and memory, slow brain aging, increase blood flow and oxygen to the brain, aid stroke recovery, and ameliorate Alzheimer's, Down's syndrome, dementia, and dyslexia, among other diseases and conditions...

     - Water-soluble racetam; The first of the racetams to be discovered (in the mid-1960s)
  • Oxiracetam
    Oxiracetam
    Oxiracetam is a nootropic drug of the racetam family.Several animal studies suggest that the substance is safe even when high doses are consumed for a long period of time. However the mechanism of action of oxiracetam is still a matter of research....

     - Water-soluble racetam (2 to 4 times more potent than Piracetam)
  • Aniracetam
    Aniracetam
    Aniracetam is a nootropic compound of the racetam family purported to be considerably more potent than piracetam. It is lipid soluble and has possible cognition enhancing effects. It has been tested in animals extensively, Alzheimer's patients and temporarily-impaired healthy subjects. It has...

     - Fat-soluble racetam (4 to 8 times more potent than Piracetam)
  • Pramiracetam
    Pramiracetam
    Pramiracetam is a nootropic drug derived from piracetam, and is more potent . It belongs to the racetam family of nootropics....

     - Fat-soluble racetam (8 to 30 times more potent than Piracetam)
  • Phenylpiracetam (Carphedon) - Fat-soluble racetam
  • Etiracetam
    Etiracetam
    Etiracetam is a nootropic drug of the racetam family. It is racemic; its biologically active optical form is levetiracetam....

  • Levetiracetam
    Levetiracetam
    Levetiracetam is an anticonvulsant medication used to treat epilepsy. It is S-enantiomer of etiracetam, structurally similar to the prototypical nootropic drug piracetam.Levetiracetam is marketed under the trade name Keppra...

     - anticonvulsant medication used to treat epilepsy. It is the S- enantiomer of etiracetam.
  • Nefiracetam
    Nefiracetam
    Nefiracetam is a nootropic drug of the racetam family.Nefiracetam’s cytoprotective actions are mediated by enhancement of GABAergic, Cholinergic, and Monoaminergic neuronal systems that give antiamnesia effects to the Alzheimer's type and cerebrovascular type of dementia....

     - an antidepressant (M1 acetylcholine receptor agonist)
  • Nicoracetam
    Nicoracetam
    Nicoracetam is a nootropic drug from the racetam family. It shares some structural similarities with aniracetam, but differs mostly in that it has a pyridine ring in place of aniracetam's benzene ring....

     - racetam structure bonded to niacin.
  • Rolziracetam
    Rolziracetam
    Rolziracetam is a nootropic drug of the racetam family.Rolziracetam was found to improve performance on a delayed-response task in aged rhesus monkeys. It has a wide margin of safety in animals and has been evaluated for use in cognitively impaired human subjects....

  • Nebracetam
    Nebracetam
    Nebracetam is nootropic drug of the racetam family, and an antidepressant ....

  • Fasoracetam
    Fasoracetam
    Fasoracetam is a nootropic drug of the racetam family....

  • Imuracetam
    Imuracetam
    Imuracetam is a nootropic drug of the racetam family....

  • Coluracetam
    Coluracetam
    Coluracetam is a nootropic drug of the racetam family. It may also have potential use in prevention and treatment of ischemic retinopathy and retinal and optic nerve injury.-References:...

     - may have potential use in prevention and treatment of ischemic retinopathy and retinal and optic nerve injury
  • Dimiracetam
    Dimiracetam
    Dimiracetam is a nootropic drug of the racetam family, derivatives of which may have application in the treatment of neuropathic pain....

     - currently being studied in the treatment of neuropathic pain.
  • Brivaracetam
    Brivaracetam
    Brivaracetam, the 4-n-propyl analog of levetiracetam, is a racetam derivative with anticonvulsant properties. Brivaracetam is believed to act by binding to the ubiquitous synaptic vesicle protein SV2. Phase II clinical trials in adult patients with refractory partial seizures were promising. The...

     - anticonvulsant properties
  • Seletracetam
    Seletracetam
    Seletracetam is a drug of the racetam family. It is currently being developed by UCB Pharmaceuticals as an anticonvulsant drug. While similar in structure to so-called nootropic drugs, it is not expected to have cognitive enhancing properties....

     - anticonvulsant, not expected to be nootropic
  • Rolipram
    Rolipram
    Rolipram is a PDE4-inhibitor. Like most PDE4-inhibitors, it is an anti-inflammatory drug. Rolipram is being researched as a possible alternative to current antidepressants. Recent studies show that rolipram may have antipsychotic effects. Other beneficial effects of rolipram are:* Improved long...

     - anti-inflammatory, antipsychotic and antidepressant drug that improves long term memory, increases wakefulness and neuroprotection (in rats).

Side effects


A 2005 review of the benefits and risks of levetiracetam
Levetiracetam
Levetiracetam is an anticonvulsant medication used to treat epilepsy. It is S-enantiomer of etiracetam, structurally similar to the prototypical nootropic drug piracetam.Levetiracetam is marketed under the trade name Keppra...

found that the effects reported which differed from placebo group included somnolence, asthenia, dizziness, and infection. Irritability, agitation, anger and aggressive behavior have also been reported and appear to be more common among learning disabled. Slightly lower white and red blood cell counts have been observed. The author concluded that levetiracetam exhibits a favorable safety profile. Interactions with other drugs have been reported and it is metabolized independently of the cytochrome P450 enzyme system.