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IDRA-21

200px-IDRA-21

Overview

IDRA-21 is a relatively new nootropic compound. It works as an ampakine stimulant drug and is currently being researched in regards to its effects in memory improvement, cognitive enhancement, stimulation, and reversing cognitive deficits. It’s likely it was developed in 1994 or 1995 as the first clinical trials and peer-reviewed research articles appear in the literature in 1995.

Other Names

IDRA-21, 7-chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, C8H9ClN2O2S

IDRA-21 In A Nootropic Stack

Due to potential AMPAkine excitotoxicity, it is not recommended to combine IDRA-21 with other ampakine drugs such as Aniracetam. Little is known about toxicity in humans. Other Nootropics which increase glutamate should be avoided as well.

IDRA-21 Dosing

IDRA-21 currently has only had animal trials. Dosing in a study with Patas Monkeys was 3 or 5.6 mg/kg p.o. in addition with 30 mg/kg p.o. of Aniracetam[1]. This study indicated that IDRA-21 was 10-fold more potent than Aniracetam at reducing learning defects. A water maze study in rats showed cognitive enhancement at oral dosages of 4-120 mumol/kg[5].

Human dosages have no history of peer-reviewed clinical studies. Some reading online suggested positive human activity at 5-25mg orally[2].

IDRA-21 Structure

IDRA-21 is a benzothiazone derivative. It’s structurally unrelated to Aniracetam, another ampakine drug. It’s a chiral molecule, with the dextrorotary isomer being the active form[6].

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IDRA-21 Absorption

There is very little information about absorption rates. Most rat and monkey studies determined efficacy with oral dosing, which would seem to indicate that oral is an effective route.

IDRA-21 Benefits

  • Increases in cognition (Matching sample tasks performed by Rhesus Monkeys)[7]

  • Increased Task Accuracy[7]

  • Increases in Short Term Memory[8]

  • Potential Therapeutic Effects On Schizophrenia[8]

  • Potental Therapeutic Effects On Depression[8]

  • Neuroprotection[5]

  • Benefits Against Alprazolam-induced Cognitive Deficit[1]

IDRA-21 Mechanism Of Action

IDRA belongs to a class of compounds known as ampakines. Ampakines are allosteric modulators of AMPA receptors in the brain. AMPA receptors are responsible for fast synaptic transmission [9] and are implicated in synaptic plasticity and long term potentiation [10].

As an Ampakine, IDRA-21 works by modulating AMPA receptors in the brain. Specifically IDRA-21 binds to the allosteric site of the AMPA receptor and induce positive modulation, this is sometimes called allosteric activation.

Initial research on IDRA-21 suggests that it may prevent AMPA receptor desensitization (1) and therefore increase synaptic responses and support memory and learning.

IDRA-21 Safety and Side Effects

IDRA-21 is a potent Ampakine. AMPA activation has been shown to exacerbate hippocampal neural damage[3]. IDRA-21 when administered with glutamate killed rat hippocampal neurons through AMPA excitoxicity[3]. This is potentially dangerous in patients with conditions that excessively activate AMPA such as strokes and seizures.

In another study, the dosages of IDRA-21 that induced neurotoxicity were several orders of magnitude higher than the doses that achieved cognitive enhancement in rats and monkeys, leading the researchers to conclude that IDRA-21 has relatively low neurotoxicity in therapeutic doses[4].

References

  1. http://www.ncbi.nlm.nih.gov/pubmed/7644474

  2. http://www.reddit.com/r/Nootropics/comments/1pqmms/experiences_with_idra21/

  3. http://www.ncbi.nlm.nih.gov/pubmed/9585363

  4. http://www.ncbi.nlm.nih.gov/pubmed/9192690

  5. http://www.ncbi.nlm.nih.gov/pubmed/7815345

  6. http://www.ncbi.nlm.nih.gov/pubmed/7500277

  7. http://www.ncbi.nlm.nih.gov/pubmed/14654093

  8. http://www.ncbi.nlm.nih.gov/pubmed/15672275

  9. http://www.ncbi.nlm.nih.gov/pubmed/16376594

  10. http://physrev.physiology.org/content/84/1/87.full