IDRA-21 is a

positive allosteric modulator In pharmacology and biochemistry, allosteric modulators are a group of substances that bind to a receptor to change that receptor's response to stimulus. Some of them, like benzodiazepines, are drugs. The site that an allosteric modulator binds to ...

of the AMPA receptor and a

benzothiadiazine Benzothiadiazine is a bicyclic heterocyclic benzene derivative with the heterocycle containing two nitrogens and one sulfur. Some benzothiadiazine derivatives are used as pharmaceutical drugs, including: * bendroflumethiazide * chlorothiazide ...

derivative. It is a chiral molecule, with (+)-IDRA-21 being the active form. IDRA-21 shows

nootropic Nootropics ( , or ) (colloquial: smart drugs and cognitive enhancers, similar to adaptogens) are a wide range of natural or synthetic dietary supplement, supplements or drugs and other substances that are claimed to improve cognitive function ...

effects in animal studies, significantly improving learning and memory. It is around 10–30 times more potent than aniracetam in reversing cognitive deficits induced by

alprazolam Alprazolam, sold under the brand name Xanax, among others, is a fast-acting, potent tranquilizer of medium duration in the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring. It is most commonly u ...

or scopolamine, and produces sustained effects lasting for up to 48 hours after a single dose. The mechanism for this action is thought to be through promoting the induction of

long-term potentiation In neuroscience, long-term potentiation (LTP) is a persistent strengthening of synapses based on recent patterns of activity. These are patterns of synaptic activity that produce a long-lasting increase in signal transmission between two neurons ...

between synapses in the brain. IDRA-21 may not produce

neurotoxicity Neurotoxicity is a form of toxicity in which a biological, chemical, or physical agent produces an adverse effect on the structure or function of the central and/or peripheral nervous system. It occurs when exposure to a substance – specificall ...

under normal conditions, although it may worsen neuronal damage following global ischemia after stroke or

seizures An epileptic seizure, informally known as a seizure, is a period of symptoms due to abnormally excessive or synchronous neuronal activity in the brain. Outward effects vary from uncontrolled shaking movements involving much of the body with l ...

. In comparison to the ampakines or benzoylpiperidine-derived AMPA receptor potentiators, IDRA-21 was more potent than CX-516, but less potent than

CX-546 CX-546 is an ampakine drug developed by Cortex Pharmaceuticals. It has been proposed as a treatment for schizophrenia. CX-546 was the second drug of note to come out of the Cortex research program, after CX-516, but while it was an improvement o ...

. Newer benzothiadiazide derivatives with greatly increased potency compared to IDRA-21 have been developed, but these have not been researched to the same extent, with the benzoylpiperidine and benzoylpyrrolidine CX-series of drugs being favoured for clinical development, most likely due to more favourable toxicity profiles at high doses.

References

{{Ionotropic glutamate receptor modulators AMPA receptor positive allosteric modulators Benzothiadiazines Chloroarenes Experimental drugs Nootropics

See also

References