CX-546 is an

ampakine Ampakines or AMPAkines are a subgroup of AMPA receptor positive allosteric modulators with a benzamide or closely related chemical structure. They are also known as "CX compounds". Ampakines take their name from the AMPA receptor (AMPAR), a type ...

drug developed by

Cortex Pharmaceuticals RespireRx Pharmaceuticals Inc. (formerly Cortex Pharmaceuticals, Inc.) () is a pharmaceutical company based in Glen Rock, New Jersey specializing in positive allosteric modulators of the AMPA receptor known as Ampakines. History In February 2 ...

. It has been proposed as a treatment for

schizophrenia Schizophrenia () is a mental disorder characterized variously by hallucinations (typically, Auditory hallucination#Schizophrenia, hearing voices), delusions, thought disorder, disorganized thinking and behavior, and Reduced affect display, f ...

. 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 over its predecessor in some respects, it still has problems with limited oral

bioavailability In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation. By definition, when a medication is administered intravenously, its bioavailability is 100%. H ...

. However, CX-546 still represented a significant advance that led on to the development of newer compounds such as CX-614 and CX-717 with superior properties over the earlier drugs. CX-546 itself has been investigated for other applications, and most notably has been found to show significant efficacy in reversing the

respiratory depression Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (''hypo'' meaning "below") to perform needed respiratory gas exchange. By definition it causes an increased concentration of carbon dioxide (hypercapni ...

produced by

sedative A sedative or tranquilliser is a substance that induces sedation by reducing irritability or Psychomotor agitation, excitement. They are central nervous system (CNS) Depressant, depressants and interact with brain activity, causing its decelera ...

drugs such as

opioid Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, ...

s and

barbiturates Barbiturates are a class of depressant drugs that are chemically derived from barbituric acid. They are effective when used medically as anxiolytics, hypnotics, and anticonvulsants, but have physical and psychological addiction potential as ...

. No effective respiratory stimulants are currently marketed for this application, with CX-546 being only the third drug discovered (after BIMU-8 and

BW373U86 (+)-BW373U86 is an opioid analgesic drug used in scientific research. BW373U86 is a selective agonist for the δ-opioid receptor, with approximately 15× stronger affinity for the δ-opioid than the μ-opioid receptor. It has potent analgesic ...

) that effectively relieves the respiratory depression induced by

fentanyl Fentanyl is a highly potent synthetic piperidine opioid primarily used as an analgesic (pain medication). It is 30 to 50 times more Potency (pharmacology), potent than heroin and 50 to 100 times more potent than morphine. Its primary Medici ...

without reducing the analgesic effects. CX-546 could be developed for this purpose, although it is more likely that Cortex will use newer and more potent analogues such as CX-1739 or CX-1763, which are likely to be more suitable for commercial development.

References

{{Ionotropic glutamate receptor modulators 1-Piperidinyl compounds Ampakines Respiratory agents AMPA receptor positive allosteric modulators Benzodioxans Benzamides Experimental drugs

See also

References