CX-546 is an

ampakine Ampakines, also stylized as 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 recepto ...

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 2005, ...

. It has been proposed as a treatment for

schizophrenia Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social withdra ...

. CX-546 was the second drug of note to come out of the Cortex research program, after

CX-516 CX-516 is an ampakine and nootropic that acts as an AMPA receptor positive allosteric modulator and had been undergoing development by a collaboration between Cortex, Shire, and Servier. It was studied as a potential treatment for Alzheimer' ...

, 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 CX-614 is an ampakine drug developed by Cortex Pharmaceuticals. It has been investigated for its effect on AMPA receptors. Chronic CX-614 treatments produce rapid increases in the synthesis of the brain-derived neurotrophic factor BDNF which has ...

and

CX-717 CX717 is an ampakine compound created by Christopher Marrs and Gary Rogers in 1996 at Cortex Pharmaceuticals. It affects the neurotransmitter glutamate, with trials showing the drug improves cognitive functioning and memory. Approval process I ...

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 (hypercapnia ...

produced by sedative drugs such as

opioid Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid us ...

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 BIMU-8 is a drug which acts as a 5-HT4 receptor selective agonist. BIMU-8 was one of the first compounds of this class. The main action of BIMU-8 is to increase the rate of respiration by activating an area of the brain stem known as the pre-Bo ...

and

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

) that effectively relieves the respiratory depression induced by

fentanyl Fentanyl, also spelled fentanil, is a very potent synthetic opioid used as a pain medication. Together with other drugs, fentanyl is used for anesthesia. It is also used illicitly as a recreational drug, sometimes mixed with heroin, cocaine ...

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 CX717 is an ampakine compound created by Christopher Marrs and Gary Rogers in 1996 at Cortex Pharmaceuticals. It affects the neurotransmitter glutamate, with trials showing the drug improves cognitive functioning and memory. Approval process In ...

or CX-1763, which are likely to be more suitable for commercial development.

References

1-Piperidinyl compounds Ampakines Respiratory agents AMPA receptor positive allosteric modulators Benzodioxans Benzamides Experimental drugs {{nervous-system-drug-stub

See also

References