CX-546

CX-546 is an ampakine drug developed by Cortex Pharmaceuticals.

CX-546
Clinical data
Other namesCX-546
Legal status
Legal status
Identifiers
IUPAC name
  • 2,3-dihydro-1,4-benzodioxin-7-yl-(1-piperidyl)methanone
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC14H17NO3
Molar mass247.294 g·mol−1
3D model (JSmol)
SMILES
  • C1CCN(CC1)C(=O)C2=CC3=C(C=C2)OCCO3
InChI
  • InChI=1S/C14H17NO3/c16-14(15-6-2-1-3-7-15)11-4-5-12-13(10-11)18-9-8-17-12/h4-5,10H,1-3,6-9H2 N
  • Key:LJUNPHMOGNFFOS-UHFFFAOYSA-N N
 NY (what is this?)  (verify)

It has been proposed as a treatment for schizophrenia.[1] 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.

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 produced by sedative drugs such as opioids and barbiturates.[2]

No effective respiratory stimulants are currently marketed for this application, with CX-546 being only the third drug discovered (after BIMU-8 and BW373U86) that effectively relieves the respiratory depression induced by fentanyl 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.

See also

References

  1. Lipina T, Weiss K, Roder J (2007). "The ampakine CX546 restores the prepulse inhibition and latent inhibition deficits in mGluR5-deficient mice". Neuropsychopharmacology. 32 (4): 745–56. doi:10.1038/sj.npp.1301191. PMID 16936708.
  2. Ren J, Poon BY, Tang Y, Funk GD, Greer JJ (Dec 2006). "Ampakines alleviate respiratory depression in rats". American Journal of Respiratory and Critical Care Medicine. 174 (12): 1384–91. doi:10.1164/rccm.200606-778OC. PMID 16973981.


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