Carbenoxolone

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Carbenoxolone
Systematic (IUPAC) name
(3β)-3-[(3-carboxypropanoyl)oxy]-11-oxoolean- 12-en-30-oic acid
Identifiers
CAS number 5697-56-3
ATC code A02BX01
PubChem 636403
DrugBank EXPT00848
Chemical data
Formula C34H50O7 
Mol. mass 570.765 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

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Legal status
Routes  ?

Carbenoxolone, a synthetic derivative of glycyrrhizinic acid, is a licensed drug (in the UK) for oesophageal ulceration and inflammation. Other uses include treatment of oral and perioral lesions.

Carbenoxolone (aka Carbenoxolone, CBX) is also finding increasing use as a Connexon (a hemichannel made up of 6 connexin subunits) blocker and as a gap junction (2 connexons joined together) blocker.

Nootropic effects

Carbenoxolone has also been investigated for nootropic effects.[1]

This research started from an observation that long-term exposure to glucocorticoids may have negative effects on cognition. Carbenoxolone may decrease the amount of active glucocortocoid in the brain, because the drug inhibits 11Beta-hydroxysteroid dehydrogenase type 1, an enzyme which activates cortisol from cortisone, a glucocorticoid. In the research trial investigating this use of carbenoloxone, it was shown that the drug improved verbal fluency in elderly healthy men (aged 55-75). In type 2 diabetics aged 52-70, the drug improved verbal memory. However, it should be noted that potassium-sparing diuretic amiloride was co-administered with carbenoxolone, since carbenoxolone used by itself may cause hypertension by increasing cortisol in the kidneys.

References

  1. ^ Sandeep TC, Yau JL, MacLullich AM, et al (2004). "11Beta-hydroxysteroid dehydrogenase inhibition improves cognitive function in healthy elderly men and type 2 diabetics". Proc. Natl. Acad. Sci. U.S.A. 101 (17): 6734–9. doi:10.1073/pnas.0306996101. PMID 15071189. 

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  • This page was last modified on 6 June 2008, at 14:52.

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