Carbenoxolone

drugbox
IUPAC_name = (3β)-3- [(3-carboxypropanoyl)oxy] -11-oxoolean- 12-en-30-oic acid



CAS_number = 5697-56-3
ATC_prefix = A02
ATC_suffix = BX01
ATC_supplemental =
PubChem = 636403
DrugBank = EXPT00848
C=34 | H=50 | O=7
molecular_weight = 570.765 g/mol
bioavailability =
protein_bound =
metabolism =
elimination_half-life =
pregnancy_category =
legal_status =
routes_of_administration =

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.cite journal |author=Sandeep TC, Yau JL, MacLullich AM, "et al" |title=11Beta-hydroxysteroid dehydrogenase inhibition improves cognitive function in healthy elderly men and type 2 diabetics |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=101 |issue=17 |pages=6734–9 |year=2004 |pmid=15071189 |doi=10.1073/pnas.0306996101 |url=http://www.pnas.org/cgi/pmidlookup?view=long&pmid=15071189]

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


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