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Carbenoxolone
Systematic (IUPAC) name
(3β)-3-[(3-carboxypropanoyl)oxy]-11-oxoolean-12-en-30-oic acid
OR
(2S,4aS,6aS,6bR,8aR,10 S,12aS,12bR,14bR)-10-(3-carboxypropanoyloxy)-2,4a,6a,6b,9,9,12a-heptamethyl-13-oxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,13,14b-icosahydropicene-2-carboxylic acid
Identifiers
CAS number 5697-56-3
ATC code A02BX01
PubChem 636403
DrugBank EXPT00848
Chemical data
Formula C 34H50O7  
Mol. mass 570.765 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
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

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