Carbenoxolone (CBX) is a

glycyrrhetinic acid Enoxolone (International Nonproprietary Name, INN, British Approved Name, BAN; also known as glycyrrhetinic acid or glycyrrhetic acid) is a pentacyclic triterpenoid derivative of the beta-amyrin type obtained from the hydrolysis of glycyrrhizic a ...

derivative with a steroid-like structure, similar to substances found in the root of the licorice plant. Carbenoxolone is used for the treatment of peptic, esophageal and oral

ulcer An ulcer is a discontinuity or break in a bodily membrane that impedes normal function of the affected organ. According to Robbins's pathology, "ulcer is the breach of the continuity of skin, epithelium or mucous membrane caused by sloughin ...

ation and inflammation. Electrolyte imbalance is a serious side effect of carbenoxolone when used systemically. Carbenoxolone reversibly inhibits the conversion of inactive

cortisone Cortisone is a pregnene (21-carbon) steroid hormone. It is a naturally-occurring corticosteroid metabolite that is also used as a pharmaceutical prodrug. Cortisol is converted by the action of the enzyme corticosteroid 11-beta-dehydrogenase ...

cortisol Cortisol is a steroid hormone in the glucocorticoid class of hormones and a stress hormone. When used as medication, it is known as hydrocortisone. Cortisol is produced in many animals, mainly by the ''zona fasciculata'' of the adrenal corte ...

by blocking 11β-hydroxysteroid dehydrogenase (11β-HSD). 11β-HSD also reversibly catalyzes the conversion of 7-ketocholesterol to 7-beta-hydroxycholesterol. Carbenoxolone is a modestly potent, reasonably effective, water-soluble blocker of

gap junctions Gap junctions are Membrane channel, membrane channels between adjacent cells that allow the direct exchange of cytoplasmic substances, such small molecules, substrates, and metabolites. Gap junctions were first described as ''close appositions' ...

. Carbenoxolone has also been used in topical creams such as Carbosan gel, marketed for treatment of lip sores and mouth ulcers.

Nootropic effects

Carbenoxolone has also been investigated for

nootropic Nootropics ( or ) (colloquially brain supplements, smart drugs, cognitive enhancers, memory enhancers, or brain boosters) are chemical substances which purportedly improve cognitive functions, such as attention, memory, wakefulness, and self ...

effects. This research started from an observation that long-term exposure to

glucocorticoid Glucocorticoids (or, less commonly, glucocorticosteroids) are a class of corticosteroids, which are a class of steroid hormones. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor that is present in almost every vertebra ...

s may have negative effects on cognition. Carbenoxolone may decrease the amount of active glucocorticoid in the brain, because the drug inhibits 11β-HSD, an enzyme which regenerates

, an active glucocorticoid, from inactive

. 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 Verbal memory is a term used in cognitive psychology which refers to memory of words and other abstractions involving language. A variety of tests is used to test verbal memory, including learning lists or pairs of words, or recalling a story after ...

. However,

potassium-sparing diuretic Potassium-sparing diuretics or antikaliuretics refer to drugs that cause diuresis without causing potassium loss in the urine. They are typically used as an adjunct in management of hypertension, cirrhosis, and congestive heart failure. The ster ...

amiloride Amiloride, sold under the trade name Midamor among others, is a medication typically used with other medications to treat high blood pressure or swelling due to heart failure or cirrhosis of the liver. Amiloride is classified as a potassium-spar ...

was co-administered with carbenoxolone, since carbenoxolone used by itself may cause

hypertension Hypertension, also known as high blood pressure, is a Chronic condition, long-term Disease, medical condition in which the blood pressure in the artery, arteries is persistently elevated. High blood pressure usually does not cause symptoms i ...

by increasing cortisol in the kidneys.

References

{{Glucocorticoidics 11β-Hydroxysteroid dehydrogenase inhibitors Drugs acting on the gastrointestinal system and metabolism Nootropics Carboxylate esters Enones Triterpenes Pentacyclic compounds Dicarboxylic acids ru:Противоязвенные препараты и препараты для лечения гастроэзофагеального рефлюкса#Карбеноксолон

Nootropic effects

See also

References