Preferred Label : 11beta-hydroxysteroid Dehydrogenase Type 1 Inhibitor AZD4017;
NCIt synonyms : 11bHSD1 Inhibitor AZD4017; 11-beta-hydroxysteroid Dehydrogenase Type 1 Inhibitor AZD4017; 11b-HSD1 inhibitor AZD4017;
NCIt related terms : AZD-4017;
NCIt definition : A selective, orally bioavailable inhibitor of the enzyme 11beta-hydroxysteroid dehydrogenase
type 1 (11b-HSD1; 11bHSD1; HSD11B1), with potential protective activity. Upon administration,
AZD4017 selectively binds to and inhibits the activity of 11b-HSD1. This prevents
the conversion of cortisone to the active hormone cortisol that activates glucocorticoid
receptors. By blocking cortisol production in metabolic tissues, AZD4017 may inhibit
the adverse metabolic effects, such as glucose intolerance, hyperinsulinemia, systolic
hypertension, increased adiposity, myoatrophy and dermal atrophy, caused by exogenous
administration of glucocorticoids in these tissues. 11bHSD1 is highly expressed in
metabolic tissues, such as liver, skeletal muscle, and adipose tissue. It plays a
crucial role in regenerating active glucocorticoid from circulating glucocorticoids
and regulates the production of cortisol to activate the glucocorticoid receptors.
AZD4017 does not inhibit the anti-inflammatory activity of the administered glucocorticoids.;
UNII : 3JL137394Y;
CAS number : 1024033-43-9;
Molecule name : AZD 4017; AZD-4017;
Origin ID : C148516;
UMLS CUI : C3501337;
Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
