Celiprolol

Celiprolol is a medication in the class of beta blockers, used in the treatment of high blood pressure. It has a unique pharmacology: it is a selective β1 receptor antagonist, but a β2 receptor partial agonist. It is also a weak α2 receptor antagonist.

Celiprolol
Clinical data
AHFS/Drugs.comInternational Drug Names
ATC code
Pharmacokinetic data
Bioavailability30-70%
Elimination half-life5 hours
Identifiers
IUPAC name
  • (RS)-N'-{3-Acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl}-N,N-diethylurea
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.054.980
Chemical and physical data
FormulaC20H33N3O4
Molar mass379.501 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
SMILES
  • O=C(N(CC)CC)Nc1ccc(OCC(O)CNC(C)(C)C)c(c1)C(=O)C

It was patented in 1973 and approved for medical use in 1982.[1]

Medical use

Celiprolol is believed to provide clinical benefit for people with vascular Ehlers–Danlos syndrome by promoting normal collagen synthesis in the blood vessels, and by shifting the pressure load away from the vessels most prone to dissection and rupture.[2] In 2019, a new drug application (NDA) for celiprolol was denied by the U.S. Food and Drug Administration (FDA), instead calling for an “adequate and well-controlled” trial to determine whether celiprolol reduced the risk of clinical events in patients with vEDS. [3]

Brand names

Brand names include Cardem, Selectol, Celipres, Celipro, Celol, Cordiax, Dilanorm

References
  1. Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 461. ISBN 9783527607495.
  2. Beridze N, Frishman WH (2012). "Vascular Ehlers-Danlos syndrome: pathophysiology, diagnosis, and prevention and treatment of its complications". Cardiology in Review. 20 (1): 4–7. doi:10.1097/CRD.0b013e3182342316. PMID 22143279. S2CID 9339508.
  3. Campbell P (25 June 2019). "FDA Denies NDA for Celiprolol". MD Magazine.
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