Celiprolol

Beta blocker drug
  • C07AB08 (WHO)
Pharmacokinetic dataBioavailability30-70%Elimination half-life5 hoursIdentifiers
  • (RS)-N'-{3-Acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl}-N,N-diethylurea
CAS Number
  • 56980-93-9
PubChem CID
  • 2663
DrugBank
  • DB04846 checkY
ChemSpider
  • 2563
UNII
  • DRB57K47QC
KEGG
  • D07660
ChEMBL
  • ChEMBL27810
CompTox Dashboard (EPA)
  • DTXSID3020259 Edit this at Wikidata
ECHA InfoCard100.054.980 Edit this at WikidataChemical and physical dataFormulaC20H33N3O4Molar mass379.501 g·mol−13D model (JSmol)
  • Interactive image
ChiralityRacemic mixture
  • O=C(N(CC)CC)Nc1ccc(OCC(O)CNC(C)(C)C)c(c1)C(=O)C

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.

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.

External links

  • Selectol Summary of Product Characteristics (from the IPHA Medicines Compendium)
  • Celiprolol data sheet for New Zealand
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α1
Agonists
Antagonists
α2
Agonists
Antagonists
β
Agonists
Antagonists
  • See also: Receptor/signaling modulators
  • Dopaminergics
  • Serotonergics
  • Monoamine reuptake inhibitors
  • Monoamine releasing agents
  • Monoamine metabolism modulators
  • Monoamine neurotoxins
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