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Celiprolol

From Wikipedia, the free encyclopedia
Beta blocker drug
Pharmaceutical compound
Celiprolol
Clinical data
AHFS/Drugs.comInternational Drug Names
ATC code
Pharmacokinetic data
Bioavailability30-70%
Eliminationhalf-life5 hours
Identifiers
  • (RS)-N'-{3-Acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl}-N,N-diethylurea
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.054.980Edit this at Wikidata
Chemical and physical data
FormulaC20H33N3O4
Molar mass379.501 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
  • O=C(N(CC)CC)Nc1ccc(OCC(O)CNC(C)(C)C)c(c1)C(=O)C

Celiprolol is amedication in the class ofbeta blockers, used in the treatment ofhigh blood pressure. It has a unique pharmacology: it is a selectiveβ1 receptorantagonist, but aβ2 receptor partialagonist. It is also a weakα2 receptor antagonist.

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

Medical use

[edit]

Celiprolol is believed to provide clinical benefit for people with vascularEhlers–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] In June 2022, Acer Therapeutics Inc. sponsored "Clinical Trial to Compare the Efficacy of Celiprolol to Placebo in Patients With Vascular Ehlers-Danlos Syndrome (DiSCOVER)".[4]

Brand names

[edit]

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

References

[edit]
  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.
  4. ^"Clinical Trial to Compare the Efficacy of Celiprolol to Placebo in Patients With Vascular Ehlers-Danlos Syndrome (DiSCOVER)".NLM.gov Clinical Trials. 2022-06-21.

External links

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β, non-selective
β1-selective
β2-selective
α1- + β-selective
α1
Agonists
Antagonists
α2
Agonists
Antagonists
β
Agonists
Antagonists


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