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. — Wikipedia
Clinical trial activity
4 trials · 5 clinical orgs · 0 marketing orgs
Earliest trial started Oct 1, 2003 (NCT00190411)
Timeline
Indications
Approved for
Mechanism of action
- Beta-1 adrenergic receptorANTAGONIST
ADRB1 antagonist
Celiprolol was developed as a third-generation ß-adrenoceptor antagonist with selective ß1-antagonist, partial ß2-agonist, and mild ¿2-antagonist actions. Given this combination of effects, celiprolol may be better described as a selective adrenoreceptor modulator. It has antihypertensive and antianginal properties.
- Adrenergic receptor alpha-2ANTAGONIST
Adrenergic receptor alpha-2 antagonist
Celiprolol was developed as a third-generation ß-adrenoceptor antagonist with selective ß1-antagonist, partial ß2-agonist, and mild ¿2-antagonist actions. Given this combination of effects, celiprolol may be better described as a selective adrenoreceptor modulator. It has antihypertensive and antianginal properties.
Weak antagonist.
- Beta-2 adrenergic receptorPARTIAL AGONIST
ADRB2 partial agonist
Celiprolol was developed as a third-generation ß-adrenoceptor antagonist with selective ß1-antagonist, partial ß2-agonist, and mild ¿2-antagonist actions. Given this combination of effects, celiprolol may be better described as a selective adrenoreceptor modulator. It has antihypertensive and antianginal properties.
Chemistry & pharmacology
SMILES
CCN(CC)C(=O)Nc1ccc(OCC(O)CNC(C)(C)C)c(C(C)=O)c1- Mol. weight
- 379.5 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL27810 ↗
- WikipediaCeliprolol ↗
- ChEMBLCHEMBL1742424 ↗
Also known as
- celectol
- celectol
- celiprolol
- celiprolol
- celiprolol
- celiprolol
- celiprolol
- celiprolol
- celiprolol
- celiprolol
- celiprolol
- celiprolol hcl
- celiprolol hcl
- celiprolol hcl
- celiprolol hydrochloride
- celiprolol hydrochloride
- celiprolol hydrochloride
- celiprolol monohydrochloride
- dl-celiprolol
- rs)-n'-{3-acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl}-n,n-diethylurea
- rs)-n'-{3-acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl}-n,n-diethylurea
- selecor
- selecor
- selectol
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05432466 | Phase 3 | Nov 7, 2022 | Acer Therapeutics |
| NCT03752931 | Phase 2 | Dec 31, 2018 | Abderrahmane Mami Hospital |
| NCT02380053 | Phase 4 | Jun 1, 2016 | University of Dundee |
| NCT00190411 | Phase 4 | Oct 1, 2003 | Aventis, University of Paris |
Organizations
Research & Development (5)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Abderrahmane Mami Hospital | Academic/Hospital | 1 | 1 | 1 | 2018 |
| Acer Therapeutics | For profit | 1 | 1 | 1 | 2022 |
| Aventis | For profit | 1 | 0 | 1 | 2003 |
| University of Dundee | Academic/Hospital | 1 | 1 | 1 | 2016 |
| University of Paris | Academic/Hospital | 1 | 1 | 1 | 2003 |