prenalterol Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
bronchodilators, phenethylamine derivatives 2258 57526-81-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • prenalterol
  • (S)-Prenalterol
  • (-)-Prenalterol
  • S-Varbian
A partial adrenergic agonist with functional beta 1-receptor specificity and inotropic effect. It is effective in the treatment of acute CARDIAC FAILURE, postmyocardial infarction low-output syndrome, SHOCK, and reducing ORTHOSTATIC HYPOTENSION in the SHY-RAGER SYNDROME.
  • Molecular weight: 225.29
  • Formula: C12H19NO3
  • CLOGP: 1.09
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 3
  • TPSA: 61.72
  • ALOGS: -1.94
  • ROTB: 6

Drug dosage:

DoseUnitRoute
10 mg P

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.48 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 33 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 4.28 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 22.10 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.85 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1980 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC C01CA13 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
Adrenergic and dopaminergic agents
MeSH PA D018663 Adrenergic Agents
MeSH PA D000322 Adrenergic Agonists
MeSH PA D058665 Adrenergic beta-1 Receptor Agonists
MeSH PA D000318 Adrenergic beta-Agonists
MeSH PA D002316 Cardiotonic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D020011 Protective Agents
MeSH PA D013566 Sympathomimetics

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.48 acidic
pKa2 9.19 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-1 adrenergic receptor GPCR Ki 6.60 WOMBAT-PK
Beta-2 adrenergic receptor GPCR Kd 5.97 CHEMBL

External reference:

IDSource
C0033051 UMLSCUI
CHEBI:8391 CHEBI
CHEMBL1160714 ChEMBL_ID
DB13777 DRUGBANK_ID
D011294 MESH_DESCRIPTOR_UI
42396 PUBCHEM_CID
4121 INN_ID
537 IUPHAR_LIGAND_ID
M4G34404CX UNII

Pharmaceutical products:

None