Repositioning Candidate Details

Candidate ID: R0284
Source ID: DB00800
Source Type: approved
Compound Type: small molecule
Compound Name: Fenoldopam
Synonyms: --
Molecular Formula: C16H16ClNO3
SMILES: OC1=CC=C(C=C1)C1CNCCC2=C(Cl)C(O)=C(O)C=C12
Structure:
DrugBank Description: A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.
CAS Number: 67227-56-9
Molecular Weight: 305.756
DrugBank Indication: For the in-hospital, short-term (up to 48 hours) management of severe hypertension when rapid, but quickly reversible, emergency reduction of blood pressure is clinically indicated, including malignant hypertension with deteriorating end-organ function.
DrugBank Pharmacology: Fenoldopam is an agonist at D<sub>1</sub>-like dopamine receptors, binds to &alpha;<sub>2</sub>-adrenoceptors, increasing renal blood flow.
DrugBank MoA: Fenoldopam is a rapid-acting vasodilator. It is an agonist for D<sub>1</sub>-like dopamine receptors and binds with moderate affinity to &alpha;<sub>2</sub>-adrenoceptors. It has no significant affinity for D<sub>2</sub>-like receptors, &alpha;<sub>1</sub> and &beta;-adrenoceptors, 5<sub>HT1</sub> and 5<sub>HT2</sub> receptors, or muscarinic receptors. Fenoldopam is a racemic mixture with the R-isomer responsible for the biological activity. The R-isomer has approximately 250-fold higher affinity for D<sub>1</sub>-like receptors than does the S-isomer. In non-clinical studies, fenoldopam had no agonist effect on presynaptic D<sub>2</sub>-like dopamine receptors, or &alpha; or &beta; -adrenoceptors, nor did it affect angiotensin-converting enzyme activity. Fenoldopam may increase norepinephrine plasma concentration.
Targets: Dopamine D5 receptor agonist; Dopamine D1 receptor agonist; Alpha-2B adrenergic receptor antagonist; Alpha-2C adrenergic receptor antagonist; Alpha-2A adrenergic receptor antagonist; Alpha-1B adrenergic receptor inhibitor; Alpha-1D adrenergic receptor inhibitor; Alpha-1A adrenergic receptor inhibitor
Inclusion Criteria: Indication associated