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Details

Stereochemistry RACEMIC
Molecular Formula C16H16ClNO3.ClH
Molecular Weight 342.217
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FENOLDOPAM HYDROCHLORIDE

SMILES

Cl.OC1=CC=C(C=C1)C2CNCCC3=C(Cl)C(O)=C(O)C=C23

InChI

InChIKey=NLMPGIXLXSPNFS-UHFFFAOYSA-N
InChI=1S/C16H16ClNO3.ClH/c17-15-11-5-6-18-8-13(9-1-3-10(19)4-2-9)12(11)7-14(20)16(15)21;/h1-4,7,13,18-21H,5-6,8H2;1H

HIDE SMILES / InChI

Molecular Formula C16H16ClNO3
Molecular Weight 305.756
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Fenoldopam (marketed under the brand name Corlopam) is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist. Fenoldopam is a rapid-acting vasodilator. It is an agonist for D1-like dopamine receptors and binds with moderate affinity to α2-adrenoceptors. It has no significant affinity for D2-like receptors, α1 and β adrenoceptors, 5HT1 and 5HT2 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 D1-like receptors than does the S-isomer. Fenoldopam Mesylate Injection, USP is indicated 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.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
40.0 nM [Ki]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
CORLOPAM

Cmax

ValueDoseCo-administeredAnalytePopulation
10.9 ng/mL
100 mg single, oral
FENOLDOPAM plasma
Homo sapiens
26.5 ng/mL
100 mg single, oral
FENOLDOPAM plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
26.8 ng × h/mL
100 mg single, oral
FENOLDOPAM plasma
Homo sapiens
44.7 ng × h/mL
100 mg single, oral
FENOLDOPAM plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
2.6 h
100 mg single, oral
FENOLDOPAM plasma
Homo sapiens
2.9 h
100 mg single, oral
FENOLDOPAM plasma
Homo sapiens

Doses

AEs

PubMed

Sample Use Guides

In Vivo Use Guide
Adults: Initiate dosing at 0.01 to 0.3 mcg/kg/min by continuous infusion. Dosing can be increased in increments of 0.05 to 0.1 mcg/kg/minute every 15 minutes or longer until target blood pressure is reached. Dilute prior to administration Pediatrics: Initiate dosing at 0.2 mcg/kg/minute by continuous infusion and titrate dose by 0.3 to 0.5 mcg/kg/min every 20-30 minutes to a maximum dose of 0.8 mcg/kg/minute
Route of Administration: Intravenous
In Vitro Use Guide
Incubation of freshly isolated mouse kidney slices with the selective D(1)-like receptor agonists fenoldopam (10 uM) and SKF-38393 (10 uM) for 1 h induced NaPi-IIa internalization and reduced expression of NaPi-IIa in the brush border membrane (BBM).
Substance Class Chemical
Record UNII
425S22SN3P
Record Status Validated (UNII)
Record Version