FENOLDOPAM

US Previously Marketed

Details

Stereochemistry	RACEMIC
Molecular Formula	C16H16ClNO3
Molecular Weight	305.756
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

InChI

InChIKey=TVURRHSHRRELCG-UHFFFAOYSA-N

InChI=1S/C16H16ClNO3/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

HIDE SMILES / InChI

Molecular Formula	C16H16ClNO3
Molecular Weight	305.756
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf | https://www.drugbank.ca/drugs/DB00800

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 Target	Pharmacology	Condition	Potency
Dopamine D1 receptor 106 Target ID: CHEMBL2056 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/9784114 \| https://www.ncbi.nlm.nih.gov/pubmed/7525564	Agonist 2752		40.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 575 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf	Primary		Approved 8583	CORLOPAM Approved Use Adult Patients: Fenoldopam 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. Transition to oral therapy with another agent can begin at any time after blood pressure is stable during fenoldopam infusion. Pediatric Patients: Fenoldopam is indicated for the in-hospital, short-term (up to 4 hours) reduction in blood pressure. Launch Date 1997

C_max

Value	Dose	Co-administered	Analyte	Population
26.5 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/1673097	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:		FENOLDOPAM plasma	Homo sapiens population: UNHEALTHY age: UNKNOWN sex: FEMALE / MALE food status: FASTED
10.9 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/1673097	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:		FENOLDOPAM plasma	Homo sapiens population: UNHEALTHY age: UNKNOWN sex: FEMALE / MALE food status: FED

AUC

Value	Dose	Co-administered	Analyte	Population
44.7 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/1673097	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:		FENOLDOPAM plasma	Homo sapiens population: UNHEALTHY age: UNKNOWN sex: FEMALE / MALE food status: FASTED
26.8 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/1673097	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:		FENOLDOPAM plasma	Homo sapiens population: UNHEALTHY age: UNKNOWN sex: FEMALE / MALE food status: FED

T_1/2

Value	Dose	Co-administered	Analyte	Population
2.9 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/1673097	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:		FENOLDOPAM plasma	Homo sapiens population: UNHEALTHY age: UNKNOWN sex: FEMALE / MALE food status: FASTED
2.6 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/1673097	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:		FENOLDOPAM plasma	Homo sapiens population: UNHEALTHY age: UNKNOWN sex: FEMALE / MALE food status: FED

Doses

Dose	Population	Adverse events
1.5 ug/kg/min single, intravenous Highest studied dose Dose: 1.5 ug/kg/min Route: intravenous Route: single Dose: 1.5 ug/kg/min Sources: https://pubmed.ncbi.nlm.nih.gov/1967592	unhealthy, 46±3 Health Status: unhealthy Age Group: 46±3 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/1967592	Sources: https://pubmed.ncbi.nlm.nih.gov/1967592
0.8 ug/kg/min single, intravenous Recommended Dose: 0.8 ug/kg/min Route: intravenous Route: single Dose: 0.8 ug/kg/min Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf	Disc. AE: Tachycardia, Hypokalemia... AEs leading to discontinuation/dose reduction: Tachycardia Hypokalemia Anaphylactic reaction Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf

AEs

AE	Significance	Dose	Population
Anaphylactic reaction	Disc. AE	0.8 ug/kg/min single, intravenous Recommended Dose: 0.8 ug/kg/min Route: intravenous Route: single Dose: 0.8 ug/kg/min Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf
Hypokalemia	Disc. AE	0.8 ug/kg/min single, intravenous Recommended Dose: 0.8 ug/kg/min Route: intravenous Route: single Dose: 0.8 ug/kg/min Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf
Tachycardia	Disc. AE	0.8 ug/kg/min single, intravenous Recommended Dose: 0.8 ug/kg/min Route: intravenous Route: single Dose: 0.8 ug/kg/min Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252	inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
MRP3 246 BSEP 550 MRP4 290 CYP2C19 2057 CYP1A2 2153 MRP2 499 CYP19A1 429	SULT 12 COMT 8 CYP 303 UGT 219

Drug as perpetrator

Target	Modality	Activity
CYP2D6 2546	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1645840#sid=170465321	inconclusive [IC50 10.964 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1671197#sid=170465321	no [IC50 9.7717 uM]
BSEP 554	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/22961681/	no [IC50 >1000 uM]
MRP2 625	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
MRP3 326	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
MRP4 345	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
CYP19A1 430	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/743139#sid=144203703	no
CYP1A2 2333	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1671199#sid=170465321	no
CYP2C9 2497	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1645842#sid=170465321	no
CYP3A4 2633	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1645841#sid=170465321	no

Drug as victim

Target	Modality	Activity
CYP 303	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/019922s019lbl.pdf#page=11 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/019922ap_corlopam_clinphrmr.pdf#page=35 Page: 11, (ClinP) 35	no
COMT 8	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/019922ap_corlopam_clinphrmr.pdf#page=35 Page: 35-46	yes
SULT 12	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/019922s019lbl.pdf#page=11 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/019922ap_corlopam_clinphrmr.pdf#page=35 Page: 11, (ClinP) 35-46	yes
UGT 219	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/019922s019lbl.pdf#page=11 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/019922ap_corlopam_clinphrmr.pdf#page=35 Page: 11, (ClinP) 35-46	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/588834#sid=50106351 \| https://pubchem.ncbi.nlm.nih.gov/bioassay/588834#sid=26752227

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:5002	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:5002
ChemicalBook	CB6729842	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB6729842
eMolecules	36518021	https://www.emolecules.com/cgi-bin/more?vid=36518021
MolPort	MolPort-006-167-637	https://www.molport.com/shop/molecule-link/MolPort-006-167-637
Selleck Chemicals	fenoldopam-corlopam	http://www.selleckchem.com/products/fenoldopam-corlopam.html

PubMed

Title	Date	PubMed
Effects of short-term fenoldopam infusion on gastric mucosal blood flow in septic shock.	2004-09	15329581
N-Acetylcysteine versus fenoldopam mesylate to prevent contrast agent-associated nephrotoxicity.	2004-08-18	15312855
Periprocedural hypertension: current concepts in management for the vascular surgeon.	2004-08-13	15306955
In vitro effects of antihypertensive drugs on thromboxane agonist (U46619)-induced vasoconstriction in human internal mammary artery.	2004-08	15169740
Prevention of radiocontrast-induced nephropathy.	2004-07	15211433
Lessons in formulary management: the case of fenoldopam for radiographic contrast material-induced nephropathy.	2004-06	15222676
Prevention of contrast media nephrotoxicity--the story so far.	2004-05	15081843
Fenoldopam versus nitroprusside for the treatment of hypertensive emergency.	2004-05	15039472
[Involvement of dopamine receptor in the pathogenesis of hypertension and hypertensive target-organ damage].	2004-03	15171362
Prophylaxis of iodinated contrast media-induced nephropathy: a pharmacological point of view.	2004-03	15076008
Dopamine D1 receptor augmentation of D3 receptor action in rat aortic or mesenteric vascular smooth muscles.	2004-03	14769810
Aberrant D1 and D3 dopamine receptor transregulation in hypertension.	2004-03	14732731
American society of nephrology-36th annual meeting and renal week 2003.	2004-01	14968812
Optimization of intestinal mucosal oxygenation in shock: a role for medical therapy?	2004-01	14707603
Dopamine under alpha1-blockade, but not dopamine alone or fenoldopam, increases depressed gastric mucosal oxygenation.	2004-01	14707574
Phlebotomy in the intensive care unit: strategies for blood conservation.	2004	15196321
Amygdaloid D1 receptors are not linked to stimulation of adenylate cyclase.	2003-12-15	14556237
Effect of fenoldopam on renal function after nephrotomy in normal dogs.	2003-12-03	14648536
Fenoldopam and N-acetylcysteine for the prevention of radiographic contrast material-induced nephropathy: a review.	2003-12	14695041
Monitoring renal oxygen supply in critically-ill patients using urinary oxygen tension.	2003-12	14633556
Fenoldopam mesylate for the prevention of contrast-induced nephropathy: a randomized controlled trial.	2003-11-05	14600187
[Fenoldopam and kidney function in a case of abdominal aortic pseudoaneurysm with supra-renal clamping in an emergency protocol].	2003-11	14679918
The effects of intraoperative fenoldopam on renal blood flow and tubular function following suprarenal aortic cross-clamping.	2003-11	14569432
Clinical review: the management of hypertensive crises.	2003-10	12974970
Perturbation of D1 dopamine and AT1 receptor interaction in spontaneously hypertensive rats.	2003-10	12900438
Effects of fenoldopam on renal blood flow and its function in a canine model of rhabdomyolysis.	2003-09	12974592
Fenoldopam for renal protection in patients undergoing cardiopulmonary bypass.	2003-08	12968238
Pharmacologic identification of putative D1 dopamine receptors in feline kidneys.	2003-08	12887611
Dopamine D1 receptor-dependent inhibition of NaCl transport in the rat thick ascending limb: mechanism of action.	2003-07-25	12892837
Fenoldopam--but not dopamine--selectively increases gastric mucosal oxygenation in dogs.	2003-07	12847395
Receptor mechanisms of prenodal lymphatic constriction by dopamine.	2003-06-15	12763634
Contrast agent--associated nephrotoxicity.	2003-06-12	12800130
Acetylcysteine and fenoldopam. Promising new approaches for preventing effects of contrast nephrotoxicity.	2003-06	12830779
Fenoldopam treatment improves peripheral insulin sensitivity and renal function in STZ-induced type 2 diabetic rats.	2003-05	12797596
Radiocontrast-induced nephropathy and percutaneous coronary intervention: a review of preventive measures.	2003-05	12739990
Pharmacological profile of the vascular responses to dopamine in the canine external carotid circulation.	2003-04	12753419
Radiocontrast-induced nephropathy.	2003-03-12	12629594
Galpha12- and Galpha13-protein subunit linkage of D5 dopamine receptors in the nephron.	2003-03	12623966
A case series of low-dose fenoldopam in seventy cardiac surgical patients at increased risk of renal dysfunction.	2003-02	12635055
The International Sepsis Forum's controversies in sepsis: my initial vasopressor agent in septic shock is dopamine rather than norepinephrine.	2003-02	12617729
Contrast nephropathy : an evidence-based approach to prevention.	2003	14728060
Hypertensive emergencies. Etiology and management.	2003	14727943
Malignant hypertension presenting as hemolysis, thrombocytopenia, and renal failure.	2003	14674379
A review of pharmacologic interventions to prevent contrast-induced nephropathy.	2003	14668708
The role of the DA1 receptor agonist fenoldopam in the management of critically ill, transplant, and hypertensive patients.	2003	12556736
Improving perioperative outcomes in patients with end-stage heart failure.	2003	12556735
Contemporary strategies to preserve renal function during cardiac and vascular surgery.	2003	12556734
A review of contemporary prevention strategies for radiocontrast nephropathy: a focus on fenoldopam and N-acetylcysteine.	2003	12556733
Cardiovascular function during induced hypotension by fenoldopam or sodium nitroprusside in anesthetized dogs.	1992-01	1346487
Effect of fenoldopam on the acute and subacute nephrotoxicity produced by amphotericin B in the dog.	1992-01	1346161

Patents

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 Created by `admin` on `Mon Mar 31 17:59:27 GMT 2025` Edited by `admin` on `Mon Mar 31 17:59:27 GMT 2025`
Record UNII	INU8H2KAWG
Record Status	`Validated (UNII)`
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Name

Type

Language

FENOLDOPAM

Official Name

English

CARLACOR

Preferred Name

English

FENOLDOPAM [MI]

Common Name

English

Fenoldopam [WHO-DD]

Common Name

English

fenoldopam [INN]

Common Name

English

FENOLDOPAM [VANDF]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C66884