FENOLDOPAM

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

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 101 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 2678		40.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 567 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf	Primary		Approved 8429	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
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
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

AUC

Value	Dose	Co-administered	Analyte	Population
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
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

T_1/2

Value	Dose	Co-administered	Analyte	Population
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
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

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 Page: 1-61	unhealthy, 46±3 n = 9 Health Status: unhealthy Condition: Hypertension Age Group: 46±3 Sex: M+F Population Size: 9 Sources: https://pubmed.ncbi.nlm.nih.gov/1967592 Page: 1-61	Sources: https://pubmed.ncbi.nlm.nih.gov/1967592 Page: 1-61
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 Page: p.1	unhealthy Health Status: unhealthy Condition: Hypertension Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf Page: p.1	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 Page: p.1

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 Page: p.1	unhealthy Health Status: unhealthy Condition: Hypertension Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf Page: p.1
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 Page: p.1	unhealthy Health Status: unhealthy Condition: Hypertension Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf Page: p.1
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 Page: p.1	unhealthy Health Status: unhealthy Condition: Hypertension Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019922s016lbl.pdf Page: p.1

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
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
eMolecules	36518021	https://www.emolecules.com/cgi-bin/more?vid=36518021

PubMed

Title	Date	PubMed

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).

Name

Type

Language

FENOLDOPAM

Official Name

English

FENOLDOPAM [MI]

Common Name

English

Fenoldopam [WHO-DD]

Common Name

English

CARLACOR

Brand Name

English

fenoldopam [INN]

Common Name

English

FENOLDOPAM [VANDF]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C66884