DA1 receptor ( EC50 = 55.5 nM )

Absorption, Distribution and Excretion
Radiolabeled studies indicate that approximately 90% of infused Fenoldopam is excreted in the urine and 10% in the feces. It is primarily excreted via conjugation reactions, not involving cytochrome P-450 enzymes. Only 4% of the administered dose is excreted unchanged. Metabolism/Metabolites It is primarily excreted via conjugation reactions, not involving cytochrome P-450 enzymes. Methylation, glucuronidation, and sulfation are the main conjugation pathways. Biological Half-Life In patients with mild to moderate hypertension, its elimination half-life is approximately 5 minutes, with little difference between the R (active) isomer and the S isomer.

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
There is currently no information regarding the use of Fenoldopam during lactation. The manufacturer recommends avoiding breastfeeding while taking Fenoldopam; however, due to its low oral bioavailability and short half-life, Fenoldopam in breast milk is unlikely to have adverse effects on breastfed infants. Furthermore, Fenoldopam can be administered intravenously to infants. Unlike dopamine, it does not lower serum prolactin levels and therefore may not interfere with breastfeeding.
◉ Effects on Breastfed Infants
No published information was found as of the revision date.
◉ Effects on Lactation and Breast Milk
No published information was found regarding lactating mothers as of the revision date. Unlike dopamine, Fenoldopam infusion does not affect serum prolactin levels in normal women. For mothers who have established lactation, prolactin levels may not affect their ability to breastfeed.

[1]. Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells. J Pharmacol Exp Ther, 1991. 258(1): p. 193-8.

[2]. The pharmacology of fenoldopam. Am J Hypertens, 1990. 3(6 Pt 2): p. 116S-119S.

Fenoldopam is a benzodiazepine drug. It has dual effects as a dopaminergic antagonist, vasodilator, alpha-adrenergic agonist, dopamine agonist, and antihypertensive. Fenoldopam is a dopamine D1 receptor agonist used as an antihypertensive drug. It lowers blood pressure by dilating small arteries. Fenoldopam is a dopaminergic agonist. The mechanism of action of Fenoldopam is as a dopamine agonist. Fenoldopam is a benzodiazepine derivative with vasodilatory and antihypertensive properties. Fenoldopam is a dopamine (DA) receptor agonist that specifically binds to peripheral DA1 receptors and binds with moderate affinity to alpha2 adrenergic receptors. However, this drug has no significant affinity for DA2 receptors, other alpha-adrenergic receptors, beta-adrenergic receptors, muscarinic receptors, or serotonergic receptors. Receptor binding regulates ion transmembrane transport, thereby stimulating adenylate cyclase activity and prolactin release. This leads to vasodilation, increased renal blood flow, and consequently enhanced sodium excretion and diuresis, ultimately lowering diastolic blood pressure.
A dopamine D1 receptor agonist used as an antihypertensive drug. It lowers blood pressure by dilating arterioles.
See also: Fenodorpan mesylate (salt form).
Indications

For short-term (up to 48 hours) treatment of severe hypertension during hospitalization, particularly in cases requiring rapid but reversible emergency blood pressure reduction, including malignant hypertension with end-organ deterioration.
FDA Label
Mechanism of Action

Fenodorpan is a rapid-acting vasodilator. It is an agonist of the D1-like dopamine receptor and binds to the α2 adrenergic receptor with moderate affinity. It has no significant affinity for D2-like receptors, α1 and β-adrenergic receptors, 5HT1 and 5HT2 receptors, or muscarinic receptors. Fenoldopam is a racemic mixture in which the R-isomer is biologically active. The R-isomer has approximately 250 times higher affinity for D1-like receptors than the S-isomer. In non-clinical studies, Fenoldopam has no agonistic effect on presynaptic D2-like dopamine receptors, α or β-adrenergic receptors, or angiotensin-converting enzyme activity. Fenoldopam may increase plasma norepinephrine levels.

C16H16CLNO3

305.75614

305.081

67227-56-9

Fenoldopam mesylate; 67227-57-0; Fenoldopam hydrochloride; 181217-39-0

3341

Typically exists as solid at room temperature

1.4±0.1 g/cm3

522.6±50.0 °C at 760 mmHg

269.9±30.1 °C

0.0±1.4 mmHg at 25°C

1.656

1.72

4

4

1

21

348

0

OC1=C(O)C=C2C(C3=CC=C(O)C=C3)CNCCC2=C1Cl

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

9-chloro-5-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol

SKF 82526; Fenoldopam

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO: ~77 mg/mL (~251.8 mM)
Water: ~10 mg/mL

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)