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

72.72

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

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。