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| Targets |
Quinagolide hydrochloride specifically targets the dopamine D2 receptor. It acts as a selective agonist at this receptor. By activating the D2 receptor on lactotroph cells in the pituitary gland, it inhibits the secretion of prolactin. This is its primary mechanism of action for the treatment of hyperprolactinemia. Its selectivity for the D2 receptor over other receptors contributes to its therapeutic profile.
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| ln Vitro |
In ectopic cell lines, quinaglidide hydrochloride (100 nM; 48 hours) decreases the expression of non-ergot dopamine receptor 2 (DRD2) mRNA [2]. Endocrine mesenchymal stromal cells' (E-MSC) ability to invade is inhibited by quinagolide hydrochloride (100 nM; 48 hours) [2]. Endothelial differentiation of E-MSCs is greatly reduced by quinagolide hydrochronide (100 nM; 24 hours) [2].
In vitro, Quinagolide hydrochloride is effective in inhibiting prolactin secretion by human pituitary tumor cells. As a D2 receptor agonist, it activates the receptor, leading to a decrease in prolactin production. Its activity has been demonstrated in cell-based assays using pituitary cells. The compound's potency and efficacy in inhibiting prolactin secretion have been characterized in these in vitro systems. |
| ln Vivo |
Quinagolide hydrochloride (0.03-0.6 mg/kg; subcutaneous injection, once daily for 2 months) can effectively inhibit tumor growth in the body [1].
In vivo, Quinagolide hydrochloride is used clinically to treat hyperprolactinemia. It is effective in inhibiting prolactin secretion, and a daily dose as low as 60 pg can achieve a pronounced and prolonged suppressive effect on serum prolactin and growth hormone secretion. Its clinical efficacy has been demonstrated in patients with hyperprolactinemia and prolactin-secreting pituitary tumors. |
| Enzyme Assay |
Cell-free assays for Quinagolide hydrochloride are not the primary method for characterizing its activity, as it is a receptor agonist. However, its affinity for the dopamine D2 receptor can be studied using radioligand binding assays. In this assay, membrane preparations from cells expressing the D2 receptor are incubated with a radiolabeled D2 antagonist (e.g., [3H]-spiperone) and varying concentrations of Quinagolide. The displacement of the radioligand is measured, and the inhibition constant (Ki) is calculated.
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: In situ and ectopic E-MSCs Tested Concentrations: 100 nM Incubation Duration: 24 hrs (hours) Experimental Results: Total AKT levels diminished in ectopic E-MSCs, AKT in situ and ectopic cell lines Phosphorylation is Dramatically diminished. In vitro cell-based assays for Quinagolide hydrochloride are performed to measure its functional activity at the D2 receptor. Cells expressing the D2 receptor are treated with the compound. The activation of the receptor leads to a decrease in intracellular cAMP levels, as the D2 receptor is Gi-coupled. The decrease in cAMP can be measured using a cAMP assay (e.g., a competitive ELISA). The EC50 for the inhibition of cAMP production is calculated from the dose-response curve. This assay confirms the compound's agonistic activity. |
| Animal Protocol |
Animal/Disease Models: Female Wistar-Furth rats bearing SMtTW tumors [1]
Doses: 0.03-0.6 mg/kg Route of Administration: subcutaneous injection; 0.03-0.6 mg/kg, one time/day for 2 months Experimental Results: vs. Plasma PRL levels in all animals tended to normalize and tumor size diminished compared with the control group at a dose of 0.3 mg/kg. The dose of 0.3 mg/kg demonstrated the greatest inhibitory effect on PRL secretion and tumor growth. In vivo animal experiments for Quinagolide hydrochloride are typically conducted to study its effects on prolactin secretion. In rodents, the compound can be administered, and the level of prolactin in the blood is measured. The reduction in serum prolactin levels is used as a pharmacodynamic marker of its activity. However, specific protocols for Quinagolide are not detailed in the available literature, as it is a clinically approved drug. |
| ADME/Pharmacokinetics |
Quinagolide hydrochloride is an orally active drug. As a clinically approved medication, its pharmacokinetic properties are well-characterized. It is absorbed after oral administration and has a half-life that allows for once-daily dosing. It is metabolized in the liver, and its elimination is primarily via the kidneys. The drug's PK profile has been established in humans during its development and clinical use. However, specific PK parameters are not detailed in the available summaries.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of use during lactation Quinagolite has not yet been approved for marketing by the U.S. Food and Drug Administration (FDA). It is a selective dopamine D2 receptor antagonist that lowers serum prolactin levels. Quinagolite is generally not used during lactation because it suppresses lactation. There is currently no published information on the use of quinagolite in lactating women. ◉ Effects on breastfed infants As of the revised date, no relevant published information has been found. ◉ Effects on lactation and breast milk A small preliminary study compared the effects of quinagolite (CV 205-502) with bromocriptine starting treatment on the first day postpartum for 21 days in mothers who did not wish to breastfeed. The results showed that serum prolactin levels returned to normal more quickly in the bromocriptine group, while more women in the quinagolite group experienced breast symptoms. The effects of suppressing lactation were similar in both groups. [1] Quinagolide hydrochloride's toxicity profile has been characterized in its clinical use. Common side effects are related to its dopaminergic activity and may include nausea, headache, dizziness, and fatigue. It can also cause orthostatic hypotension. In rare cases, it may cause psychiatric symptoms. As a non-ergot dopamine agonist, it has a lower risk of fibrotic complications compared to ergot-derived dopamine agonists. Its safety in pregnancy and lactation has been established. |
| References |
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| Additional Infomation |
See also: Quinagolide Hydrochloride (note moved to).
Quinagolide hydrochloride is a clinically approved drug marketed under the brand name Norprolac® for the treatment of hyperprolactinemia. It is a valuable therapeutic option for patients with elevated prolactin levels, including those with prolactin-secreting pituitary adenomas. Its non-ergot structure gives it a favorable safety profile compared to older ergot-derived dopamine agonists. It is available in oral tablet form. All information is for research reference and not for diagnostic or clinical use. |
| Molecular Formula |
C20H33N3O3S.HCL
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| Molecular Weight |
432.02026
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| Exact Mass |
431.201
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| CAS # |
94424-50-7
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| Related CAS # |
94424-50-7 (HCl);87056-78-8;
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| PubChem CID |
3086400
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| Appearance |
White to off-white solid powder
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| Boiling Point |
539.1ºC at 760 mmHg
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| Flash Point |
279.8ºC
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| LogP |
4.347
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
576
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CCCN1C[C@H](C[C@H]2[C@H]1CC3=C(C2)C(=CC=C3)O)NS(=O)(=O)N(CC)CC.Cl
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| InChi Key |
DVLKVIJLALMCBQ-MSSRUXLCSA-N
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| InChi Code |
InChI=1S/C20H33N3O3S.ClH/c1-4-10-22-14-17(21-27(25,26)23(5-2)6-3)11-16-12-18-15(13-19(16)22)8-7-9-20(18)24;/h7-9,16-17,19,21,24H,4-6,10-14H2,1-3H3;1H/t16-,17+,19-;/m1./s1
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| Chemical Name |
(3S,4aS,10aR)-3-(diethylsulfamoylamino)-6-hydroxy-1-propyl-3,4,4a,5,10,10a-hexahydro-2H-benzo[g]quinoline;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~3.85 mg/mL (~8.91 mM)
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| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3147 mL | 11.5735 mL | 23.1471 mL | |
| 5 mM | 0.4629 mL | 2.3147 mL | 4.6294 mL | |
| 10 mM | 0.2315 mL | 1.1574 mL | 2.3147 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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