Bromocriptine mesylate
Based on 20 publication(s) in Google Scholar
Bromocriptine mesylate is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pKi of 8.05. Bromocriptine mesylate is permeable to the blood-brain barrier.
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- Pureté: 99.53%
- CAS No.: 22260-51-1
- Formule: C33H44BrN5O8S
- Masse moléculaire:750.70
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Stockage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Bromocriptine mesylate
More- Nat Commun. 2020 Feb 18;11(1):941. [Abstract]
- Sci Adv. 2021 Nov 26;7(48):eabj4624. [Abstract]
- Int J Biol Macromol. 2026 Jan;340(Pt 1):150002. [Abstract]
- Phytomedicine. 2025 Jun:141:156707. [Abstract]
- Br J Pharmacol. 2021 Sep;178(17):3570-3586. [Abstract]
- Antioxid Redox Signal. 2025 Jun;42(16-18):954-972. [Abstract]
- J Ethnopharmacol. 2021 Jun 12:273:113994. [Abstract]
- Int J Mol Sci. 2024 Nov 21;25(23):12483. [Abstract]
- Eur J Pharmacol. 2023 Jan 5:938:175443. [Abstract]
- Neuropharmacology. 2026 Nov 1:298:111068. [Abstract]
- Mol Pharm. 2022 Nov 7;19(11):4320-4332. [Abstract]
- Aquaculture. 2025 Apr 15.
- Clin Immunol. 2025 Oct 14:281:110604. [Abstract]
- J Endocrinol Invest. 2025 Jan;48(1):67-80. [Abstract]
- Toxicol Appl Pharmacol. 2024 Apr:485:116876. [Abstract]
- BMC Endocr Disord. 2021 Nov 23;21(1):235. [Abstract]
- J Biomol Struct Dyn. 2022;40(23):12800-12811. [Abstract]
- Eur J Integr Med. 2021, 101322.
- Pharmacogn Mag. 2023 Oct 12.
- bioRxiv. 2025 Oct 13.
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Voir tous les produits spécifiques à Isoform Dopamine Receptor
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Activité biologique
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D2 Receptor |
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Cell Line
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Type | Value | Description | References |
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| Vero | CC50 |
>40 μM
Compound: 34
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Cytotoxicity against African green monkey Vero cells by MTT assay
Cytotoxicity against African green monkey Vero cells by MTT assay
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[PMID: 31549836] |
| Vero | EC50 |
13.04 μM
Compound: 34
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Inhibition of NS2B-NS3 protease in Zika virus Puerto Rico/PRVABC5 infected in African green monkey Vero cells assessed as antiviral activity by measuring reduction in virus-induced cytopathic effect preincubated with cells for 2 hrs followed by compound w
Inhibition of NS2B-NS3 protease in Zika virus Puerto Rico/PRVABC5 infected in African green monkey Vero cells assessed as antiviral activity by measuring reduction in virus-induced cytopathic effect preincubated with cells for 2 hrs followed by compound w
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[PMID: 31549836] |
Bromocriptine stimulates [35S]-GTPγS binding at D2 dopamine receptor expressed in CHO cells with pEC50 of 8.15±0.05[1]. Bromocriptine also is a strong inhibitor of brain nitric oxide synthase. The ergot alkaloid Bromocriptine (BKT) is found to act as a strong inhibitor of purified neuronal nitric oxide synthase (NOS) (IC50=10±2 μM) whereas it is poorly active towards inducible macrophage NOS (IC50>100 μM) [2]. Bromocriptine is found to inhibit the activity of at least one human cytochrome P450 enzyme. Bromocriptine is a potent inhibitor of CYP3A4 with a calculated IC50 value for the interaction of 1.69 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 22260-51-1
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Appearance Solid
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Masse moléculaire 750.70
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Formule C33H44BrN5O8S
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Color White to off-white
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SMILES
[H][C@@]12CC3=C(Br)NC4=CC=CC(C1=C[C@@H](C(N[C@@]5(C(C)C)C(N6[C@@H](CC(C)C)C(N7CCC[C@]7([C@]6(O)O5)[H])=O)=O)=O)CN2C)=C43.OS(=O)(C)=O
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Synonyms
CB-154
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)
Publications (20)
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Journal Impact Factor
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Most Recent
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Nat Commun
Pyridoxine induces glutathione synthesis via PKM2-mediated Nrf2 transactivation and confers neuroprotection. [Abstract]2020 Feb 18;11(1):941. PMID: 32071304
Bromocriptine mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Feb 18;11(1):941. [Abstract]
GSH levels in astrocytes from wild-type mice or Drd2-knockout mice after quinpirole (10 μM), quinelorane (20 μM), or Bromocriptine mesylate (40 μM) treatment for 12 h.
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Int J Biol Macromol
Effect and mechanism of maternal prolactin levels on depressive-like behavior in prenatally stressed offspring. [Abstract]2026 Jan;340(Pt 1):150002. PMID: 41485664 -
Phytomedicine
Valproic acid promotes transcriptional activation of Drd2 by mediating histone acetylation to inhibit the mTOR-Pttg1 signaling axis and exerts anti-PitNETs activity. [Abstract]2025 Jun:141:156707. PMID: 40220407 -
Br J Pharmacol
Exploiting D2 receptor β-arrestin2-biased signalling to suppress tumour growth of pituitary adenomas. [Abstract]2021 Sep;178(17):3570-3586. PMID: 33904172
Bromocriptine mesylate purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2021 Sep;178(17):3570-3586. [Abstract]
The cell viability of rat pituitary tumor cells (MMQ) pretreated with pertussis toxin for 2 hours and then stimulated with different doses of Bromocriptine mesylate (BRC) for 48 hours was evaluated.
Bromocriptine mesylate purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2021 Sep;178(17):3570-3586. [Abstract]
After siRNA transfection, MMQ cells were treated with Bromocriptine mesylate (BRC: 20 μM) for 24 h. Cleaved-caspase3 (c-CASP3) from cell extracts were analysed by immunoblotting.
Bromocriptine mesylate purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2021 Sep;178(17):3570-3586. [Abstract]
After treatment with Bromocriptine mesylate (BRC) or UNC9994 for 24 hours, ROS levels in MMQ and GH3 cells were measured.
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Antioxid Redox Signal
Androgen Receptor Mediates Dopamine Agonist Resistance by Regulating Intracellular Reactive Oxygen Species in Prolactin-Secreting Pituitary Adenoma. [Abstract]2025 Jun;42(16-18):954-972. PMID: 39360800 -
J Ethnopharmacol
Total barley maiya alkaloids inhibit prolactin secretion by acting on dopamine D2 receptor and protein kinase A targets. [Abstract]2021 Jun 12:273:113994. PMID: 33711439 -
Int J Mol Sci
The Activation of p300 Enhances the Sensitivity of Pituitary Adenomas to Dopamine Agonist Treatment by Regulating the Transcription of DRD2. [Abstract]2024 Nov 21;25(23):12483. PMID: 39684198
Bromocriptine mesylate purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Nov 21;25(23):12483. [Abstract]
q-PCR analysis of p300 expression after treating MMQ and AtT-20 cells with Bromocriptine mesylate (BRC: 0, 5, 10 μM) for 24 hours.
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Eur J Pharmacol
Dopamine D2 receptor agonist Bromocriptine ameliorates Aβ1-42-induced memory deficits and neuroinflammation in mice. [Abstract]2023 Jan 5:938:175443. PMID: 36470446 -
Neuropharmacology
Acute restraint stress exacerbates compulsive grooming in male Sapap3 knockout mice: Critical role of nucleus accumbens D2 receptors. [Abstract]2026 Nov 1:298:111068. PMID: 42250868 -
Mol Pharm
2022 Nov 7;19(11):4320-4332. PMID: 36269563 -
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Clin Immunol
Glial-derived neurotrophic factor promotes aberrant basal cell hyperplasia in nasal polyps. [Abstract]2025 Oct 14:281:110604. PMID: 41075855 -
J Endocrinol Invest
Bromocriptine sensitivity in bromocriptine-induced drug-resistant prolactinomas is restored by inhibiting FGF19/FGFR4/PRL. [Abstract]2025 Jan;48(1):67-80. PMID: 38926262 -
Toxicol Appl Pharmacol
Mechanisms of adverse mammary effect induced by olanzapine and therapeutic interventions in rat model. [Abstract]2024 Apr:485:116876. PMID: 38437955 -
BMC Endocr Disord
The role of MAPK11/12/13/14 (p38 MAPK) protein in dopamine agonist-resistant prolactinomas. [Abstract]2021 Nov 23;21(1):235. PMID: 34814904 -
J Biomol Struct Dyn
In silico and in vitro assays reveal potential inhibitors against 3CL pro main protease of SARS-CoV-2. [Abstract]2022;40(23):12800-12811. PMID: 34550861 -
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Solvant et solubilité
DMSO : 175 mg/mL (233.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1.1 mg/mL (1.47 mM; ultrasonic and adjust pH to 3 with HCl)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (2.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (2.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
The [35S]-GTPγS binding assay is carried out. Cell membranes (25 ±75 ug) are incubated in Buffer B containing 0.1 mM dithiothreitol (DTT) and 1 uM GDP and drugs in a volume of 0.9 mL for 30 min at 30°C. This preincubation ensures that the agonists tested are at equilibrium when the [35S]-GTPγS (50±150 pM, final concentration) is added (in 100 uL of Buffer B) to initiate the reaction. The assay mixture is incubated for a further 20 min unless otherwise stated. The assays are terminated by rapid filtration and bound radio-activity determined as described for the radio-ligand binding assays above. The total binding of [35S]-GTPγS is less than 20% of that added[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[4]
Swiss mice (20-25 g) of either sex (total 150) are used. Bromocriptine mesylate is used as dopamine receptor (D2) agonist. Haloperidol is diluted in distilled water which is used for a vehicle of injection. Bromocriptine mesylate is dissolved in one drop of glacial acetic acid and made up to volume in distilled water. Imipramine is dissolved in 0.9% normal saline. Haloperidol (0.1 mg/kg, i.p.) and Bromocriptine mesylate (2 mg/kg, i.p.) are administered for 7 days in groups of mice in Forced Swimming Test (FST) and Tail Suspension Test (TST). Imipramine (10 mg/kg, p.o.) as a standard is administered in positive control groups for 7 days.
Rats[5]
Adult male Sprague-Dawley rats (N=112, 275-325 g) are used. Two weeks after the 6-OHDA injection, the animals are briefly (<3 min) anesthetized with 2 % halothane using a mask and received for intracisternal administration Bromocriptine (7 μg/kg dissolved in 5 μL vehicle) or the vehicle alone (5 μL of 0.9 % saline). For i.p. injection we used Bromocriptine (1 mg/kg) and SKF81297 (3 mg/kg dissolved in 0.9 % saline) concentrations. Following a recovery period (<2 min), the rats are placed in the observation field for 40 min period-test by a blind-experimenter.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (282 KB)
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SDS (399 KB)
- English - EN (399 KB)
- Français - FR (399 KB)
- Deutsch - DE (399 KB)
- Norwegian - NO (399 KB)
- Español - ES (399 KB)
- Swedish - SV (399 KB)
- Italian - IT (399 KB)
- Korean - KR (399 KB)
- Portuguese - PT (399 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Gardner B, et al. Agonist action at D2(long) dopamine receptors: ligand binding and functional assays. Br J Pharmacol. 1998 Jul;124(5):978-84. [Content Brief]
[2]. Renodon A, et al. Bromocriptine is a strong inhibitor of brain nitric oxide synthase: possible consequences for the origin of its therapeutic effects.FEBS Lett. 1997 Apr 7;406(1-2):33-6. [Content Brief]
[3]. Wynalda MA, et al. Assessment of potential interactions between dopamine receptor agonists and various human cytochrome P450 enzymes using a simple in vitro inhibition screen. Drug Metab Dispos. 1997 Oct;25(10):1211-4. [Content Brief]
[4]. Rana DG, et al. Dopamine mediated antidepressant effect of Mucuna pruriens seeds in various experimental models of depression. Ayu. 2014 Jan;35(1):90-7. [Content Brief]
[5]. Dieb W, et al. Nigrostriatal dopaminergic depletion increases static orofacial allodynia. J Headache Pain. 2016;17:11. [Content Brief]
[6]. Friis ML, et al. Transfer of bromocriptine across the blood-brain barrier in man. Acta Neurol Scand. 1979 Mar;59(2-3):88-95. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.3321 mL | 6.6605 mL | 13.3209 mL | 33.3023 mL |
| DMSO | 5 mM | 0.2664 mL | 1.3321 mL | 2.6642 mL | 6.6605 mL |
| 10 mM | 0.1332 mL | 0.6660 mL | 1.3321 mL | 3.3302 mL | |
| 15 mM | 0.0888 mL | 0.4440 mL | 0.8881 mL | 2.2202 mL | |
| 20 mM | 0.0666 mL | 0.3330 mL | 0.6660 mL | 1.6651 mL | |
| 25 mM | 0.0533 mL | 0.2664 mL | 0.5328 mL | 1.3321 mL | |
| 30 mM | 0.0444 mL | 0.2220 mL | 0.4440 mL | 1.1101 mL | |
| 40 mM | 0.0333 mL | 0.1665 mL | 0.3330 mL | 0.8326 mL | |
| 50 mM | 0.0266 mL | 0.1332 mL | 0.2664 mL | 0.6660 mL | |
| 60 mM | 0.0222 mL | 0.1110 mL | 0.2220 mL | 0.5550 mL | |
| 80 mM | 0.0167 mL | 0.0833 mL | 0.1665 mL | 0.4163 mL | |
| 100 mM | 0.0133 mL | 0.0666 mL | 0.1332 mL | 0.3330 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Bromocriptine mesylate Related Classifications
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