Bromocriptine
Based on 20 publication(s) in Google Scholar
Bromocriptine is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pKi of 8.05±0.2.
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- 純度: 98.38%
- CAS 番号: 25614-03-3
- 分子式: C32H40BrN5O5
- 分子量:654.59
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Bromocriptine
More- Nat Commun. 2020 Feb 18;11(1):941. [Abstract]
- Sci Adv. 2021 Nov 26;7(48):eabj4624. [Abstract]
- Phytomedicine. 2025 Jun:141:156707. [Abstract]
- Int J Biol Macromol. 2026 Jan;340(Pt 1):150002. [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]
- Eur J Pharmacol. 2023 Jan 5:938:175443. [Abstract]
- Int J Mol Sci. 2024 Nov 21;25(23):12483. [Abstract]
- Mol Pharm. 2022 Nov 7;19(11):4320-4332. [Abstract]
- Neuropharmacology. 2026 Nov 1:298:111068. [Abstract]
- Aquaculture. 2025 Apr 15.
- Clin Immunol. 2025 Dec:281:110604. [Abstract]
- J Endocrinol Invest. 2025 Jan;48(1):67-80. [Abstract]
- BMC Endocr Disord. 2021 Nov 23;21(1):235. [Abstract]
- Toxicol Appl Pharmacol. 2024 Apr:485:116876. [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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Dopamine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
pKi: 8.05±0.2 (dopamine D2 receptor)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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 |
0.8 μM
Compound: 124
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Antiviral activity against DENV2 16681 infected in African green monkey Vero cells after 3 days by focus reduction assay
Antiviral activity against DENV2 16681 infected in African green monkey Vero cells after 3 days by focus reduction assay
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[PMID: 31128447] |
| Vero | EC50 |
0.8 μM
Compound: 124
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Antiviral activity against DENV3 00-40 infected in African green monkey Vero cells after 3 days by focus reduction assay
Antiviral activity against DENV3 00-40 infected in African green monkey Vero cells after 3 days by focus reduction assay
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[PMID: 31128447] |
| Vero | EC50 |
0.8 μM
Compound: 124
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Antiviral activity against DENV4 09-48 infected in African green monkey Vero cells after 3 days by focus reduction assay
Antiviral activity against DENV4 09-48 infected in African green monkey Vero cells after 3 days by focus reduction assay
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[PMID: 31128447] |
| Vero | EC50 |
1.6 μM
Compound: 124
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Antiviral activity against DENV1 02-20 infected in African green monkey Vero cells after 3 days by focus reduction assay
Antiviral activity against DENV1 02-20 infected in African green monkey Vero cells after 3 days by focus reduction assay
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[PMID: 31128447] |
| 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.
化学情報
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CAS 番号 25614-03-3
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性状 Solid
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分子量 654.59
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分子式 C32H40BrN5O5
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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
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別名
CB-154 free base
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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 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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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 -
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 -
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 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 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 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 -
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 -
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 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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Mol Pharm
2022 Nov 7;19(11):4320-4332. PMID: 36269563 -
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 -
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Clin Immunol
Glial-derived neurotrophic factor promotes aberrant basal cell hyperplasia in nasal polyps. [Abstract]2025 Dec: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 -
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 -
Toxicol Appl Pharmacol
Mechanisms of adverse mammary effect induced by olanzapine and therapeutic interventions in rat model. [Abstract]2024 Apr:485:116876. PMID: 38437955 -
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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プロトコル
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.
純度とドキュメンテーション
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データシート (281 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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取扱説明書 (2659 KB)
参考文献
[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]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Bromocriptine 関連分類
HY-12705 関連分類
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