Referencia número: HY-12705

Bromocriptine

(Synonyms: CB-154 free base)

20 Cited Publications

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Based on 20 publication(s) in Google Scholar

Bromocriptine is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pK_i of 8.05±0.2.

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Pureza: 98.38%
No. CAS: 25614-03-3
Fòrmula: C₃₂H₄₀BrN₅O₅
Peso molecular:654.59

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Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Bromocriptine Chemical Structure

No. CAS: 25614-03-3

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (20)
Protocolo
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Bromocriptine is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pK_i of 8.05±0.2.

IC₅₀ & Target

pKi: 8.05±0.2 (dopamine D2 receptor)^[1]

Ver todos los productos específicos de isoformas Dopamine Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
Vero	CC₅₀	>40 μM Compound: 34	Cytotoxicity against African green monkey Vero cells by MTT assay Cytotoxicity against African green monkey Vero cells by MTT assay	[PMID: 31549836]
Vero	EC₅₀	0.8 μM Compound: 124	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	[PMID: 31128447]
Vero	EC₅₀	0.8 μM Compound: 124	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	[PMID: 31128447]
Vero	EC₅₀	0.8 μM Compound: 124	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	[PMID: 31128447]
Vero	EC₅₀	1.6 μM Compound: 124	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	[PMID: 31128447]
Vero	EC₅₀	13.04 μM Compound: 34	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	[PMID: 31549836]

In Vitro

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.

In Vivo

Bromocriptine (a dopamine agonist) treatment (2 mg/kg, i.p.) group shows significant anti-immobility action as compared to control. When Bromocriptine administered 30 min after the last dose of 7 days MPE treatment and subjected to FST, this dopaminergic agonist produces significant and dose dependent potentiation of anti-immobility action of MPE (200 mg/kg, p.o.) as compared to MPE treatment alone. Bromocriptine (a dopamine agonist) treatment (2 mg/kg, i.p.) group shows a significant reduction of immobility time as compared to control. Bromocriptine administration after 7 days pretreatment with MPE (100 and 200 mg/kg, p.o.) shows significant and dose dependent potentiation of anti-immobility action of MPE as compared to MPE treatment alone^[4]. Intraperitoneal administration of Bromocriptine induces a significant, dose dependent (0.1 mg and 1 mg/Kg) decrease in pain scores in CCI-IoN group when compared to sham and its effect lasted for 6 h. The highest dose induces the highest score decrease, (P<0.01). As a positive control SKF8129 (DR1 agonist) is used. Its intraperitoneal administration induces a non-significant increase in the SMA score when compared to sham (saline-injected). Intracisternal administration of Bromocriptine decreases significantly the SMA score when compared to sham (saline-injected). Bromocriptine effect lasted for 20 min. Intraperitoneal administration of Bromocriptine induces a significant dose dependent decrease in SMA score in CCI-IoN + 6-OHDA lesioned group compared to that of sham. Its effect lasted for 6 h. SKF81297 administration increases the allodynic score. Intracisternal administration of Bromocriptine decreases significantly the SMA score compared to that of sham (saline-injected rats) and its effect lasted for 30 min^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

No. CAS 25614-03-3
Appearance Solid
Peso molecular 654.59
Fòrmula C₃₂H₄₀BrN₅O₅
Color White to off-white
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
Synonyms

CB-154 free base
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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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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.
Sci Adv

Implantable system for chronotherapy. [Abstract]

2021 Nov 26;7(48):eabj4624. PMID: 34826238
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.
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.
Mol Pharm

Machine Learning Models Identify New Inhibitors for Human OATP1B1. [Abstract]

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
Aquaculture

2025 Apr 15.
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
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
Eur J Integr Med

2021, 101322.
Pharmacogn Mag

2023 Oct 12.
bioRxiv

2025 Oct 13.

Protocolo

Kinase Assay^[1]

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.

Animal Administration^[4]^[5]

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.

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (281 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

Bromocriptine

20 Cited Publications

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Bromocriptine

Publications Citing Use of MedChemExpress (MCE) Bromocriptine

Ver todos los productos específicos de isoformas Dopamine Receptor

Actividad biológica

Chemical Information

Publications (20)

Protocolo

Pureza y Documentación

Referencias

Calculators

Help & FAQs

Bromocriptine Related Classifications

HY-12705 Related Classifications