Bromocriptine (Synonyms: CB-154 free base)

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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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CAS No. : 25614-03-3

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Other In-stock Forms of Bromocriptine:

Bromocriptine mesylate

Other Forms of Bromocriptine:

Bromocriptine mesylate In-stock
Bromocriptine-¹³C,d₃ Get quote

19 Publications Citing Use of MCE Bromocriptine

Cell Proliferation/Viability Assay

RT-PCR

Others

: 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.

: 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.

: 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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Biological Activity
Protocol
Purity & Documentation
References
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Description

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]

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 wash out and subsequent virus addition along with compound and measured after 6 days by inverted light microscopy 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 wash out and subsequent virus addition along with compound and measured after 6 days by inverted light microscopy	[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.

Molecular Weight

654.59

Formula

C₃₂H₄₀BrN₅O₅

CAS No.

25614-03-3

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

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]. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Bromocriptine Related Classifications

Neurological Disease

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Bromocriptine25614-03-3CB-154CB154CB 154Dopamine ReceptorInhibitorinhibitorinhibit

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