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5mg | ||
10mg | ||
25mg | ||
50mg | ||
100mg |
Purity: ≥98%
Bromocriptine (Parlodel) is a semisynthetic ergotamine alkaloid that acts as a dopamine D2 agonist. It suppresses prolactin secretion. It is used in the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes.
ln Vitro |
In CHO cells, bromocriptine increases the expression of D2 dopamine receptors, which then bind to [35S]-GTPγS with a pEC50 of 8.15±0.05[1]. Another potent inhibitor of brain nitric oxide synthase is bromocriptine. It was shown that the ergot alkaloid bromocriptine (BKT) had weak effect against inducible macrophage NOS (IC50>100 μM), but it was a potent inhibitor of pure neuronal nitric oxide synthase (NOS) (IC50=10±2 μM) [2]. It has been discovered that at least one human cytochrome P450 enzyme is inhibited by bromocriptine. Strong CYP3A4 inhibitor bromocriptine has an interaction IC50 value of 1.69 μM [3].
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ln Vivo |
When compared to the control group, the group administered with 2 mg/kg intraperitoneal injections of bromocriptine, a dopamine agonist, demonstrated a noteworthy anti-immobility effect. When bromocriptine was given 30 minutes after the last dose of the 7-day MPE therapy and an FST was conducted, the anti-immobility effects of this dopaminergic agonist on MPE (200 mg/kg, orally) were shown to be significantly and dose-dependently enhanced when compared with MPE treatment alone. When compared to the control group, the group treated with 2 mg/kg of the dopamine agonist bromocriptine intraperitoneally (i.p.) exhibited a substantial decrease in immobility time. When bromocriptine (100 and 200 mg/kg, po) was administered following 7 days of pretreatment with MPE, the anti-immobility effect of MPE was significantly and dose-dependently enhanced when compared to MPE treatment alone [4]. When bromocriptine was administered intraperitoneally, the CCI-IoN group saw a significant, dose-dependent (0.1 mg and 1 mg/Kg) reduction in pain scores when compared to the sham group. This effect persisted for six hours. Scores decreased most when the highest dose was applied (P<0.01). The DR1 agonist SKF8129 was employed as a positive control. Comparing intraperitoneal delivery to sham surgery (saline injection), there was a nonsignificant rise in SMA scores. When bromocriptine was administered intracervically, the SMA scores were much lower than when saline injection was used as a sham procedure. Bromocriptine has a 20-minute half-life. as bromocriptine was administered intraperitoneally, the SMA scores of the CCI-IoN α + α 6-OHDA damage group significantly decreased in a dose-dependent manner as compared to the sham group. Six hours pass during its impact. Administration of SKF81297 resulted in higher allodynia scores. When compared to sham surgery (rats injected with normal saline), intraacisternal infusion of bromocriptine dramatically reduced SMA scores, and its effects lasted for 30 minutes [5].
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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.
[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. [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. [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. [5]. Dieb W, et al. Nigrostriatal dopaminergic depletion increases static orofacial allodynia. J Headache Pain. 2016;17:11 |
Molecular Formula |
C32H40BRN5O5
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Molecular Weight |
654.606
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Exact Mass |
653.2213
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CAS # |
25614-03-3
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Related CAS # |
Bromocriptine mesylate;22260-51-1
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
[H][C@@]12CC3=C(Br)NC4=C3C(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)=CC=C4
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InChi Key |
OZVBMTJYIDMWIL-AYFBDAFISA-N
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InChi Code |
InChI=1S/C32H40BrN5O5/c1-16(2)12-24-29(40)37-11-7-10-25(37)32(42)38(24)30(41)31(43-32,17(3)4)35-28(39)18-13-20-19-8-6-9-22-26(19)21(27(33)34-22)14-23(20)36(5)15-18/h6,8-9,13,16-18,23-25,34,42H,7,10-12,14-15H2,1-5H3,(H,35,39)/t18-,23-,24+,25+,31-,32+/m1/s1
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Chemical Name |
Ergotaman-3',6',18-trione, 2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)-, (5'alpha)-
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Synonyms |
CB154 CB 154 Bromocriptine CB-154
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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 |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.5276 mL | 7.6381 mL | 15.2763 mL | |
5 mM | 0.3055 mL | 1.5276 mL | 3.0553 mL | |
10 mM | 0.1528 mL | 0.7638 mL | 1.5276 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.