| 中文名称: | 甲磺酸溴隐亭 | ||||
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| 英文名称: | Bromocriptine mesylate | ||||
| 别名: | 甲磺酸溴隐亭 (5'a)-2-Bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)ergotaman-3',6',18-trione mesylate | ||||
| CAS No: | 22260-51-1 | 分子式: | C33H44BrN5O8S | 分子量: | 750.7 |
| CAS No: | 22260-51-1 | ||||
| 分子式: | C33H44BrN5O8S | ||||
| 分子量: | 750.7 | ||||
| EINEC: | 244-881-1 | ||||
| EINEC: | 244-881-1 | ||||
基本信息
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产品编号： |
B10769 |
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产品名称： |
Bromocriptine mesylate |
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CAS: |
22260-51-1 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
750.70 |
-20℃ |
1个月 |
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化学名： |
(5'a)-2-Bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)ergotaman-3',6',18-trione mesylate |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
1.3321mL |
6.6605mL |
13.3209mL |
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5mM |
0.2664mL |
1.3321mL |
2.6642mL |
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10mM |
0.1332mL |
0.6660mL |
1.3321mL |
生物活性
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产品描述 |
一种有效的多巴胺D2/D3受体激动剂，结合多巴胺D2受体，pKi为 8.05±0.2。 |
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靶点 |
pKi:8.05±0.2(dopamine D2 receptor) |
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体外研究 |
Bromocriptine stimulates [35S]-GTPγS binding at D2 dopamine receptor expressed in CHO cells with pEC50 of 8.15±0.05.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±2μM) whereas it is poorly active towards inducible macrophage NOS (IC50>100μM).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 1.69μM. |
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体内研究 |
Bromocriptine mesylate (2mg/kg,i.p.) is administered for 7 days in groups of mice in forced swimming test (FST) and tail suspension test (TST).Bromocriptine 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 (200mg/kg,p.o.) as compared to MPE treatment alone.Bromocriptine treatment group shows a significant reduction of immobility time as compared to control.Bromocriptine administration after 7 days pretreatment with MPE (100 and 200mg/kg,p.o.) shows significant and dose dependent potentiation of anti-immobility action of MPE as compared to MPE treatment alone.Intracisternal administration of Bromocriptine decreases significantly the static mechanical allodynia (SMA) score compared to that of sham (saline-injected rats) and its effect lasted for 30 min.Intraperitoneal administration of Bromocriptine induces a significant,dose dependent (0.1mg and 1mg/kg) decrease in pain scores in CCI-IoN group when compared to sham and its effect lasted for 6h.The highest dose induces the highest score decrease (P<0.01).Bromocriptine effect lasts 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 lasts for 6h. |
推荐实验方法(仅供参考)
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激酶实验： |
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The [35S]-GTPγS binding assay is carried out.Cell membranes (25±75ug) are incubated in Buffer B containing 0.1mM dithiothreitol (DTT) and 1uM GDP and drugs in a volume of 0.9mL for 30 min at 30℃.This preincubation ensures that the agonists tested are at equilibrium when the [35S]-GTPγS (50±150 pM,final concentration) is added (in 100uL ofBuffer 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. |
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动物实验: |
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Mice Swiss mice (20-25g) 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 (0.1mg/kg,i.p.) and Bromocriptine mesylate (2mg/kg,i.p.) are administered for 7 days in groups of mice in Forced Swimming Test (FST) and Tail Suspension Test (TST).Imipramine (10mg/kg,p.o.) as a standard is administered in positive control groups for 7 days. Rats Adult male Sprague-Dawley rats (N=112,275-325g) are used.Two weeks after the 6-OHDA injection,the animals are briefly ( |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
