22260-51-1
基本信息
甲磺酸溴隐亭
甲黄酸溴麦角环肽
(+)-2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)ergotaman-3',6'-18-trione methanesulfonate salt
2-BROMO-12'-HYDROXY-2'-(1-METHYLETHYL)-5'-(2-METHYL-PROPYL)ERGOTAMAN-3',6',18-TRIONE-METHANESULFONATE
2-BROMO-ALPHA-ERGOCRYPTINE METHANESULFONATE
2-BROMO-ALPHA-ERGOCRYPTINE METHANESULFONATE SALT
2-BROMOERGOCRYPTINE MONOMETHANESULFONATE SALT
(5'A)-2-BROMO-12'-HYDROXY-2'-(1-METHYLETHYL)-5'-(2-METHYLPROPYL)ERGOTAMAN-3',6',18-TRIONE MESYLATE
BCT
BRC
(+)-BROMOCRIPTINE MESYLATE
BROMOCRIPTINE MESYLATE
(+)-BROMOCRIPTINE METHANESULFONATE
BROMOCRIPTINE METHANESULPHONATE
BROMOCRYPTINE MESYLATE METHANESULFONATE SALT
2-bromo-alpha-ergocryptinemesylate
2-bromo-alpha-ergocryptinmethanesulfonate
2-bromo-alpha-ergokryptine-mesilate
bromocriptinemesilate
bromocryptinemethanesulfonate
cb-154
物理化学性质
| 熔点 | 192-196° (dec) |
| 比旋光度 | D20 +95° (c = 1 in methanol-methylene chloride) |
| 储存条件 | 2-8°C |
| 储存条件 | 2-8°C |
| 溶解度 | H2O: 0.8 mg/mL |
| 溶解度 | H2O：0.8 mg/mL |
| 酸度系数(pKa) | 4.90(at 25℃) |
| 形态 | solid |
| 颜色 | white |
| 旋光性 (optical activity) | [α]20/D +95°, c = 1 in methanol: methylene chloride (1:1)(lit.) |
| Merck | 13,1400 |
| BRN | 4115238 |
| 稳定性 | 从购买之日起 2 年内保持稳定。 DMSO 或乙醇溶液可在 -20°C 下保存长达 3 个月 |
| InChIKey | NOJMTMIRQRDZMT-JGYCFGIMSA-N |
| CAS 数据库 | 22260-51-1(CAS DataBase Reference) |
安全数据
| 危险性符号(GHS) |   GHS07,GHS09 |
| 警示词 | 警告 |
| 危险性描述 | H302-H410 |
| 防范说明 | P273-P301+P312+P330 |
| 危险品标志 | Xn |
| 危险类别码 | 20/21/22 |
| 安全说明 | 22-24/25-36 |
| 安全说明 | S22-S24/25 |
| 危险品运输编号 | UN 3077 9 / PGIII |
| WGK Germany | 3 |
| WGK Germany | 3 |
| RTECS号 | KE1595000 |
| F | 3-10 |
| 海关编码 | 29396900 |
| 毒性 | LD50 in mice, rats, rabbits (mg/kg): 190, 72, 12.5 i.v. (Parkes) |
22260-51-1(安全特性,毒性,储运)
常见问题列表
1）溴隐亭的合成
将α-麦角隐亭12g（20.8mmoL）和二氯甲烷120mL加入反应瓶中，搅拌溶清后依次加入5，5-二溴巴比妥酸3.69g（12.9mmoL）、33％氢溴酸的冰乙酸溶液0.2mL，控温25～30℃反应5～6h，过滤，滤液依次用1moL／L的硫代硫酸钠（30mL），5％的碳酸氢钠溶液（30mL），20％氯化钠溶液（30mL）洗涤。有机相用无水硫酸镁干燥，过滤，并加入硅胶36g浓缩将溶剂完全拉干。柱层析：流动相先为二氯甲烷，后为V（二氯甲烷）∶V（丙酮）＝6∶1的混合溶液。得10.6g溴隐亭，收率７8％。
2）甲磺酸溴隐亭的合成
将溴隐亭6.0g用二氯甲烷120mL溶清后加入2-丁酮200mL，控制内温20～30℃，加入甲磺酸1.14g，生成结晶型沉淀，搅拌1h。滤出固体，用2-丁酮30mL洗涤，干燥得6.13g甲磺酸溴隐亭，收率86％。
pKi: 8.05±0.2 (dopamine D2 receptor)
Bromocriptine stimulates [ 35 S]-GTPγS binding at D2 dopamine receptor expressed in CHO cells with pEC 50 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) (IC 50 =10±2 μM) whereas it is poorly active towards inducible macrophage NOS (IC 50 >100 μM) . 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 IC 50 value for the interaction of 1.69 μM.
Bromocriptine mesylate (2 mg/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 (200 mg/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 200 mg/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 (0.1 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). 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 6 h.