中文名 | 甲磺酸溴隐亭 |
英文名 | 2-bromo-alpha-ergocryptine methane-sulfonate |
别名 | 甲磺酸溴隐亭 甲黄酸溴麦角环肽 甲磺酸溴隐亭 EP标准品 甲磺酸溴隐亭 USP标准品 2-溴-Α-麦角隐亭甲磺酸盐 2-溴-alpha-麦角环肽甲磺酸盐 (6AR,9R)-5-溴-N-((2R,5S,10AS,10BS)-10B-羟基-5-异丁基-2-异丙基-3,6-二氧八氢-2H-恶唑[3,2-A]吡咯并[2,1-C]吡嗪-2-基)-7-甲基-4,6,6A,7,8,9-六氢吲哚并[4,3-FG]喹啉-9-甲酰胺甲磺酸盐 |
英文别名 | BRC BCT Bromocriptine Mesylate BROMOCRIPTINE MESYLATE (+)-BROMOCRIPTINE MESYLATE BROMOCRIPTINE METHANESULPHONATE (+)-BROMOCRIPTINE METHANESULFONATE 2-bromo-alpha-ergocryptine methane-sulfonate BROMOCRYPTINE MESYLATE METHANESULFONATE SALT 2-bromo-A-ergocryptine methanesulfonate salt (5'A)-2-BROMO-12'-HYDROXY-2'-(1-METHYLETHYL)-5'-(2-METHYLPROPYL)ERGOTAMAN-3',6',18-TRIONE MESYLATE (8xi,12'xi)-2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)-3',6',18-trioxoergotaman methanesulfonate (salt) (5xi,5'alpha)-2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)-3',6',18-trioxoergotaman methanesulfonate (salt) |
CAS | 22260-51-1 |
EINECS | 244-881-1 |
化学式 | C33H44BrN5O8S |
分子量 | 750.7 |
InChI | InChI=1/C32H40BrN5O5.CH4O3S/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;1-5(2,3)4/h6,8-9,13,16-18,23-25,34,42H,7,10-12,14-15H2,1-5H3,(H,35,39);1H3,(H,2,3,4)/t18?,23-,24?,25+,31-,32?;/m1./s1 |
InChIKey | NOJMTMIRQRDZMT-JGYCFGIMSA-N |
熔点 | 192-196° (dec) |
沸点 | 992.4°C at 760 mmHg |
比旋光度 | D20 +95° (c = 1 in methanol-methylene chloride) |
闪点 | 554°C |
蒸汽压 | 0mmHg at 25°C |
溶解度 | H2O: 0.8mg/ml |
酸度系数 | 4.90(at 25℃) |
存储条件 | 2-8°C |
稳定性 | 从提供的购买之日起稳定2年。DMSO或乙醇中的溶液可在-20 °C下储存长达3个月 |
外观 | 固体 |
颜色 | white |
Merck | 13,1400 |
BRN | 4115238 |
体外研究 | 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. |
体内研究 | 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. |
危险品标志 | Xn - 有害物品 |
风险术语 | 20/21/22 - 吸入、皮肤接触及吞食有害。 |
安全术语 | S22 - 切勿吸入粉尘。 S24/25 - 避免与皮肤和眼睛接触。 S36 - 穿戴适当的防护服。 |
危险品运输编号 | UN 3077 9 / PGIII |
WGK Germany | 3 |
RTECS | KE1595000 |
FLUKA BRAND F CODES | 3-10 |
海关编号 | 29396900 |
上游原料 | 麦角克碱 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.332 ml | 6.66 ml | 13.321 ml |
5 mM | 0.266 ml | 1.332 ml | 2.664 ml |
10 mM | 0.133 ml | 0.666 ml | 1.332 ml |
5 mM | 0.027 ml | 0.133 ml | 0.266 ml |
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