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甲磺酸溴隐亭

甲磺酸溴隐亭用途

Bromocriptine mesylate 是一种有效的多巴胺 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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甲磺酸溴隐亭名称

[ CAS 号 ]:
22260-51-1

[ 中文名 ]:
甲磺酸溴隐亭

[ 英文名 ]:
CB-154 mesylate

[中文别名 ]:

[英文别名 ]:

Bromocriptine mesilate
CB-154 mesylate
Apo-Bromocriptine
2-Bromine-a-ergocryptine Methanesulfonate
Parlodel
2-Bromo α-Ergocryptine Mesylate
hydroindolo[4,3-fg]chinolin-9-carboxamid(1:1)
EINECS 244-881-1
MFCD00069218
Bromocriptine (mesylate)

甲磺酸溴隐亭生物活性

[ 描述 ]:

Bromocriptine mesylate 是一种有效的多巴胺 D2/D3 受体激动剂,结合多巴胺 D2 受体,pKi 为 8.05±0.2。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体

信号通路 >> 神经信号通路 >> 多巴胺受体

研究领域 >> 神经疾病

天然产物 >> 其他

[ 靶点 ]

pKi: 8.05±0.2 (dopamine D2 receptor)[1]

[体外研究]

Bromocriptine刺激[35S]-GTPγS与CHO细胞中表达的D2多巴胺受体结合,pEC50为8.15±0.05 [1]。 Bromocriptine也是脑一氧化氮合酶的强抑制剂。麦角生物碱Bromocriptine(BKT)被发现作为纯化的神经元型一氧化氮合酶(NOS)的强抑制剂(IC50 = 10±2μM),而它对诱导型巨噬细胞NOS(IC50>100μM)的活性很差[2] 。发现溴隐亭抑制至少一种人细胞色素P450酶的活性。 Bromocriptine是一种有效的CYP3A4抑制剂,计算出的相互作用IC50值为1.69μM[3]。

[体内研究]

在强迫游泳试验(FST)和尾部悬吊试验(TST)中,在小鼠组中给予甲磺酸布洛霉素(2mg/kg,ip)7天。与对照相比,Bromocriptine组显示出显着的抗不动作用。当在最后一次7天MPE处理后30分钟给予溴隐亭并进行FST时,与单独的MPE处理相比,该多巴胺能激动剂产生MPE(200mg/kg,口服)的抗不动作用的显着和剂量依赖性增强。与对照相比,Bromocriptine治疗组显示出不动时间的显着减少。用MPE(100和200mg/kg,po)预处理7天后给予溴隐亭,与单独的MPE治疗相比,显示出MPE的抗不动作用的显着和剂量依赖性增强[4]。与假手术(注射盐水的大鼠)相比,脑室内给予溴隐亭显着降低静态机械异常性疼痛(SMA)评分,并且其效果持续30分钟。与假手术相比,腹膜内给予溴隐亭诱导CCI-IoN组疼痛评分显着,剂量依赖性(0.1 mg和1 mg/kg)降低,其效果持续6 h。最高剂量诱导评分降低最高(P <0.01)。 Bromocriptine效应持续20分钟。与假手术相比,腹膜内施用溴隐亭诱导CCI-IoN + 6-OHDA损伤组中SMA评分的显着剂量依赖性降低。它的效果持续6小时[5]。

[激酶实验]

进行[35S]-GTPγS结合测定。将细胞膜（25±75μg）在含有0.1mM二硫苏糖醇（DTT）和1μMGDP的缓冲液B和体积为0.9mL的药物中于30℃温育30分钟。当加入[35S]-GTPγS（50±150pM，最终浓度）（在100uL缓冲液B中）以引发反应时，该预温育确保测试的激动剂处于平衡状态。除非另有说明，否则将测定混合物再温育20分钟。通过快速过滤终止测定，并如上文对放射配体结合测定所述测定结合的放射活性。 [35S]-GTPγS的总结合小于添加[1]的20％。

[动物实验]

小鼠[4]使用任一性别的瑞士小鼠（20-25g）（总共150只）。 Bromocriptine mesylate用作多巴胺受体（D2）激动剂。氟哌啶醇在蒸馏水中稀释，蒸馏水用于注射载体。将甲磺酸布洛霉素溶于一滴冰醋酸中，并在蒸馏水中定容。将丙咪嗪溶于0.9％生理盐水中。在强迫游泳试验（FST）和尾部悬浮试验（TST）中，在小鼠组中施用氟哌啶醇（0.1mg / kg，ip）和布洛霉素甲磺酸盐（2mg / kg，ip）7天。作为标准的丙咪嗪（10mg / kg，口服）在阳性对照组中施用7天。大鼠[5]使用成年雄性Sprague-Dawley大鼠（N = 112,275-325g）。注射6-OHDA两周后，使用面罩将动物短暂（<3分钟）用2％氟烷麻醉，并接受脑池内给药Bromocriptine（溶于5μL载体中的7μg/ kg）或单独的载体（5μL） 0.9％盐水）。对于ip注射，我们使用Bromocriptine（1mg / kg）和SKF81297（3mg / kg溶于0.9％盐水中）浓度。在恢复期（<2分钟）后，将大鼠置于观察区域中40分钟，由盲实验者进行测试。

[参考文献]

[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.

[相关活性小分子]

甲磺酸溴隐亭物理化学性质

[ 沸点 ]:
891.3ºC at 760 mmHg

[ 分子式 ]:
C₃₃H₄₄BrN₅O₈S

[ 分子量 ]:
750.700

[ 闪点 ]:
492.8ºC

[ 精确质量 ]:
749.209412

[ PSA ]:
180.96000

[ LogP ]:
3.98220

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
0mmHg at 25°C

[ 储存条件 ]:
库房通风干燥低温

[ 水溶解性 ]:
H2O: 0.8 mg/mL

甲磺酸溴隐亭毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KE1595000

CHEMICAL NAME :: alpha-Ergocryptine, 2-bromo-, methanesulfonate

CAS REGISTRY NUMBER :: 22260-51-1

LAST UPDATED :: 199504

DATA ITEMS CITED :: 24

MOLECULAR FORMULA :: C32-H4O-Br-N5-O5.C-H4-O3-S

MOLECULAR WEIGHT :: 714.43

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 50 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 340,1410,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 650 ug/kg/9D-I

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Behavioral - headache Cardiac - cardiomyopathy including infarction

REFERENCE :: AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 118,199,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 375 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Cardiac - pulse rate increase, without fall in BP Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: JOPDAB Journal of Pediatrics. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63141) V.1- 1932- Volume(issue)/page/year: 105,838,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 1 mg/kg/20D-I

TOXIC EFFECTS :: Behavioral - toxic psychosis

REFERENCE :: AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921- Volume(issue)/page/year: 143,935,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 52 mg/kg/35W-I

TOXIC EFFECTS :: Brain and Coverings - changes in cerebral spinal fluid

REFERENCE :: NEURAI Neurology. (Modern Medicine Pub., Inc., 1 E. First St., Duluth, MN 55802) V.1- 1951- Volume(issue)/page/year: 35,1193,1985

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 30,809,1979

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 30,809,1979

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 10500 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 29,1231,1978

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2502 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 30,809,1979

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 189 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 30,809,1979

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 30,809,1979

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 8200 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,232,1979 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1400 mg/kg

SEX/DURATION :: lactating female 1-14 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - postpartum

REFERENCE :: JRPMAP Journal of Reproductive Medicine. (2 Jacklynn Ct., St. Louis, MO 63132) V.3- 1969- Volume(issue)/page/year: 33,630,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 42 mg/kg

SEX/DURATION :: female 1-7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

REFERENCE :: EXPEAM Experientia. (Birkhaeuser Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1945- Volume(issue)/page/year: 30,1358,1974

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 60 mg/kg

SEX/DURATION :: female 6 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Maternal Effects - uterus, cervix, vagina Reproductive - Maternal Effects - other effects

REFERENCE :: BIREBV Biology of Reproduction. (Soc. for the Study of Reproduction, 309 W. Clark St., Champaign, IL 61820) V.1- 1969- Volume(issue)/page/year: 34,788,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 3 mg/kg

SEX/DURATION :: male 15 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct

REFERENCE :: IJANDP International Journal of Andrology. (Scriptor Publisher ApS, 15 Gasvaerksvej, DK-1656 Copenhagen V, Denmark) V.1- 1978- Volume(issue)/page/year: 5,331,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 10500 ug/kg

SEX/DURATION :: female 1-7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

REFERENCE :: EXPEAM Experientia. (Birkhaeuser Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1945- Volume(issue)/page/year: 30,1358,1974

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 225 ug/kg

SEX/DURATION :: female 3 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

REFERENCE :: EXPEAM Experientia. (Birkhaeuser Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1945- Volume(issue)/page/year: 24,1130,1968

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 10500 ug/kg

SEX/DURATION :: female 6-8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - postpartum

REFERENCE :: EXPEAM Experientia. (Birkhaeuser Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1945- Volume(issue)/page/year: 24,1130,1968

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 2 mg/kg

SEX/DURATION :: female 5 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

REFERENCE :: TOLED5 Toxicology Letters. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1977- Volume(issue)/page/year: 50,189,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

DOSE :: 35 mg/kg

SEX/DURATION :: female 14-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - other effects to embryo

REFERENCE :: GCENA5 General and Comparative Endocrinology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1961- Volume(issue)/page/year: 39,118,1979

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 20 mg/kg

SEX/DURATION :: male 10 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands Reproductive - Paternal Effects - other effects on male

REFERENCE :: IJEBA6 Indian Journal of Experimental Biology. (Publications & Information Directorate, CSIR, Hillside Rd., New Delhi 110 012, India) V.1- 1963- Volume(issue)/page/year: 23,679,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 3 mg/kg

SEX/DURATION :: lactating female 3 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - postpartum

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 26,51,1976 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4920 No. of Facilities: 27 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 499 (estimated) No. of Female Employees: 225 (estimated)

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甲磺酸溴隐亭安全信息

[ 符号 ]:

GHS07, GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H410

[ 警示性声明 ]:
P301 + P312 + P330

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R20/21/22

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
UN 3077 9 / PGIII

[ WGK德国 ]:
3

[ RTECS号 ]:
KE1595000

甲磺酸溴隐亭制备

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甲磺酸溴隐亭文献

Dopamine-2 receptor activation suppresses PACAP expression in gonadotrophs.

Endocrinology 155(7) , 2647-57, (2014)

Pituitary adenylate cyclase-activating polypeptide (PACAP) is expressed at a high level in the fetal pituitary and decreases profoundly between embryonic day 19 and postnatal day 1 (PN1), with a furth...

Does bromocriptine play a role in decreasing oxidative stress for early weaned programmed obesity?

Life Sci. 95(1) , 14-21, (2014)

Studies have demonstrated that early weaning can promote metabolic syndrome during adulthood and that obesity increases oxidative stress. Thus, we aimed to evaluate redox status in a pharmacological e...

Mediation of dopamine D2 receptors activation in post-conditioning-attenuated cardiomyocyte apoptosis

Exp. Cell Res. 323(1) , 118-30, (2014)

The physiological and pathological roles of dopamine D2 receptors (DR2) in the regulation of cardiovacular functions have been recognized. DR2 activation protects hypoxia/reoxygenation (H/R)-induced c...

更多文献

甲磺酸溴隐亭

甲磺酸溴隐亭用途

甲磺酸溴隐亭名称

甲磺酸溴隐亭生物活性

甲磺酸溴隐亭物理化学性质

甲磺酸溴隐亭毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

甲磺酸溴隐亭安全信息

甲磺酸溴隐亭制备

甲磺酸溴隐亭文献

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