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地舍平

地舍平用途

Deserpidine (Harmonyl) 是与 Reserpine 相关的从 Rauwolfia canescens 的根中分离的生物碱。Deserpidine 被用作抗高血压药和镇定剂。Deserpidine 是一种竞争性血管紧张素转化酶 (ACE) 抑制剂。Deserpidine 还减少了肾上腺皮质血管紧张素 II 诱导的醛固酮分泌。
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地舍平名称

[ CAS 号 ]:
131-01-1

[ 中文名 ]:
蛇根平定

[ 英文名 ]:
Deserpidine

[中文别名 ]:

[英文别名 ]:

地舍平生物活性

[ 描述 ]:

Deserpidine (Harmonyl) 是与 Reserpine 相关的从 Rauwolfia canescens 的根中分离的生物碱。Deserpidine 被用作抗高血压药和镇定剂。Deserpidine 是一种竞争性血管紧张素转化酶 (ACE) 抑制剂。Deserpidine 还减少了肾上腺皮质血管紧张素 II 诱导的醛固酮分泌。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 血管紧张素转换酶(ACE)
研究领域 >> 代谢疾病
研究领域 >> 神经疾病

[ 靶点 ]

Angiotensin converting enzyme (ACE)[3]


[体外研究]

地塞米松是一种有效的神经节阻断剂,与利血平的区别在于C-11处没有甲氧基。德西匹定已被用于治疗高血压和精神病。此外,德塞匹丁似乎是其他心脏疾病的控制者[1][2]。

[参考文献]

[1]. Varchi G, et al. Synthesis of deserpidine from reserpine. J Nat Prod. 2005 Nov;68(11):1629-31.

[2]. Zhang H, et al. Liquid chromatography/tandem mass spectrometry method for the quantification of deserpidine in human plasma: Application to a pharmacokinetic study. J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Oct 1;877(27):3221-5.

[3]. Fulton SC, et al. Comparison of the effectiveness of deserpidine, reserpine, and alpha-methyltyrosine on brain biogenic amines. Fed Proc. 1976 Dec;35(14):2558-62.

地舍平物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
676.1±55.0 °C at 760 mmHg

[ 熔点 ]:
~275 °C (dec.)(lit.)

[ 分子式 ]:
C32H38N2O8

[ 分子量 ]:
578.653

[ 闪点 ]:
362.7±31.5 °C

[ 精确质量 ]:
578.262817

[ PSA ]:
108.55000

[ LogP ]:
4.19

[ 外观性状 ]:
白色晶体粉末

[ 蒸汽压 ]:
0.0±2.1 mmHg at 25°C

[ 折射率 ]:
1.626

[ 储存条件 ]:
-20°C

[ 水溶解性 ]:
slightly soluble

地舍平毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
ZG0875000
CHEMICAL NAME :
3-beta,20-alpha-Yohimban-16-beta-carboxylic acid, 18-beta-hydroxy-17-alpha-methoxy-, methyl ester, 3,4,5-trimethoxybenzoate (ester)
CAS REGISTRY NUMBER :
131-01-1
BEILSTEIN REFERENCE NO. :
0101820
LAST UPDATED :
199612
DATA ITEMS CITED :
12
MOLECULAR FORMULA :
C32-H38-N2-O8
MOLECULAR WEIGHT :
578.72
WISWESSER LINE NOTATION :
T F6 D5 C666 EM ON&&TTTJ SOVR CO1 DO1 EO1& TO1 UVO1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
15 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,104,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
500 mg/kg
TOXIC EFFECTS :
Behavioral - coma Lungs, Thorax, or Respiration - dyspnea Gastrointestinal - hypermotility, diarrhea
REFERENCE :
JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 44,688,1955
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
60 mg/kg
TOXIC EFFECTS :
Behavioral - coma Lungs, Thorax, or Respiration - dyspnea Gastrointestinal - hypermotility, diarrhea
REFERENCE :
JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 44,688,1955 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
25690 mg/kg/4W-C
TOXIC EFFECTS :
Related to Chronic Data - death
REFERENCE :
JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 44,688,1955
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
80 mg/kg/4D-I
TOXIC EFFECTS :
Related to Chronic Data - death
REFERENCE :
JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 44,688,1955 ** TUMORIGENIC DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
16 mg/kg/9Y-C
TOXIC EFFECTS :
Tumorigenic - neoplastic by RTECS criteria Skin and Appendages - tumors
REFERENCE :
LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 2,672,1974
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
54 mg/kg/77W-C
TOXIC EFFECTS :
Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors Blood - lymphoma, including Hodgkin's disease
REFERENCE :
COREAF Comptes Rendus Hebdomadaires des Seances, Academie des Sciences. (Paris, France) V.1-261, 1835-1965. For publisher information, see CRASEV. Volume(issue)/page/year: 254,1535,1962 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Unreported
DOSE :
4950 mg/kg
SEX/DURATION :
female 6-16 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)
REFERENCE :
CRSBAW Comptes Rendus des Seances de la Societe de Biologie et de Ses Filiales. (SPPIF, B.P.22, F-41353 Vineuil, France) V.1- 1849- Volume(issue)/page/year: 155,2291,1961
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Unreported
DOSE :
1600 ug/kg
SEX/DURATION :
female 1 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Fertility - other measures of fertility
REFERENCE :
AJOGAH American Journal of Obstetrics and Gynecology. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1920- Volume(issue)/page/year: 83,1405,1962 *** REVIEWS *** TOXICOLOGY REVIEW CLPTAT Clinical Pharmacology and Therapeutics (St. Louis). (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1960- Volume(issue)/page/year: 5,480,1964 TOXICOLOGY REVIEW ADVPA3 Advances in Pharmacology. (New York, NY) V.1-6, 1962-68. For publisher information, see AVPCAQ. Volume(issue)/page/year: 4,263,1966 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X9135 No. of Facilities: 35 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 430 (estimated) No. of Female Employees: 239 (estimated)
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地舍平安全信息

[ 危险品运输编码 ]:
UN 9111

[ WGK德国 ]:
3

地舍平合成路线

地舍平上下游产品

地舍平上游产品

地舍平下游产品

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产品详情:Deserpidine


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相关化合物

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