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分类

• {SNA} Approved Therapeutics/Drug Candidates, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Cytokines, Growth Factors and Hormones, Hormones, Other Steroid Products, Pfizer Compounds, S, Steroid Hormones
• {uni_hamburg} no charge; oxygen heterocycle; carbocycle; alicycle; large ring; fused rings; 5ring; 6ring; 9ring; 10ring; 13ring; 14ring; 17ring; spiro; ester; ketone; thioester; lactone; chiral; 1fragment
• Approved Therapeutics/Drug Candidates, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Cytokines, Growth Factors and Hormones, Hormones, Other Steroid Products, Pfizer Compounds, S, Steroid Hormones

产品应用

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相关文献及参考

• [2]. Fagart J, et al. A new mode of mineralocorticoid receptor antagonism by a potent and selective nonsteroidal molecule. J Biol Chem. 2010;285(39):29932-29940.
• [3]. Dong D, et al. Spironolactone alleviates diabetic nephropathy through promoting autophagy in podocytes. Int Urol Nephrol. 2019;51(4):755-764.
• Corp MSDS 1 (2), 3167:D / FT-IR 2 (3), 4254:D / FT-IR 1 (2), 1062:D / FT-NMR 1 (3), 604:B / IR-Spectra (3), 1506:F / NMR-Reference 2 (2), 939:C / RegBook 1 (2), 2875:C / Sax 6 , 152 / Sigma FT-IR 1 (1), 1318:A / Structure Index 1 , 460:A:7
• Merck 14 ,8760
• Moghetti, P., et al. J. Clin. Endocrinol. Metab. 84 , 1250, (1999) 摘要
• Pitt, B., et al. New Engl. J. Med. 341 , 709, (1999) 摘要
• Sato, A., et al. Hypertens. Res. 22 , 17, (1999) 摘要
• Short: EINECS Title: EINECS (European Inventory of Existing Commercial Chemical Substances) Source: Official Journal of the European Communities V

安全信息

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Human - woman
DOSE/DURATION           : 122 mg/kg/61D-I
TOXIC EFFECTS :
   Kidney, Ureter, Bladder - changes in tubules (including acute renal failure,
   acute tubular necrosis)
REFERENCE :
   NZMJAX New Zealand Medical Journal.  (New Zealand Medical Assoc., P.O. Box
   156, Wellington, New Zealand)  V.1-    1900-  Volume(issue)/page/year:
   83,147,1976

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 260 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   NIIRDN Drugs in Japan (Ethical Drugs).  (Yakugyo Jiho Co., Ltd., Tokyo,
   Japan)  Volume(issue)/page/year: 6,381,1982

{hazard_com

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Human
DOSE/DURATION           : 5600 mg/kg
TOXIC EFFECTS :
   Kidney, Ureter, Bladder - urine volume increased
   Nutritional and Gross Metabolic - changes in sodium
   Nutritional and Gross Metabolic - changes in calcium
REFERENCE :
   JLCMAK Journal of Laboratory and Clinical Medicine.  (C.V. Mosby Co., 11830
   Westline Industrial Dr., St. Louis, MO 63141)  V.1-    1915-
   Volume(issue)/page/year: 80,224,19

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 :
   JEPTDQ Journal of Environmental Pathology and Toxicology.  (Park Forest
   South, IL)  V.1-5(3), 1977-81(?).  For publisher information, see JEPOEC.
   Volume(issue)/page/year: 1(5),641,1978

TYPE OF

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Unreported
SPECIES OBSERVED        : Human - woman
DOSE                    : 280 mg/kg
SEX/DURATION            : female 35 day(s) pre-mating
TOXIC EFFECTS :
   Reproductive - Maternal Effects - menstrual cycle changes or disorders
   Reproductive - Maternal Effects - breasts, lactation (prior to or during
   pregnancy)
REFERENCE :
   AIMEAS Annals of Internal Medicine.  (American College of Physicians, 4200
   Pine St., Philadelphia, PA 19104)  V.1-    1927-  Volume(issue)/page/year:
   69,685,1968

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Human - man
DOSE                    : 1208 mg/kg
SEX/DURATION            : male 47 week(s) pre-mating
TOXIC EFFECTS :
   Reproductive - Paternal Effects - impotence
   Reproductive - Paternal Effects - breast development
REFERENCE :
   BMJOAE British Medical Journal.  (British Medical Assoc., BMA House,
   Tavistock Sq., London WC1H 9JR, UK)  V.1-    1857- Volume(issue)/page/year:
   2,729,1972

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 360 mg/kg
SEX/DURATION            : female 13-21 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Specific Developmental Abnormalities - urogenital system
REFERENCE :
   ACENA7 Acta Endocrinologica (Copenhagen).  (Periodica, Skolegade 12 E,
   DK-2500 Valby, Denmark) V.1-    1948-  Volume(issue)/page/year: 95,540,1980

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 160 mg/kg
SEX/DURATION            : female 1 day(s) pre-mating
TOXIC EFFECTS :
   Reproductive - Fertility - other measures of fertility
REFERENCE :

其他信息

• 螺内酯价格(试剂级):更新日期 产品编号 产品名称 包装 价格 2010/06/21 207460010 螺内酯 Spironolactone 99% 1 GR 666元 2010/06/21 207460050 螺内酯 Spironolactone 99% 5 GR 2629元
• 毒害物质数据:52-01-7(Hazardous Substances Data)
• 毒性分级:高毒
• TCI Shanghai:螺内酯 Spironolactone,>;95.0%(E)(52-01-7)
• EPA Substance Registry System:52-01-7(EPA Substance)
• MOL 文件:52-01-7.mol
• 利尿药:螺内酯是一种弱的保钾利尿药，又名安体舒通、螺旋内酯，为白色或类白色细微结晶性粉末，微有苦味，无臭或有轻微硫醇臭。在氯仿中极易溶解，不溶于水，溶于乙醇，易溶于苯或醋酸乙酯。化学结构与醛固酮相似，可与醛固酮竞争远曲小管及集合管细胞浆内的醛固酮受体，影响醛固酮和受体结合，从而阻碍醛固酮诱导蛋白的合成，进而抑制K+-Na+交换，钾的排出减少，起到保钾利尿作用。螺内酯的利尿作用强度与体内醛固酮分泌多少有关，分泌多则作用强，分泌少则作用弱，无醛固酮分泌的病人服用无利尿作用。 由于本药仅作用于远曲小管和集合管，对肾小管其他各段无作用，故该药利尿作用弱，起效慢，维持时间长，主要用于伴有醛固酮增多的顽固性水肿，如肝硬化腹水、充血性心力衰竭、肾病综合征等，对充血性心力衰竭因缺钠而引起继发性醛固酮增多患者疗效较好，单用本品时利尿作用往往较差，常与氢氯噻嗪或双氢克尿噻合用可增强疗效。此外用于原发性醛固酮增多症、原发性高血压的治疗。高钾血症及肾功能衰竭的患者禁用。 本品口服迅速吸收而不规则，其吸收速率与螺内酯的颗粒大小有关。一般制法，生物利用度仅为5%，如制成微粒其吸收率可达 90%，达峰血药浓度约为3小时。在体内代谢迅速，主要代谢物烯睾丙内酯 (孕烯内酯，Canrenone) 能发挥药理活性，其他代谢物逐渐转化为烯睾丙内酯。一次口服后2～4小时血清中代谢物达峰值。代谢物的浓度在 12小时内浓度迅速下降，在12～96小时缓慢下降。口服多次剂量后烯睾丙内酯代谢物的半衰期为13～24小时。螺内酯的半衰期仅约10分钟。烯睾丙内酯的血浆蛋白结合率为98%。其代谢物经胆汁和尿液排泄。烯睾丙内酯代谢有肠肝循环。本品可透过胎盘屏障并进入乳汁。还有抑制雌激素和雄激素合成的作用。
• 图谱信息:螺内酯(52-01-7)红外图谱(IR1) 螺内酯(52-01-7)红外图谱(IR2)
• 用途一:利尿药。
• 可燃性危险特性:易燃; 燃烧产生有毒硫氧化物烟雾
• 储运特性:库房通风低温干燥; 与食品原料分开存放
• 灭火剂:干粉、泡沫、砂土、二氧化碳, 雾状水
• 急性毒性:腹腔-大鼠 LD50: 277 毫克/公斤; 口腹腔-小鼠 LD50: 260 毫克/公斤
• 比旋光度:-37 ° (c=1, CHCl3)
• 适应证:螺内酯为醛固酮的竞争性抑制药，药物本身并没有活性，利尿作用是与内源性醛固酮竞争性拮抗而发生，属于保钾利尿剂。 ①水肿性疾病，与其他利尿药合用，治疗充血性心力衰竭、肝硬化腹水、肾性水肿等水肿性疾病，其目的在于纠正上述疾病伴发的继发性醛固酮分泌增多，并对抗其他利尿药的排钾作用;也用于特发性水肿的治疗。 ②高血压，作为高血压的辅助治疗药物。 ③原发性醛固酮增多症，螺内酯可用于此病的诊断和治疗。 ④低钾血症的预防，与噻嗪类利尿药合用，增强利尿效应和预防低钾血症。
• 上游原料:皂素 --> 雄烯二酮
• 类别:有毒物品