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盐酸地尔硫卓

盐酸地尔硫卓用途

Diltiazem hydrochloride是钙离子流入抑制剂(缓慢通道阻断剂或钙拮抗剂)。
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盐酸地尔硫卓作用

  1 药理本品为钙离子通道阻滞剂,其作用与心肌及血管平滑肌除极时抑制钙离子内流有关。本品可以有效地扩张心外膜和心内膜下的冠状动脉,缓解自发性心绞痛或由麦角新碱诱发冠状动脉痉挛所致心绞痛;通过减慢心率和降低血压,减少心肌需氧量,增加运动耐量并缓解劳力型心绞痛。本品可以使血管平滑肌松弛,周围血管阻力下降,血压降低;其降压的幅度与高血压的程度有关,血压正常者仅使血压轻度下降。本品有负性肌力作用,并可减慢窦房结和房室结的传导。
  2 毒理致癌、致突变和生殖毒性作用有报告大鼠服用本品24个月,小鼠服用本品21个月未发现致癌作用。体外细菌实验未发现致突变作用。动物实验证实本品对生育力无明显作用。 
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盐酸地尔硫卓名称

[ CAS 号 ]:
33286-22-5

[ 中文名 ]:
盐酸地尔硫卓

[ 英文名 ]:
diltiazem hydrochloride

[中文别名 ]:

[英文别名 ]:

盐酸地尔硫卓生物活性

[ 描述 ]:

Diltiazem hydrochloride是钙离子流入抑制剂(缓慢通道阻断剂或钙拮抗剂)。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道
研究领域 >> 心血管疾病

[体外研究]

苯并硫氮杂卓Ca2 +拮抗剂地尔硫卓盐酸盐与L型Ca2 +通道α1亚基中的跨膜区段IIIS6和IVS6相互作用[1]。地尔硫卓引起剂量依赖性的收缩抑制以及由α肾上腺素能受体激活和高K +去极化刺激的Ca2 +流入。地尔硫卓在抑制高钾和低浓度去甲肾上腺素(NE)引起的收缩方面大致同样有效[2]。地尔硫卓还抑制心脏线粒体中Na依赖性Ca-外流。地尔硫卓的顺式和反式形式的(+)-光学异构体均抑制Na-Ca交换活性,具有相当的效力(IC50为10-20μM)[3]。

[体内研究]

地尔硫卓对去极化兔主动脉的Ca2 +诱导的收缩产生非竞争性抑制。此外,去除[Ca2 +] ex和添加地尔硫卓的平滑肌作用之间缺乏平行[2]。地尔硫卓可改善大鼠甲亢实验模型中的心脏微循环和功能。用氯沙坦地尔硫卓治疗甲状腺功能亢进大鼠(4.7±0.7%; P <0.001)可显着降低左心室纤维化区域的百分比[4]。在有意识的自发性高血压大鼠(SHR)中,地尔硫卓剂量依赖性地降低血压并且在静脉内施用后增加心率(0.03-1mg/kg)。口服施用地尔硫卓(100 mg/kg)也可降低SHR的血压[5]。

[参考文献]

[1]. Kraus RL, et al. Molecular mechanism of diltiazem interaction with L-type Ca2+ channels. J Biol Chem. 1998 Oct 16;273(42):27205-12.

[2]. van Breemen C, et al. The mechanism of inhibitory action of diltiazem on vascular smooth muscle contractility. J Pharmacol Exp Ther. 1981 Aug;218(2):459-63.

[3]. Chiesi M, et al. Stereospecific action of diltiazem on the mitochondrial Na-Ca exchange system and on sarcolemmal Ca-channels. Biochem Pharmacol. 1987 Sep 1;36(17):2735-40.

[4]. Freitas F, et al. Cardiac microvascular rarefaction in hyperthyroid rats is reversed by losartan, diltiazem, and propranolol. Fundam Clin Pharmacol. 2015 Feb;29(1):31-40.

[5]. Sato M, et al. Hypotensive effects of diltiazem hydrochloride in the normotensive, spontaneously hypertensive and renal hypertensive rats (author's transl). Nihon Yakurigaku Zasshi. 1979 Mar;75(2):99-106.


[相关活性小分子]

硫酸新霉素 | 硝苯地平 | 氯化乙酰胆碱; 乙酰氯化胆碱 | 离子霉素 | (S)-2,6-二甲基-5-硝基-4-(2-三氟甲基)苯基)-1,4-二氢吡啶-3-甲酸甲酯 | 尼莫地平 | 米贝拉地尔 | 左乙拉西坦 | CDN1163 | 丹曲林钠 | 毒胡萝卜素 | 氟芬那酸 | ABT-639 | N-(2,6-二甲基苯基)-2-(4-(2-羟基-3-(2-甲氧基苯氧基)-丙基)哌嗪-1-基)乙酰胺 二盐酸盐 | 色甘酸钠

盐酸地尔硫卓物理化学性质

[ 密度 ]:
1.26g/cm3

[ 沸点 ]:
594.4ºC at 760mmHg

[ 熔点 ]:
212-214 °C

[ 分子式 ]:
C22H27ClN2O4S

[ 分子量 ]:
450.979

[ 闪点 ]:
313.3ºC

[ 精确质量 ]:
450.138000

[ PSA ]:
84.38000

[ LogP ]:
4.23550

[ 外观性状 ]:
无气味的白色粉末

[ 折射率 ]:
118 ° (C=1, H2O)

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
soluble

盐酸地尔硫卓MSDS

盐酸地尔硫卓毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
DL0310000
CHEMICAL NAME :
1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-3-(acetyloxy)-5-(2-(dimethylamino)ethyl)- 2-(4- methoxyphenyl)-, monohydrochloride, cis-(+)-
CAS REGISTRY NUMBER :
33286-22-5
LAST UPDATED :
199607
DATA ITEMS CITED :
37
MOLECULAR FORMULA :
C22-H26-N2-O4-S.Cl-H
MOLECULAR WEIGHT :
451.02
WISWESSER LINE NOTATION :
T67 GNV KS&TJ G2N1&1 IOV1 JR DO1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
21 mg/kg
TOXIC EFFECTS :
Cardiac - cardiomyopathy including infarction Cardiac - pulse rate Vascular - BP lowering not characterized in autonomic section
REFERENCE :
PGMJAO Postgraduate Medical Journal. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1925- Volume(issue)/page/year: 69,474,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
3429 ug/kg/2D-I
TOXIC EFFECTS :
Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 341,967,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
8400 ug/kg
TOXIC EFFECTS :
Cardiac - pulse rate Vascular - BP lowering not characterized in autonomic section
REFERENCE :
AEMED3 Annals of Emergency Medicine. (American College of Emergency Physicians, 1125 Executive Circle, Irving, TX 75038) Volume(issue)/page/year: 22,196,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
18 mg/kg
TOXIC EFFECTS :
Cardiac - cardiomyopathy including infarction Cardiac - pulse rate Vascular - BP lowering not characterized in autonomic section
REFERENCE :
JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 29,45,1991
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
120 mg/kg
TOXIC EFFECTS :
Cardiac - cardiomyopathy including infarction
REFERENCE :
HETOEA Human & Experimental Toxicology. (Macmillan Press Ltd., Brunel Road, Houndmills, Basingstoke, Hampshire, RG21 2XS, UK) V.9- 1990- Volume(issue)/page/year: 13,161,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
19 mg/kg
TOXIC EFFECTS :
Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
PGMJAO Postgraduate Medical Journal. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1925- Volume(issue)/page/year: 64,467,1988
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
36 mg/kg/13D-I
TOXIC EFFECTS :
Liver - hepatitis, fibrous (cirrhosis, post-necrotic scarring)
REFERENCE :
GASTAB Gastroenterology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1943- Volume(issue)/page/year: 88,1260,1985
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
18 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Vascular - BP lowering not characterized in autonomic section Skin and Appendages - sweating
REFERENCE :
JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 29,45,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
7200 ug/kg/2D-I
TOXIC EFFECTS :
Behavioral - hallucinations, distorted perceptions Behavioral - toxic psychosis
REFERENCE :
JRSMD9 Journal of the Royal Society of Medicine. (Oxford Univ. Press, Walton St., Oxford OX2 6DP, UK) V.71- 1978- Volume(issue)/page/year: 81,296,1988
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
7200 ug/kg
TOXIC EFFECTS :
Behavioral - hallucinations, distorted perceptions Behavioral - toxic psychosis
REFERENCE :
JRSMD9 Journal of the Royal Society of Medicine. (Oxford Univ. Press, Walton St., Oxford OX2 6DP, UK) V.71- 1978- Volume(issue)/page/year: 81,296,1988
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
560 mg/kg
TOXIC EFFECTS :
Behavioral - antipsychotic
REFERENCE :
JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 22,467,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
520 mg/kg
TOXIC EFFECTS :
Behavioral - antipsychotic
REFERENCE :
JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 22,467,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
38 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Behavioral - tetany
REFERENCE :
JMGZAI Japan Medical Gazette. (Tokyo, Japan) V.1-18(?), 1964-81. Discontinued. Volume(issue)/page/year: 11(1),12,1974
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
508 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 33,2192,1990
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
177 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 29,820,1986
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
260 mg/kg
TOXIC EFFECTS :
Behavioral - antipsychotic
REFERENCE :
JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 22,467,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
58 mg/kg
TOXIC EFFECTS :
Behavioral - antipsychotic
REFERENCE :
JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 22,467,1972
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
40 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - nausea or vomiting
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 21,4843,1987 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
45500 mg/kg/26W-C
TOXIC EFFECTS :
Nutritional and Gross Metabolic - weight loss or decreased weight gain Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases Related to Chronic Data - death
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 8,757,1974
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1638 mg/kg/13W-I
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Endocrine - changes in adrenal weight Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 21,4851,1987 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1200 mg/kg
SEX/DURATION :
female 9-14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - parturition Reproductive - Effects on Embryo or Fetus - fetal death
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 8,3401,1974
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
60 mg/kg
SEX/DURATION :
female 9-14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - live birth index (measured after birth)
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 8,3401,1974
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
700 mg/kg
SEX/DURATION :
female 15-21 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 8,3401,1974
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
600 mg/kg
SEX/DURATION :
female 11 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 8,3401,1974
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
480 mg/kg
SEX/DURATION :
female 9-14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - other developmental abnormalities
REFERENCE :
OFAJAE Okajimas Folia Anatomica Japonica. (Keio Univ., School of Medicine, Dept. of Anatomy, 35 Shinano-machi, Shinjuku-ku, Tokyo 160, Japan) V.14- 1936- Volume(issue)/page/year: 52,103,1975
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
80 mg/kg
SEX/DURATION :
female 13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
OFAJAE Okajimas Folia Anatomica Japonica. (Keio Univ., School of Medicine, Dept. of Anatomy, 35 Shinano-machi, Shinjuku-ku, Tokyo 160, Japan) V.14- 1936- Volume(issue)/page/year: 52,103,1975
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
130 mg/kg
SEX/DURATION :
female 17-21 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 21,4869,1987
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
378 mg/kg
SEX/DURATION :
female 14 day(s) pre-mating female 1-7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - other measures of fertility
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 21,4857,1987
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
60 mg/kg
SEX/DURATION :
female 7-12 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 8,3401,1974
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
25 mg/kg
SEX/DURATION :
female 9 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 8,3401,1974
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
100 mg/kg
SEX/DURATION :
female 9 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - sex ratio
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 8,3401,1974
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
25 mg/kg
SEX/DURATION :
female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 8,3401,1974
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
12500 ug/kg
SEX/DURATION :
female 11 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
REFERENCE :
OFAJAE Okajimas Folia Anatomica Japonica. (Keio Univ., School of Medicine, Dept. of Anatomy, 35 Shinano-machi, Shinjuku-ku, Tokyo 160, Japan) V.14- 1936- Volume(issue)/page/year: 52,103,1975
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
25 mg/kg
SEX/DURATION :
female 9 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
OFAJAE Okajimas Folia Anatomica Japonica. (Keio Univ., School of Medicine, Dept. of Anatomy, 35 Shinano-machi, Shinjuku-ku, Tokyo 160, Japan) V.14- 1936- Volume(issue)/page/year: 52,103,1975
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
50 mg/kg
SEX/DURATION :
female 9 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
OFAJAE Okajimas Folia Anatomica Japonica. (Keio Univ., School of Medicine, Dept. of Anatomy, 35 Shinano-machi, Shinjuku-ku, Tokyo 160, Japan) V.14- 1936- Volume(issue)/page/year: 52,103,1975
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
50 mg/kg
SEX/DURATION :
female 13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - other developmental abnormalities
REFERENCE :
OFAJAE Okajimas Folia Anatomica Japonica. (Keio Univ., School of Medicine, Dept. of Anatomy, 35 Shinano-machi, Shinjuku-ku, Tokyo 160, Japan) V.14- 1936- Volume(issue)/page/year: 52,103,1975
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
125 mg/kg
SEX/DURATION :
female 7-16 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
OFAJAE Okajimas Folia Anatomica Japonica. (Keio Univ., School of Medicine, Dept. of Anatomy, 35 Shinano-machi, Shinjuku-ku, Tokyo 160, Japan) V.14- 1936- Volume(issue)/page/year: 52,103,1975
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盐酸地尔硫卓安全信息

[ 符号 ]:

GHS02, GHS07

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H302 + H312 + H332-H319

[ 警示性声明 ]:
P210-P261-P302 + P352 + P312-P304 + P340 + P312-P337 + P313-P403 + P235

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R22;R40

[ 安全声明 (欧洲) ]:
S36-S45-S36/37

[ 危险品运输编码 ]:
3249

[ WGK德国 ]:
3

[ RTECS号 ]:
DL0310000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2934999090

盐酸地尔硫卓合成路线

盐酸地尔硫卓上下游产品

盐酸地尔硫卓制备

1、 由2-氨基硫酚与对甲氧苯基环氧丙酸乙酯缩合得2-(4-甲氧基苯基)-3-羟基-1,5-苯并硫氮杂 -4(5H)-酮。再经酰化、与二甲氨基氯乙烷缩合、成盐制得硫氮卓酮。

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盐酸地尔硫卓海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

盐酸地尔硫卓文献

Characterization of Species Differences in Tissue Diltiazem Deacetylation Identifies Ces2a as a Rat-Specific Diltiazem Deacetylase.

Drug Metab. Dispos. 43 , 1218-25, (2015)

Diltiazem, a calcium channel blocker, is mainly metabolized via demethylation or deacetylation in humans. Diltiazem demethylation is catalyzed by cytochrome P450 2D6 and 3A4. Although it was previousl...

A predictive ligand-based Bayesian model for human drug-induced liver injury.

Drug Metab. Dispos. 38 , 2302-8, (2010)

Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predicti...

Chemical genetics reveals a complex functional ground state of neural stem cells.

Nat. Chem. Biol. 3(5) , 268-273, (2007)

The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain canc...


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