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盐酸钠洛酮

盐酸钠洛酮用途

Naloxone hydrochloride 是一种有效的阿片受体拮抗剂。

盐酸钠洛酮名称

[ CAS 号 ]:
357-08-4

[ 中文名 ]:
盐酸纳洛酮

[ 英文名 ]:
Naloxone HCl

[中文别名 ]:

[英文别名 ]:

盐酸钠洛酮生物活性

[ 描述 ]:

Naloxone hydrochloride 是一种有效的阿片受体拮抗剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体
信号通路 >> 神经信号通路 >> 阿片受体
研究领域 >> 神经疾病

[体内研究]

纳洛酮(2.0 mg/kg,持续输注1.7 mg/kg/h)可显著改善大鼠的神经行为结果,该结果可持续到注射后4周。纳洛酮治疗引起平均动脉血压(MAP)适度且不显著的升高[1]。纳洛酮(0.4 mg/kg)可促进大鼠记忆,并拮抗促肾上腺皮质激素和肾上腺素的遗忘作用[2]。纳洛酮治疗以剂量相关的方式降低猫最初破伤风的强度。纳洛酮(5或10 mg/kg,静脉注射)会导致后续剂量的吗啡产生较少的PTP抑制,但对最大抽搐抑制没有影响[3]。

[动物实验]

在试验中使用年轻成年Wistar大鼠:雌性用于实验1和3(年龄50-70天,体重100-185g),雄性用于实验2和4(年龄51-69天,体重140-200g)。两者都使用相同的设备:一个50×25×25厘米的盒子,由胶合板制成,正面有玻璃墙,地板由间隔10毫米的1毫米口径青铜条组成。在任务l中,将一个5厘米高、25×25厘米的木制平台引入盒子中,以覆盖网格的左半部分。老鼠被身体轻轻地抱着,懒洋洋地躺在面向左后角的平台上,这时石英计时器就会启动。对时间进行计数,直到动物从平台上下来并将它们的四只爪子放在格栅上,在格栅上持续施加0.5毫安、60赫兹的脚跳,直到动物返回平台。在任务2中,平台只有7厘米宽,并且只覆盖网格的最左边的七条;脚跳仅为0.3mA,并且每2秒以0.4msec脉冲传送一次直到动物爬回平台。每次任务训练后,立即将动物从盒子中取出,腹膜内注射以下药物之一:生理盐水(1.0 mL/kg)、ACTH1-24(0.2或2.0μg/kg)、盐酸肾上腺素(5.0或50.0μg/kg),人β-内啡肽(0.1或1.0μg/kg)和盐酸纳洛酮(0.4 mg/kg),或ACTH或肾上腺素与β-内窥肽或纳洛酮一起服用。将所有药物溶解在盐水中,注射体积为1.0mL/kg。在训练24小时后,再次将动物放在平台上(宽的用于任务1,实验1和2,窄的用于任务2,实验3和4),并测量它们再次下放到网格上的延迟,如同在训练会话中一样。这项措施的时间上限为180秒。

[参考文献]

[1]. McIntosh TK, et al. Beneficial effect of the nonselective opiate antagonist naloxone hydrochloride and the thyrotropin-releasing hormone (TRH) analog YM-14673 on long-term neurobehavioral outcome following experimental brain injury in the rat. J Neurotrau  

[2]. Sun L, et al. Endocannabinoid activation of CB1 receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. Eur J Pain. 2017 May;21(5):804-814.  

[3]. Izquierdo I, et al. Effect of ACTH, epinephrine, beta-endorphin, naloxone, and of the combination of naloxone or beta-endorphinwith ACTH or epinephrine on memory consolidation. Psychoneuroendocrinology. 1983;8(1):81-7.  

[4]. Soteropoulos GC, et al. Neuromuscular effects of morphine and naloxone. J Pharmacol Exp Ther. 1973 Jan;184(1):136-42.  

盐酸钠洛酮物理化学性质

[ 沸点 ]:
532.8ºC at 760 mmHg

[ 熔点 ]:
200-2050C

[ 分子式 ]:
C19H22ClNO4

[ 分子量 ]:
363.84

[ 闪点 ]:
276.1ºC

[ 精确质量 ]:
363.123749

[ PSA ]:
70.00000

[ LogP ]:
2.04130

[ 外观性状 ]:
白色至灰白色/粉末

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
ethanol: 3.3 mg/mL stable for several months refrigerated if protected from light.

盐酸钠洛酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
QD2275000
CHEMICAL NAME :
Morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-, hydrochloride, (5-alpha)-
CAS REGISTRY NUMBER :
357-08-4
LAST UPDATED :
199806
DATA ITEMS CITED :
16
MOLECULAR FORMULA :
C19-H21-N-O4.Cl-H
MOLECULAR WEIGHT :
363.87
WISWESSER LINE NOTATION :
T B6566 B6/CO 4ABBC R BX FV HO PN GHT&&TTJ CQ JQ P2U1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
32 ug/kg/3M-C
TOXIC EFFECTS :
Cardiac - pulse rate increase, without fall in BP Lungs, Thorax, or Respiration - acute pulmonary edema Skin and Appendages - sweating
REFERENCE :
AEMED3 Annals of Emergency Medicine. (American College of Emergency Physicians, 1125 Executive Circle, Irving, TX 75038) Volume(issue)/page/year: 16,1294,1987
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
13 ug/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
AJEMEN American Journal of Emergency Medicine. (WB Saunders, Philadelphia, PA) V.1- 1983- Volume(issue)/page/year: 7,127,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 36,655,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
239 mg/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: 16,357,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
500 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 36,655,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
107 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 36,655,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 36,655,1985
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
80 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
RCOCB8 Research Communications in Chemical Pathology and Pharmacology. (PJD Pub. Ltd., P.O. Box 966, Westbury, NY 11590) V.1- 1970- Volume(issue)/page/year: 17,255,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
286 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: 20,844,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
90 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 36,655,1985 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
560 mg/kg
SEX/DURATION :
female 7-20 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - behavioral
REFERENCE :
NTOTDY Neurobehavioral Toxicology and Teratology. (Fayetteville, NY) V.3-8, 1981-86. For publisher information, see NETEEC. Volume(issue)/page/year: 3,295,1981
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
18 mg/kg
SEX/DURATION :
female 14-22 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - behavioral
REFERENCE :
NTOTDY Neurobehavioral Toxicology and Teratology. (Fayetteville, NY) V.3-8, 1981-86. For publisher information, see NETEEC. Volume(issue)/page/year: 5,479,1983
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
75 mg/kg
SEX/DURATION :
female 4-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Effects on Newborn - behavioral
REFERENCE :
NETEEC Neurotoxicology and Teratology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.9- 1987- Volume(issue)/page/year: 11,441,1989
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
1800 ug/kg
SEX/DURATION :
lactating female 1 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects Endocrine - changes in luteinizing hormone
REFERENCE :
THGNBO Theriogenology. (Geron-X, Inc., P.O. Box 1108, Los Altos, CA 94022) V.1- 1974- Volume(issue)/page/year: 39,1193,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
3 mg/kg
SEX/DURATION :
lactating female 2 hour(s) post-birth
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - endocrine system
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: 39,532,1988 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5315 No. of Facilities: 152 (estimated) No. of Industries: 1 No. of Occupations: 5 No. of Employees: 10824 (estimated) No. of Female Employees: 9407 (estimated)

盐酸钠洛酮安全信息

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S22-S24/25-S26-S36/37/39

[ WGK德国 ]:
3

盐酸钠洛酮合成路线

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推荐生产厂家/供应商:

公司名:上海吉至生化科技有限公司

区域:上海市奉贤区

价格:
¥1058.0/250mg

联系人:刘佳

产品详情:盐酸纳洛酮


公司名:上海源溪生物科技有限公司

区域:上海市浦东新区

价格:
¥需询单/1g

联系人:赖经理

产品详情:Naloxone (hydrochloride)


公司名:上海阿拉丁生化科技股份有限公司

区域:上海市浦东新区

价格:
¥1035.9/1ml ¥372.9/250mg ¥137.9/50mg ¥需询单/1g

联系人:阿拉丁李高志

产品详情:Naloxone HCl


公司名:湖北魏氏化学试剂股份有限公司

区域:武汉市洪山区

价格:
¥需询单/5mg ¥需询单/25mg ¥需询单/10g ¥需询单/50g

联系人:张栋

产品详情:盐酸纳洛酮(二水物)


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