Naloxone盐酸盐是阿片类拮抗剂,对阿片受体的IC50为3 nM。
Naloxone hydrochloride is an opioid inverse agonist drug used to counter the effects of opiate overdose. Studies have identified this product as a significant immunoadjuvant in cancer immunotherapy.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Liu B, et al. J Pharmacol Exp Ther, 2000, 293(2), 607-617.
[2] Pinelli and Trivulzio (1997) Quantitative evaluation of opioid withdrawal signs in rats repeatedly treated with morphine and injected with naloxone, in the absence or presence of the antiabstinence agent clonidine. J.Pharmacol.Toxicol.Methods 38 117.
[3] Spivak et al (1997) Naloxone activation of mu-opioid receptors mutated at a histidine residue lining the opioid cavity. Mol.Pharmacol. 52 983.
[4] Olson et al (1996) Endogenous opiates: 1995. Peptides 17 1421.
分子式 C19H22ClNO4 |
分子量 363.84 |
CAS号 357-08-4 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 70 mg/mL |
Water 70 mg/mL |
Ethanol 4 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01105871 | Pain | Drug: naloxone|Drug: Placebo | University of Washington | 2010-08-01 | 2012-08-17 | |
NCT01531439 | Pain, Postoperative|Postoperative Nausea and Vomiting|Scoliosis | Drug: Naloxone|Drug: Naloxone | Children's Mercy Hospital Kansas City | 2011-06-01 | 2016-01-26 | |
NCT02307721 | Drug Overdose | Drug: Intranasal naloxone|Drug: Intramuscular naloxone|Drug: Remifentanil|Device: Aptar Unidose | Norwegian University of Science and Technology|St. Olavs Hospital | Phase 1|Phase 2 | 2014-12-01 | 2015-10-26 |
NCT02405988 | Drug Overdose | Drug: Intravenous naloxone|Drug: Remifentanil | Norwegian University of Science and Technology|St. Olavs Hospital | 2015-04-01 | 2017-02-02 | |
NCT01935206 | Hyperalgesia|Pain|Naloxone|Opioid Antagonist | Drug: Naloxone (2 mg/kg)|Drug: Placebo | Rigshospitalet, Denmark | Phase 1 | 2013-06-01 | 2014-02-24 |
NCT00890942 | Morphine Adverse Reaction | Drug: naloxone|Drug: normal saline | Mahidol University | 2009-05-01 | 2011-07-22 | |
NCT02137213 | Constipation | Drug: Naloxone|Drug: Placebo | Centre for Addiction and Mental Health|Academic Health Science Centres | Phase 2 | 2014-08-01 | 2015-06-23 |
NCT02700048 | Hypoglycemia Unawareness|Type 1 Diabetes | Drug: intra-nasal naloxone|Drug: Intra-nasal saline | University of Minnesota - Clinical and Translational Science Institute | Phase 1|Phase 2 | 2016-06-01 | 2016-08-01 |
NCT02733822 | Drug Overdose|Opioid-Related Disorders | Drug: Naloxone | King's College London | Phase 1 | 2016-06-01 | 2016-05-16 |
NCT02581111 | Brain Death|Organ Donors|Lung Transplantation | Drug: Naloxone|Drug: Normal saline | Washington University School of Medicine | Phase 2|Phase 3 | 2015-09-01 | 2016-05-23 |
NCT01939444 | Drug Overdose | Drug: naloxone intranasal|Drug: naloxone intravenous | Norwegian University of Science and Technology|St. Olavs Hospital|University of Iceland | Phase 2 | 2013-08-01 | 2015-01-02 |
NCT02669901 | Opiate Antagonist Overdose|Opioid-Related Disorders | Behavioral: Naloxone Auto-Injector | University of New Mexico|Kaleo Pharmaceuticals | 2016-04-01 | 2016-10-24 | |
NCT00880841 | Healthy | Drug: Buprenorphine / Naloxone | Nanotherapeutics, Inc. | 2009-04-01 | 2016-04-11 | |
NCT01912573 | Drug Overdose | Drug: Intranasal (IN) naloxone|Drug: Intravenous (IV) naloxone|Drug: Intramuscular (IM) naloxone|Drug: Intraosseus (IO) naloxone | Judith Feinberg|University of Cincinnati | Phase 4 | 2013-09-01 | 2013-07-29 |
NCT02158117 | Drug Overdose | Drug: nasal naloxone | Norwegian University of Science and Technology|St. Olavs Hospital | Phase 1 | 2014-03-01 | 2017-02-02 |
NCT01160432 | Opiate Dependence | Drug: Methadone, naloxone | Kuopio University Hospital | 2013-05-01 | 2013-07-03 | |
NCT02294253 | Opioid Dependence | Drug: Buprenorphine/naloxone | New York State Psychiatric Institute|National Institute on Drug Abuse (NIDA) | Phase 2|Phase 3 | 2014-09-01 | 2014-11-18 |
NCT01071057 | Pruritus | Drug: Naloxone|Drug: Saline/Morphine | University of British Columbia | Phase 2|Phase 3 | 2010-12-01 | 2015-01-16 |
NCT02120612 | Opioid Dependence|Opioid Use Disorder | Other: Naloxone Education Intervention | Edward Hospital|Edward-Elmhurst Health System | 2014-04-01 | 2017-02-06 | |
NCT00799201 | Constipation|Analgesia | Drug: Naloxone and Docusate | CAMC Health System | Phase 4 | 2007-08-01 | 2015-07-27 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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