Amitriptyline HCl 是一种三环抗抑郁药,抑制5-羟色胺受体,去甲肾上腺素受体, 5-HT4, 5-HT2和sigma 1受体。
Amitriptyline inhibits serotonin receptor, norepinephrine receptor, 5-HT4, 5-HT2 and sigma 1 receptor with IC50 of 3.45 nM, 13.3 nM, 7.31 nM, 235 nM and 287 nM, respectively.
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] Vaishnavi SN, et al. Biol Psychiatry, 2004, 55(3), 320-322.
[2] Sawynok et al (2001) Antidepressants as analgesics: an overview of central and peripheral mechanisms of action. J.Psychiatry Neurosci. 26 21.
[3] Ghelardini et al (2000) Antinociception induced by amitriptyline and imipramine is mediated by α2A-adrenoceptors. Jpn.J.Pharmacol. 82 130.
[4] Sanchez and Hyttel (1999) Comparison of the effects of antidepressants and their metabolites on reuptake of biogenic amines and on receptor binding. Cell.Mol.Neurobiol. 19 467.
分子式 C20H24ClN |
分子量 313.86 |
CAS号 549-18-8 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 65 mg/mL |
Water 15 mg/mL |
Ethanol 65 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02256943 | Chronic Pain | Drug: Amitriptyline|Drug: Tolterodine | University Hospital Inselspital, Berne|University of Washington|Ludwig-Maximilians - University of Munich|Aalborg University | Phase 4 | 2014-11-01 | 2016-04-05 |
NCT02256956 | Chronic Pain | Drug: Amitriptyline|Drug: Tolterodine | University Hospital Inselspital, Berne|University of Washington|Aalborg University|Ludwig-Maximilians - University of Munich | Phase 4 | 2014-11-01 | 2016-04-05 |
NCT02256878 | Healthy | Drug: BIRT 2584 XX|Drug: Amitriptyline | Boehringer Ingelheim | Phase 1 | 2004-08-01 | 2014-10-02 |
NCT01856270 | Brain Injuries|Post-Traumatic Headache | Drug: Amitriptyline | University of Washington | Phase 2 | 2013-04-01 | 2016-05-20 |
NCT01566825 | Healthy Subjects | Drug: Amitriptyline|Drug: Placebo | Dieter Kunz, MD|Charite University, Berlin, Germany | 2008-08-01 | 2012-03-27 | |
NCT02519400 | Depression | Drug: Amitriptyline | Asan Medical Center | Phase 1 | 2015-08-01 | 2015-08-09 |
NCT01561209 | Neck Pain | Drug: Amitryptiline|Drug: Placebo | St Joseph University, Beirut, Lebanon | Phase 4 | 2012-03-01 | 2014-06-09 |
NCT01014520 | Herniated Disc|Intervertebral Disc Displacement | Drug: Gabapentin , Amitriptyline | Tabriz University | Phase 2 | 2009-05-01 | 2009-11-16 |
NCT02090998 | Transformed Migraine|Chronic Daily Headache | Procedure: SPG Block with 5% Lidocaine gel|Drug: Amitriptyline | Rutgers, The State University of New Jersey | Phase 4 | 2014-05-01 | 2016-12-13 |
NCT00471445 | Neurotoxicity|Pain|Peripheral Neuropathy|Unspecified Adult Solid Tumor, Protocol Specific | Drug: ketamine/amitriptyline NP-H cream|Other: placebo | Gary Morrow|National Cancer Institute (NCI)|University of Rochester | Phase 3 | 2007-10-01 | 2015-10-13 |
NCT00766350 | Fibromyalgia | Drug: amitriptyline|Drug: quetiapine | Universidad de Granada|AstraZeneca|Hospital Clinico Universitario San Cecilio | Phase 4 | 2008-11-01 | 2014-12-01 |
NCT00740571 | Cancer|Neuralgia | Drug: amitriptyline|Drug: pregabalin | Radboud University|Erasmus Medical Center|Universiteit van Amsterdam | Phase 3 | 2008-09-01 | 2009-02-04 |
NCT00564525 | Functional Gastrointestinal Disorders | Drug: Amitriptyline|Drug: Placebo | Ann & Robert H Lurie Children's Hospital of Chicago|American College of Gastroenterology | Phase 4 | 2002-10-01 | 2007-11-27 |
NCT02552225 | Laryngeal Diseases | Drug: Amitriptyline|Other: Placebo | Boston Medical Center|American Laryngological Association | Phase 2|Phase 3 | 2016-04-01 | 2016-10-07 |
NCT00515229 | Cystic Fibrosis|Infection|Pseudomonas Aeruginosa | Drug: amitriptyline | University Hospital Tuebingen | Phase 2 | 2006-10-01 | 2007-08-10 |
NCT02190526 | Diarrhea- Predominant Irritable Bowel Syndrome|Quality of Life | Drug: Mesalazine(asacol 800 mg)|Drug: Amitriptyline|Drug: placebo like asacol|Drug: placebo like amitriptyline | Tehran University of Medical Sciences|Tillotts Pharma AG | Phase 4 | 2014-09-01 | 2016-04-14 |
NCT00124306 | Bladder Diseases|Interstitial Cystitis | Drug: Amitriptyline|Other: Placebo | National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|University of Pennsylvania | Phase 3 | 2005-02-01 | 2013-10-28 |
NCT01206478 | Chronic Oral Food Refusal | Drug: Amitriptyline|Drug: Placebo|Drug: Megestrol | Ann Davis, PhD, MPH, ABPP|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|University of Kansas Medical Center | Phase 2 | 2010-08-01 | 2016-07-01 |
NCT02434523 | Laryngeal Diseases|Chronic Laryngeal Neuropathy | Drug: Amitriptyline|Other: Placebo | Boston Medical Center|American Laryngological Association | Phase 2|Phase 3 | 2013-09-01 | 2016-10-07 |
NCT00000817 | HIV Infections|Peripheral Nervous System Disease | Drug: Amitriptyline hydrochloride|Drug: Amitriptyline hydrochloride placebo|Procedure: Point acupuncture | National Institute of Allergy and Infectious Diseases (NIAID) | 1994-11-01 | 2013-09-28 | |
NCT02638870 | Irritable Bowel Syndrome | Drug: Amitriptyline | Samsung Medical Center | 2016-01-01 | 2015-12-23 | |
NCT00189059 | Chronic Neuropathic Pain | Drug: amitriptyline | UMC Utrecht|Utrecht University | Phase 4 | 2002-10-01 | 2005-09-12 |
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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