Amitriptyline
(Synonyms: MK-230, N-750, Ro41575) 目录号 : GC25060Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties, widely used to treat depression and neuropathic pain. Amitriptyline is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. This product is a waxy solid.
Cas No.:50-48-6
Sample solution is provided at 25 µL, 10mM.
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Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties, widely used to treat depression and neuropathic pain. Amitriptyline is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. This product is a waxy solid.
| Cas No. | 50-48-6 | SDF | Download SDF |
| 别名 | MK-230, N-750, Ro41575 | ||
| 分子式 | C20H23N | 分子量 | 277.4 |
| 溶解度 | DMSO : 100 mg/mL (360.49 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6049 mL | 18.0245 mL | 36.049 mL |
| 5 mM | 0.721 mL | 3.6049 mL | 7.2098 mL |
| 10 mM | 0.3605 mL | 1.8025 mL | 3.6049 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Classics in Chemical Neuroscience: Amitriptyline
ACS Chem Neurosci 2021 Feb 3;12(3):354-362.PMID:33438398DOI:10.1021/acschemneuro.0c00467.
Amitriptyline was the second tricyclic antidepressant to appear on the market for major depressive disorder under the brand name Elavil in 1961. Since its emergence, Amitriptyline has been an effective therapeutic in various disease states and disorders but has also been a concerning source of cardiotoxicity. Amitriptyline inhibits serotonin and norepinephrine reuptake as well as produces off-target activity at histaminergic, muscarinic, and various other receptors. Its role as a modulator of monoamines helped further establish the monoamine theory to understand various mood disorders, paving the way for the now more common selective serotonin/norepinephrine reuptake inhibitors. In this review, we will discuss Amitriptyline's synthesis, manufacturing information, drug metabolism, pharmacology, adverse effects, and its history and importance in therapy to present Amitriptyline as a true classic in chemical neuroscience.
Amitriptyline for the treatment of fibromyalgia: a comprehensive review
Expert Rev Neurother 2015 Oct;15(10):1123-50.PMID:26395929DOI:10.1586/14737175.2015.1091726.
Fibromyalgia is characterized by chronic generalized pain accompanied by a wide range of clinical manifestations. Most clinical practice guidelines recommend multidisciplinary treatment using a combination of pharmacological and non-pharmacological therapies. The tricyclic antidepressant Amitriptyline has been most thoroughly studied in fibromyalgia. Amitriptyline has been evaluated in placebo-controlled studies, and it has served as an active comparator to other therapeutic interventions in the treatment of fibromyalgia. In addition, several systematic reviews and meta-analyses have evaluated its efficacy and safety for the treatment of fibromyalgia. Data from individual studies as well as from systematic reviews indicate that low doses (10-75 mg/day) of Amitriptyline are effective for the treatment of fibromyalgia and, despite the limited quality of the data, they do not seem to be associated with relevant tolerability or safety issues. Consistent with some clinical guidelines, we believe Amitriptyline in low doses should be considered a first-line drug for the treatment of fibromyalgia.
Abuse of Amitriptyline
JAMA 1978 Sep 22;240(13):1372-3.PMID:682328doi
Amitriptyline hydrocholride (Elavil) is frequently used in treating mild to moderate depressive states. A survey of 346 persons enrolled in a methadone maintenance program showed that 86 (25%) had admitted taking Amitriptyline with the purpose of achieving euphoria. Thin-layer chromatography of random urine specimens over five months showed that 34% of the patients had a positive result for Amitriptyline at least once during this time. These results suggest that misuse of Amitriptyline is not uncommon and should be carefully considered prior to prescribing this agent to narcotic dependent persons.
Amitriptyline-induced prolonged cholestasis
Gastroenterology 1988 Jan;94(1):200-3.PMID:3335290DOI:10.1016/0016-5085(88)90631-2.
We report the case of a patient in whom Amitriptyline administration for 5 wk was followed by prolonged cholestasis. Jaundice and pruritus lasted 19 and 20 mo, respectively. Three liver biopsies were performed at different stages of the disease showing the course of liver lesions. Cholestasis initially located in the region of the hepatic venule came to be associated with the progressive development of portal tract lesions consisting of inflammatory infiltration, fibrosis, and disappearance of interlobular bile ducts. Amitriptyline hydroxylation and dextromethorphan O-demethylation are deficient in subjects with the poor metabolizer phenotype of debrisoquine. Drug oxidation phenotyping with dextromethorphan showed that this patient had the extensive metabolizer phenotype. This observation demonstrates that Amitriptyline can induce prolonged cholestasis and suggests that the susceptibility to develop liver injury while taking this drug may not be related to a genetic deficiency of its hydroxylation.
Amitriptyline's anticholinergic adverse drug reactions-A systematic multiple-indication review and meta-analysis
PLoS One 2023 Apr 5;18(4):e0284168.PMID:37018325DOI:10.1371/journal.pone.0284168.
Background: Half the US population uses drugs with anticholinergic properties. Their potential harms may outweigh their benefits. Amitriptyline is among the most frequently prescribed anticholinergic medicinal products, is used for multiple indications, and rated as strongly anticholinergic. Our objective was to explore and quantify (anticholinergic) adverse drug reactions (ADRs) in patients taking Amitriptyline vs. placebo in randomized controlled trials (RCTs) involving adults and healthy individuals. Methods: We searched electronic databases from their inception until 09/2022, and clinical trial registries from their inception until 09/2022. We also performed manual reference searches. Two independent reviewers selected RCTs with ≥100 participants of ≥18 years, that compared Amitriptyline (taken orally) versus placebo for all indications. No language restrictions were applied. One reviewer extracted study data, ADRs, and assessed study quality, which two others verified. The primary outcome was frequency of anticholinergic ADRs as a binary outcome (absolute number of patients with/without anticholinergic ADRs) in Amitriptyline vs. placebo groups. Results: Twenty-three RCTs (mean dosage 5mg to 300mg Amitriptyline/day) and 4217 patients (mean age 40.3 years) were included. The most frequently reported anticholinergic ADRs were dry mouth, drowsiness, somnolence, sedation, fatigue, constitutional, and unspecific anticholinergic ADRs. Random-effects meta-analyses showed anticholinergic ADRs had a higher odd's ratio for Amitriptyline versus placebo (OR = 7.41; [95% CI, 4.54 to 12.12]). Non-anticholinergic ADRs were as frequent for Amitriptyline as placebo. Meta-regression analysis showed anticholinergic ADRs were not dose-dependent. Discussion: The large OR in our analysis shows that ADRs indicative of anticholinergic activities can be attributed to Amitriptyline. The low average age of participants in our study may limit the generalizability of the frequency of anticholinergic ADRs in older patients. A lack of dose-dependency may reflect limited reporting of the daily dosage when the ADRs occurred. The exclusion of small studies (<100 participants) decreased heterogeneity between studies, but may also have reduced our ability to detect rare events. Future studies should focus on older people, as they are more susceptible to anticholinergic ADRs. Registration: PROSPERO: CRD42020111970.