Amitriptyline-d6 hydrochloride
Amitriptyline-d6 (hydrochloride) 是 Amitriptyline hydrochloride 的氘代物。Amitriptyline hydrochloride 是一种血清素再摄取转运体 (SERT) 和去甲肾上腺素再摄取转运体 (NET) 抑制剂，对人的 SERT 和 NET 作用的 Ki 值分别为 3.45 nM 和 13.3 nM。Amitriptyline hydrochloride 还与多巴胺再摄取转运体 (DAT) 结合，其 Ki 为 2.58 μM。Amitriptyline hydrochloride 也抑制肾上腺素能受体 (adrenergic receptor)、毒蕈碱受体 (muscarinic receptor )、组胺受体 (histamine receptor )、5-羟色胺受体 (5-HT receptor)。Amitriptyline hydrochloride 是一种具有强神经营养活性的 TrkA 和 TrkA 受体激动剂。Amitriptyline hydrochloride 具有抗抑郁作用。
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包装价格促销价数量
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1mg￥1537.001230.00- +
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5mg￥3737.002990.00- +
- 货号: ajcf35288
- CAS: 203645-63-0
- 别名: 盐酸阿米替林 d6 (盐酸盐
- 分子式: C20H18D6ClN
- 分子量: 319.9
- 纯度: ＞98%
- 溶解度: DMSO: ≥100 mg/mL (312.60 mM); H<sub>2</sub>O: ≥50 mg/mL (156.30 mM)
- 储存: 4°C, sealed storage, away from moisture and light
- 库存: 现货
Background
Amitriptyline-d6 (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity[1][2][3].
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
参考文献:
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Kim Lawson. A Brief Review of the Pharmacology of Amitriptyline and Clinical Outcomes in Treating Fibromyalgia. Biomedicines. 2017 Jun; 5(2): 24.
[3]. S Neil Vaishnavi , et al. Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity. Biol Psychiatry. 2004 Feb 1;55(3):320-2.
[4]. Jang, S.W., et al., Amitriptyline is a TrkA and TrkB receptor agonist that promotes TrkA/TrkB heterodimerization and has potent neurotrophic activity. Chem Biol, 2009. 16(6): p. 644-56.
