1,4-Diaminobutane-d8 dihydrochloride is the deuterium-substituted 1,4-Diaminobutane dihydrochloride, which is more stable and largely as tracer for quantitation during the drug development process[1]. 1,4-Diaminobutane-d8 dihydrochloride is an endogenous metabolite, acts as an indicator of pollution-induced stress in higher plants[2]. 1,4-Diaminobutane-d8 dihydrochloride can be used as an internal standard in LC-MS/MS for the quantification of polyamines in biological samples[3].
1,4-Diaminobutane-d8 dihydrochloride (100-1000μM; 24h) promotes the growth of CT-26 tumor cells[4]. 1,4-Diaminobutane-d8 dihydrochloride (0-50mM; 2h) protected against oxidative stress induced by polymyxin B (PmB; 1mg/ml) in Burkholderia cenocepacia, resulted in increased ROS generation and a parallel increased sensitivity to PmB[5].
1,4-Diaminobutane-d8 dihydrochloride (0.1-100mg/kg; i.p. ; 30min) significantly decreased the immobility time in mice in the forced swimming test (FST), which produces a antidepressant-like effect[6]. 1,4-Diaminobutane-d8 dihydrochloride (200-400mg/kg; i.p. ; 30, 60, 90, 120, 150, 180, 210 and 240min) has dose dependent analgesic activity in rats in hot plate test (55.5±0.1℃), to which tolerance develops[7].
References:
[1] RUSSAK E M, BEDNARCZYK E M. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals [J]. Ann Pharmacother, 2019, 53(2): 211-6.
[2] SEQUERRA E B, GARDINO P, HEDIN-PEREIRA C, et al. Putrescine as an important source of GABA in the postnatal rat subventricular zone [J]. Neuroscience, 2007, 146(2): 489-93.
[3] HAKKINEN M R, ROINE A, AURIOLA S, et al. Analysis of free, mono- and diacetylated polyamines from human urine by LC-MS/MS [J]. J Chromatogr B Analyt Technol Biomed Life Sci, 2013, 941(81-9.
[4] FARRIOL M, SEGOVIA-SILVESTRE T, CASTELLANOS J M, et al. Role of putrescine in cell proliferation in a colon carcinoma cell line [J]. Nutrition, 2001, 17(11-12): 934-8.
[5] EL-HALFAWY O M, VALVANO M A. Putrescine reduces antibiotic-induced oxidative stress as a mechanism of modulation of antibiotic resistance in Burkholderia cenocepacia [J]. Antimicrob Agents Chemother, 2014, 58(7): 4162-71.
[6] ZOMKOWSKI A D, SANTOS A R, RODRIGUES A L. Putrescine produces antidepressant-like effects in the forced swimming test and in the tail suspension test in mice [J]. Prog Neuropsychopharmacol Biol Psychiatry, 2006, 30(8): 1419-25.
[7] GENEDANI S, PICCININI G, BERTOLINI A. Putrescine has analgesic activity, in rats [J]. Life Sci, 1984, 34(24): 2407-12.
1,4-Diaminobutane-d8 dihydrochloride是氘取代的1,4-Diaminobutane dihydrochloride,它更稳定,在药物开发过程中主要用作定量示踪剂[1]。1,4-Diaminobutane-d8 dihydrochloride是一种内源代谢物,在高等植物中作为污染诱导胁迫的指示物[2]。1,4-Diaminobutane-d8 dihydrochloride可作为LC-MS/MS定量生物样品中多胺的内标定物[3]。
1,4-Diaminobutane-d8 dihydrochloride(100-1000μM; 24h)促进CT-26肿瘤细胞生长[4]。1,4-Diaminobutane-d8 dihydrochloride(0-50mM; 2h)对多粘菌素B(PmB, 1mg/ml)诱导的洋葱伯克霍尔德菌的氧化应激有保护作用,导致ROS生成增加,同时对PmB的敏感性增加[5]。
使用1,4-Diaminobutane-d8 dihydrochloride (0.1-100mg/kg; i.p; 30min)处理小鼠,1,4-Diaminobutane-d8 dihydrochloride显著减少小鼠在FST(forced swimming test,强迫游泳试验)中的静止时间,产生抗抑郁样作用[6]。使用1,4-Diaminobutane-d8 dihydrochloride(200-400mg/kg; i.p. ; 30, 60, 90, 120, 150, 180, 210 and 240min)处理进行55.5±0.1℃热板实验的大鼠,1,4-Diaminobutane-d8 dihydrochloride对大鼠有剂量依赖性镇痛活性,并产生耐受[7]。
















