Histamine dihydrochloride (Ceplene) is a synthetic derivative of the biogenic amine histamine. Histamine dihydrochloride inhibits the formation of reactive oxygen species (ROS) that suppress the activation of T cells and natural killer cells. Histamine dihydrochloride and IL-2 as maintenance therapy significantly prolonged LFS (longer leukaemia-free survival) compared with no treatment and had an acceptable tolerability profile in a large phase III trial in patients with AML (acute myeloid leukaemia)[3]. Clinical trials in solid tumors and in AML have demonstrated the potential to improve treatment outcome when histamine dihydrochloride is combined with immunotherapy[4]. In vitro ROS detection assays proved that the HDC (histamine dihydrochloride) loaded graphene nanoplatform could effectively inhibit ROS and thus prevent the immunosuppression caused by leukemic cells[5].
Histamine 2HCl/二盐酸组胺 细胞实验
Cell Line
Concentration
Treated Time
Description
References
human airway smooth muscle cells
10 μM
~127 seconds delay before shortening
Study histamine-induced cell contraction and shortening
ACS Nano. 2021 Jul 27;15(7):11585-11596
HEK293T cells
2.5 μM
30 minutes
Identified CG1358 (HisT) as a histamine-specific transporter, whose transport activity is Na+-dependent but Cl−-independent, and highly specific to histamine
Sci Adv. 2022 Oct 28;8(43):eabq1780
CINs (cholinergic interneurons)
10 μM
To assess the effects of histamine on CIN excitability, results showed histamine significantly increased spontaneous firing frequency of CINs
To assess the effects of histamine on PV-IN excitability and resting membrane potential, results showed no significant effect of histamine on PV-IN excitability or resting membrane potential
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