Disease relevance of CAS 997

• Tenilsetam prevents early diabetic retinopathy without correcting pericyte loss [1].
• Tenilsetam did not affect glycemic control or body weight in diabetic animals [1].
• Candidates are selegiline, a MAO-B inhibitor well established in the therapy of Parkinson's disease, and tenilsetam, which is believed to be an AGE-inhibitor [2].
• Pre-incubation of methylglyoxal with a variety of carbonyl scavengers such as aminoguanidine or tenilsetam and the thiol antioxidant lipoic acid significantly reduced its toxicity [3].

Psychiatry related information on CAS 997

• These experimental data, and clinical studies, reporting a marked improvement in cognition and memory in Alzheimer's disease patients after Tenilsetam treatment, suggest that AGEs might play an important role in the etiology or progression of the disease [4].

High impact information on CAS 997

• The impact of tenilsetam (0-30 mM) on endothelial proliferation, apoptosis, sprouting, cytokine-induced leucocyte-endothelial interaction, and VEGF expression was tested in vitro [1].
• In vitro, tenilsetam inhibited endothelial proliferation at lower doses, while inducing apoptosis at high doses [1].
• Long-term treatment with the AGE-inhibitor and iron-chelating compound tenilsetam inhibits the formation of acellular capillaries without correcting pericyte loss [1].
• Streptozotocin diabetic male Wistar rats (60 mg/kg BW) received 50 mg/kg BW tenilsetam (D-T) for 36 weeks, or no treatment (D) [1].
• These data suggest that, independent of known properties, tenilsetam shows important rescue functions on endothelial cells which could be useful for the treatment of early diabetic retinopathy [1].

Biological context of CAS 997

• The cognition-enhancing drug tenilsetam is an inhibitor of protein crosslinking by advanced glycosylation [5].
• According to the mechanism proposed, Tenilsetam acts via covalent attachment to glycated proteins, thus blocking the reactive sites for further polymerisation reactions [5].

Anatomical context of CAS 997

• A beneficial effect of Tenilsetam in Alzheimer's disease could come from the interference with AGE-derived crosslinking of amyloid plaques and a decreased inflammatory response by diminished activation of phagocytosing microglia [5].

Associations of CAS 997 with other chemical compounds

• The formation of AGE crosslinks as a result of the Maillard reaction is reduced by several drugs (aminoguanidine, OPB-9195, tenilsetam, aspirin), substances of natural origin (carnosine, homocarnosine) and antioxidants [6].

Gene context of CAS 997

• At weekly intervals, the subjects received randomized single oral doses of placebo, 150 mg, 300 mg and 900 mg tenilsetam (TEN) and 5 mg co-dergocrine-mesylate (CDM) as reference drug [7].

Analytical, diagnostic and therapeutic context of CAS 997

• Determination of tenilsetam in human plasma and urine by high-performance liquid chromatography [8].

References