Nicotinamide riboside (NR) is in wide use as an NAD +
precursor vitamin. Here we determine the time and dose-dependent effects of NR
on blood NAD + metabolism in humans. We report that human blood NAD + can rise
as much as 2.7-fold with a single oral dose of NR in a pilot study of one
individual, and that oral NR elevates mouse hepatic NAD + with distinct and
superior pharmacokinetics to those of nicotinic acid and nicotinamide. We
further show that single doses of 100, 300 and 1,000 mg of NR produce
dose-dependent increases in the blood NAD + metabolome in the first clinical
trial of NR pharmacokinetics in humans. We also report that nicotinic acid
adenine dinucleotide (NAAD), which was not thought to be en route for the
conversion of NR to NAD +, is formed from NR and discover that the rise in NAAD
is a highly sensitive biomarker of effective NAD + repletion.
Talabostat mesylate is the orally bioavailable mesylate salt of an amino boronic dipeptide with antineoplastic and hematopoiesis- stimulating activities. By cleaving N-terminal Xaa-Pro or Xaa-Ala residues, talabostat inhibits dipeptidyl peptidases, such as fibroblast activation protein (FAP), resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell- dependent activity. Talabostat mesylate
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