Neurinostat is a histone deacetylase (HDAC) inhibitor and possible cognitive enhancer.
Pharmacology + Enzyme (nM) HDAC1 1.1 HDAC2 10.8 HDAC3 0.8 HDAC4 HDAC5 HDAC6 0.5 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 Refs:
Neurinostat is a histone deacetylase (HDAC) inhibitor and potently inhibits the class I HDAC1, HDAC2, and HDAC3 and the class IIb HDAC6, with values of 0.5 to 10.8nM at the preceding HDACs, whereas no activity against the class IIa HDAC5 was observed. Activities at the class I HDAC8 and at the class IIb HDAC4, HDAC7, and HDAC9 were not assessed nor described. The pharmacokinetics of neurinostat in rodents have been studied.
Chemistry The chemical synthesis of neurinostat has been described. A notable analogue of neurinostat is crebinostat.
History Neurinostat was first described in the scientific literature by 2016. It was derived via structural modification of the earlier HDAC inhibitor crebinostat and differs from this compound only in the replacement of a phenyl ring with a pyridine ring. The drug shows enhanced potency as well as modestly improved pharmacokinetics compared to crebinostat. In addition, while potency against HDAC1 and HDAC3 was increased, neurinostat showed reduced potency at HDAC2 compared to crebinostat, thus having around 10- to 14-fold selectivity for HDAC1 and HDAC3 over HDAC2.
See also Histone deacetylase inhibitor Crebinostat Synapsinostat Vorinostat
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