Supply Gts-21 CAS: 156223-05-1 Nootropics

GTS-21 dihydrochloride is a selectiv α7 nicotinic acetylcholin receptor (α7-nAChR) agonist with anti-inflammatory and cognitive enhancing activities. GTS-21 dihydrochloride is also an α4β2 (human α4β2: Ki=20 nM) and 5-HT3A receptor (IC50=3.1 μM) antagonist.

GTS-21, also known as DMXB-A, is a synthetic compound and a selective α7 nicotinic acetylcholine receptor (α7nAChR) partial agonist.

GTS-21 is known for its interaction with α7 nicotinic receptors in the brain. α7nAChRs are involved in modulating neurotransmitter release, particularly the release of acetylcholine, and are linked to cognitive processes.

 GTS-21 (also known as DMBX-A), is a novel, small-molecule, orally active and selective
alpha-7 nicotinic acetylcholine (nACh) receptor agonist that has demonstrated memory and
cognition enhancement activity in human clinical trials. Athenagen licensed the exclusive
rights to the compound and a related library of analogs as part of the acquisition of Osprey
Pharmaceutical Company in April 2006. GTS-21 has been studied in multiple Phase I studies
in healthy volunteers and one Phase I/II study in schizophrenic patients. In all studies, the
compound was well tolerated. In a Phase I multi-dose, double-blind, placebo controlled study
in healthy adults, GTS-21 also demonstrated cognitive enhancement across all doses, with a
statistically significant improvement in attention related and memory related tasks.

    GTS-21 was O-demethylated to yield compounds that were then subject to glucuronidation.
Three of the metabolites in rat urine were isolated and characterized as 4-OH-GTS-21,
4-OH-GTS-21 glucuronide and 2-OH-GTS-21 glucuronide. The major urinary metabolites
were 4-OH-GTS-21 glucuronide and 2-OH-GTS-21 glucuronide. In vitro chemical inhibition
of cytochrome P450 in human liver microsomes indicated that CYPIA2 and CYP2E1 were the
isoforms primarily responsible for the O-demethylation of GTS-21, with some contribution from
CYP3A.