HT-2157 (former development code SNAP-37889) is a drug which acts as a selective non-peptide
antagonist for the receptor
GAL-3, which is usually activated by the
neuropeptide
Neuropeptides are chemical messengers made up of small chains of amino acids that are synthesized and released by neurons. Neuropeptides typically bind to G protein-coupled receptors (GPCRs) to modulate neural activity and other tissues like the ...
galanin
Galanin is a neuropeptide encoded by the ''GAL'' gene, that is widely expressed in the brain, spinal cord, and gut of humans as well as other mammals. Galanin signaling occurs through three G protein-coupled receptors.
Much of galanin's function ...
. Blocking this receptor with HT-2157 produced increased
serotonin release, as well as producing
antidepressant and
anxiolytic
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiet ...
effects in animal studies, and it was also being researched for treatment of
cognitive dysfunction
Cognitive disorders (CDs), also known as neurocognitive disorders (NCDs), are a category of mental health disorders that primarily affect cognitive abilities including learning, memory, perception, and problem solving. Neurocognitive disorders i ...
.
All human clinical trials were terminated due to safety concerns however, and new GAL-3 antagonists are now being sought instead.
References
Peptides
Receptor antagonists
Abandoned drugs
Trifluoromethyl compounds
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