NESS-0327

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NESS-0327 is a drug that acts as a potent and selective antagonist for the neurotensin receptor NTS1, and was the first non-peptide antagonist developed for this receptor. It is used in scientific research.

Pharmacology[edit | edit source]

NESS-0327 is a potent and selective antagonist for the NTS1 receptor, with a binding affinity of 0.2 nM, and over 100x selectivity over the related NTS2 receptor. It has a novel mechanism of action, binding to a site on the receptor distinct from the endogenous ligand binding site, and so is classed as an allosteric modulator. This makes it useful in scientific research into the function of the neurotensin system.

Chemistry[edit | edit source]

The chemical structure of NESS-0327 is a quinolinone derivative, and it was the first non-peptide antagonist developed for the NTS1 receptor. It is not orally active and must be administered by injection.

Research[edit | edit source]

Research into NESS-0327 has shown it to be a useful tool in the study of the neurotensin system, and it has potential applications in the treatment of certain types of cancer, as well as neurodegenerative diseases such as Parkinson's disease and Alzheimer's disease.

See also[edit | edit source]


NESS-0327 Resources

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Contributors: Prab R. Tumpati, MD