Navacaprant, a novel and selective kappa opioid receptor antagonist, has no agonist properties implicated in opioid-related abuse.

Filomene G Morrison¹, Lori Jean Van Orden¹, Karla Zeitz¹, Eloise J Kuijer², Sharon L Smith³, David J Heal⁴, Tanya L Wallace⁵

¹Neumora Therapeutics, Inc., 490 Arsenal Way, Watertown, MA, 02472, USA.

²Department of Life Sciences, University of Bath, Bath, BA2 7AY, UK.

³DevelRx Ltd., BioCity, Nottingham, NG1 1GF, UK.

⁴Department of Life Sciences, University of Bath, Bath, BA2 7AY, UK; DevelRx Ltd., BioCity, Nottingham, NG1 1GF, UK.

⁵Neumora Therapeutics, Inc., 490 Arsenal Way, Watertown, MA, 02472, USA. Electronic address: tanya.wallace@neumoratx.com.

PubMed DOI

Abstract

Kappa opioid receptors (KORs) are implicated in the pathophysiology of various psychiatric and neurological disorders creating interest in targeting the KOR system for therapeutic purposes. Accordingly, navacaprant (NMRA-140) is a potent, selective KOR antagonist being evaluated as a treatment for major depressive disorder. In the present report, we have extended the pharmacological characterizati…

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