Physics:PNV-001

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PNV-001, also known as deuterated basmisanil, is a highly selective α5 subunit-containing GABAA receptor negative allosteric modulator which is under investigation for the treatment of treatment-resistant depression and suicidal ideation.[1][2] It is a deuterated analogue of basmisanil with improved pharmacokinetics and metabolic stability.[2] The drug's half-life is 5.5-fold longer than that of basmisanil in human liver microsomes in vitro.[2] It produces rapid and persistent antidepressant-like effects in animals.[2] PNV-001 and related drugs are said to lack the undesirable central effects of hallucinogens like ketamine and serotonergic psychedelics and of non-subunit-selective GABAA receptor negative allosteric modulators like flumazenil.[2] It is being developed by ProNovo Therapeutics.[1] As of September 2023, it is in the preclinical research stage of development.[1]

See also

References

  1. 1.0 1.1 1.2 "Modulators of GABAA receptor-mediated inhibition in the treatment of neuropsychiatric disorders: past, present, and future". Neuropsychopharmacology 49 (1): 83–95. January 2024. doi:10.1038/s41386-023-01728-8. PMID 37709943. 
  2. 2.0 2.1 2.2 2.3 2.4 "P267. Development and evaluation of an α5 Subunit–Containing Gaba-A receptor selective nam as a rapid-acting antidepressant without the undesirable CNS effects of ketamine and psychedelics". Neuropsychopharmacology. ACNP 64th Annual Meeting: Poster Abstracts P1-P291 51 (Suppl 1): 74–242. January 2026. doi:10.1038/s41386-025-02279-w. PMID 41507444. 

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See also
Receptor/signaling modulators
GABAA receptor positive modulators
GABA metabolism/transport modulators

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