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Kenazepine is a benzodiazepine containing a functional alkylating moiety.[1] The chemical formula is C19H16BrClFN3O2.[2]

Uses

The compound functions as a research tool in pharmacology. It binds irreversibly and non-competitively to some brain benzodiazepine receptors and competitively to others, providing evidence for the existence of different receptor populations within the central nervous system. Kenazepine exhibits long-lasting anticonvulsant effects, likely due to its irreversible binding mechanism, and is used to study the heterogeneity and function of benzodiazepine receptors.[3]

Studies show that kenazepine provides a long-lasting protection against convulsions caused by pentylenetetrazole in vivo, suggesting a similar irreversible binding mechanism in the body.[2]

References

  1. ^ Skolnick P, Paul SM (1982). Benzodiazepine Receptors in the Central Nervous System. International Review of Neurobiology. Vol. 23. pp. 103–140 (115). doi:10.1016/S0074-7742(08)60623-6. ISBN 978-0-12-366823-3. PMID 6288605. Kenazepine , a derivative of the benzodiazepine Ro 7/1986 has a bromoacetyl moiety that can react with binucleophiles such as SH and – NH2.
  2. ^ a b Williams EF, Rice KC, Mattson M, Paul SM, Skolnick P (April 1981). “In vivo effects of two novel alkylating benzodiazepines, irazepine and kenazepine”. Pharmacology, Biochemistry, and Behavior. 14 (4): 487–91. doi:10.1016/0091-3057(81)90307-5. PMID 7232472.
  3. ^ Williams EF, Rice KC, Paul SM, Skolnick P (1980). “Heterogeneity of Benzodiazepine Receptors in the Central Nervous System Demonstrated with Kenazepine, an Alkylating Benzodiazepine”. Journal of Neurochemistry. 35 (3): 591–597. doi:10.1111/j.1471-4159.1980.tb03695.x. ISSN 1471-4159. PMID 6256492. Retrieved 14 September 2025.