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ZK 91296, a partial agonist at benzodiazepine receptors

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Abstract

ZK 91296 (ethyl 5-benzyloxy-4-methoxymethyl-β-carboline-3-carboxylate) is a potent and selective ligand for benzodiazepine (BZ) receptors. Biochemical investigations indicate that ZK 91296 may be a partial agonist at BZ receptors. Such partial agonism may explain to some extent why ZK 91296 needs higher BZ receptor occupancy than diazepam for the same effect against chemical convulsants and for behavioural effects. The lack of sedatiye effects, and the very potent inhibition of reflex epilepsy, spontaneous epilepsy and DMCM-induced seizures suggest, furthermore, that ZK 91296 may possess pharmacological selectivity for a particular type of BZ receptor interaction, perhaps including topographic as well as receptor subtype differentiation.

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Authors and Affiliations

  1. A/S Ferrosan Research Division, Sydmarken 5, DK-2860, Soeborg, Denmark

    Erling N. Petersen, Leif H. Jensen, Tage Honoré & Claus Braestrup

  2. Schering AG, Berlin and Bergkamen, FRG

    Wolfgang Kehr, David N. Stephens, Helmuth Wachtel, Dieter Seidelman & Ralph Schmiechen

Authors
  1. Erling N. Petersen
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  2. Leif H. Jensen
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  3. Tage Honoré
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  4. Claus Braestrup
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  5. Wolfgang Kehr
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  6. David N. Stephens
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  7. Helmuth Wachtel
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  8. Dieter Seidelman
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  9. Ralph Schmiechen
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Petersen, E.N., Jensen, L.H., Honoré, T. et al. ZK 91296, a partial agonist at benzodiazepine receptors. Psychopharmacology 83, 240–248 (1984). https://doi.org/10.1007/BF00464788

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  • DOI: https://doi.org/10.1007/BF00464788

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