ZK 91296, a partial agonist at benzodiazepine receptors |
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Authors: | Petersen Erling N Jensen Leif H Honoré Tage Braestrup Claus Kehr Wolfgang Stephens David N Wachtel Helmuth Seidelman Dieter Schmiechen Ralph |
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Institution: | (1) A/S Ferrosan Research Division, Sydmarken 5, DK-2860 Soeborg, Denmark;(2) Schering AG, Berlin and Bergkamen, FRG |
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Abstract: | ZK 91296 (ethyl 5-benzyloxy-4-methoxymethyl- -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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Keywords: | Benzodiazepine receptors -Carboline-3-carboxylates" target="_blank">gif" alt="beta" align="MIDDLE" BORDER="0">-Carboline-3-carboxylates Anxiety Epilepsy Ataxia Rat Mouse |
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