ZK 91296, a partial agonist at benzodiazepine receptors.

Abstract

5-benzyloxy-4-methoxymethyl-beta-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 sedative 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.

• Authors: E N Petersen, L H Jensen, T Honoré, C Braestrup, W Kehr, D N Stephens, H Wachtel, D Seidelman, R Schmiechen
• Journal: Psychopharmacology (Psychopharmacology (Berl)) Vol. 83 Issue 3 Pg. 240-8 ( 1984) ISSN: 0033-3158 [Print] Germany
• PMID: 6089246 (Publication Type: Journal Article)

Chemical References

• Anticonvulsants
• Carbolines
• Indoles
• Receptors, Cell Surface
• Receptors, GABA-A
• Receptors, Neurotransmitter
• ZK 91296

Topics

• Animals
• Anticonvulsants (pharmacology)
• Behavior, Animal (drug effects)
• Binding, Competitive
• Brain Chemistry (drug effects)
• Carbolines (pharmacology)
• Indoles (pharmacology)
• Male
• Mice
• Mice, Inbred DBA
• Organ Specificity
• Rats
• Rats, Inbred Strains
• Receptors, Cell Surface (drug effects)
• Receptors, GABA-A
• Receptors, Neurotransmitter (drug effects)
• Synaptosomes (metabolism)