ZK 91296, an anticonvulsant beta-carboline which lacks muscle relaxant properties. 1985

T Klockgether, and M Schwarz, and L Turski, and K H Sontag

ZK 91296, a newly synthesised beta-carboline with partial agonistic activity at the benzodiazepine receptor raised the threshold current necessary to elicit electroconvulsions in mice. This effect was dose-dependent and could be reversed by Ro 15-1788. ZK 91296 antagonised the anticonvulsant action of diazepam, but potentiated that of phenobarbitone. ZK 91296 protected mice from DMCM-induced seizures with high potency, this effect being benzodiazepine specific. In mutant rats exhibiting an increased muscle tone of the hindlimbs, ZK 91296 was devoid of muscle relaxant effect and antagonised the muscle relaxant action of both diazepam and phenobarbitone. The latter effect could be blocked by Ro 15-1788. The results suggest that the actions of ZK 91296 are only partly due to its partial agonistic properties at the benzodiazepine receptor.

UI MeSH Term Description Entries
D007211 Indoles Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
D008297 Male Males
D008815 Mice, Inbred Strains Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations, or by parent x offspring matings carried out with certain restrictions. All animals within an inbred strain trace back to a common ancestor in the twentieth generation. Inbred Mouse Strains,Inbred Strain of Mice,Inbred Strain of Mouse,Inbred Strains of Mice,Mouse, Inbred Strain,Inbred Mouse Strain,Mouse Inbred Strain,Mouse Inbred Strains,Mouse Strain, Inbred,Mouse Strains, Inbred,Strain, Inbred Mouse,Strains, Inbred Mouse
D009119 Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments. Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D009125 Muscle Relaxants, Central A heterogeneous group of drugs used to produce muscle relaxation, excepting the neuromuscular blocking agents. They have their primary clinical and therapeutic uses in the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. They have been used also for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in MULTIPLE SCLEROSIS. (From Smith and Reynard, Textbook of Pharmacology, 1991, p358) Centrally Acting Muscle Relaxants,Central Muscle Relaxants,Relaxants, Central Muscle
D009129 Muscle Tonus The state of activity or tension of a muscle beyond that related to its physical properties, that is, its active resistance to stretch. In skeletal muscle, tonus is dependent upon efferent innervation. (Stedman, 25th ed) Muscle Tension,Muscle Tightness,Muscular Tension,Tension, Muscle,Tension, Muscular,Tightness, Muscle,Tonus, Muscle
D010634 Phenobarbital A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations. Phenemal,Phenobarbitone,Phenylbarbital,Gardenal,Hysteps,Luminal,Phenobarbital Sodium,Phenobarbital, Monosodium Salt,Phenylethylbarbituric Acid,Acid, Phenylethylbarbituric,Monosodium Salt Phenobarbital,Sodium, Phenobarbital
D011919 Rats, Inbred Strains Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding. August Rats,Inbred Rat Strains,Inbred Strain of Rat,Inbred Strain of Rats,Inbred Strains of Rats,Rat, Inbred Strain,August Rat,Inbred Rat Strain,Inbred Strain Rat,Inbred Strain Rats,Inbred Strains Rat,Inbred Strains Rats,Rat Inbred Strain,Rat Inbred Strains,Rat Strain, Inbred,Rat Strains, Inbred,Rat, August,Rat, Inbred Strains,Rats Inbred Strain,Rats Inbred Strains,Rats, August,Rats, Inbred Strain,Strain Rat, Inbred,Strain Rats, Inbred,Strain, Inbred Rat,Strains, Inbred Rat
D002243 Carbolines A group of pyrido-indole compounds. Included are any points of fusion of pyridine with the five-membered ring of indole and any derivatives of these compounds. These are similar to CARBAZOLES which are benzo-indoles. Carboline,Pyrido(4,3-b)Indole,Beta-Carbolines,Pyrido(4,3-b)Indoles,Beta Carbolines
D003292 Convulsants Substances that act in the brain stem or spinal cord to produce tonic or clonic convulsions, often by removing normal inhibitory tone. They were formerly used to stimulate respiration or as antidotes to barbiturate overdose. They are now most commonly used as experimental tools. Convulsant,Convulsant Effect,Convulsant Effects,Effect, Convulsant,Effects, Convulsant

Related Publications

T Klockgether, and M Schwarz, and L Turski, and K H Sontag
July 1983, European journal of pharmacology,
T Klockgether, and M Schwarz, and L Turski, and K H Sontag
February 1987, The Journal of pharmacology and experimental therapeutics,
T Klockgether, and M Schwarz, and L Turski, and K H Sontag
July 1984, European journal of pharmacology,
T Klockgether, and M Schwarz, and L Turski, and K H Sontag
January 1986, Brain research,
T Klockgether, and M Schwarz, and L Turski, and K H Sontag
May 1987, Journal of neurochemistry,
T Klockgether, and M Schwarz, and L Turski, and K H Sontag
January 1984, Psychopharmacology,
T Klockgether, and M Schwarz, and L Turski, and K H Sontag
November 1987, European journal of pharmacology,
T Klockgether, and M Schwarz, and L Turski, and K H Sontag
April 1987, Life sciences,
T Klockgether, and M Schwarz, and L Turski, and K H Sontag
May 1987, Neuropharmacology,
T Klockgether, and M Schwarz, and L Turski, and K H Sontag
March 1961, Archives internationales de pharmacodynamie et de therapie,
Copied contents to your clipboard!