Gabazin
| Structural formula | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|||||||||||||
| General | |||||||||||||
| Surname | Gabazin | ||||||||||||
| other names |
2- (3-carboxypropyl) -3-amino-6- (4 methoxyphenyl) pyridazinium bromide |
||||||||||||
| Molecular formula | C 15 H 17 N 3 O 3 • HBr | ||||||||||||
| Brief description |
White dust |
||||||||||||
| External identifiers / databases | |||||||||||||
|
|||||||||||||
| properties | |||||||||||||
| Molar mass | 368.23 g mol −1 | ||||||||||||
| Physical state |
firmly |
||||||||||||
| solubility |
soluble in water at 25 mM and DMSO at 100 mM |
||||||||||||
| safety instructions | |||||||||||||
|
|||||||||||||
| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | |||||||||||||
Gabazine ( SR-95531 ) is a selective, potent allosteric GABA A receptor - antagonist , which, today from Sanofi Research Sanofi was developed in 1986 and presented.
effect
Similar to other GABA A receptor antagonists, e.g. B. Picrotoxin and Bicuculline it has a convulsive and exciting effect on the nervous system . Applied in the mouse , it causes a tonic-clonic seizure .
Gabazine reduces the GABA-mediated synaptic inhibitory chloride current into the cell. This prevents inhibitory hyperpolarization and gabazin has an effective excitatory effect. Gabazin acts more selectively on the GABA A receptor than other blockers. For example, it can only partially inhibit currents triggered by barbiturates and steroids (such as pentobarbital and alphaxalone ). It replaces GABA with a dissociation constant of K i = 150 nM.
application
Gabazine is used in basic research similar to other GABA receptor antagonists, for example the plant toxins picrotoxin from the pseudo myrtle and bicuculline from the heart flowers .
See also
- Strychnine
- The pharmaceuticals baclofen and muscimol , one of the toxins in the toadstool, are GABA agonists .
Individual evidence
- ↑ a b c Datasheet Gabazin from Sigma-Aldrich , accessed on October 9, 2014 ( PDF ).
- ↑ Tocris: Gabazine , accessed October 9, 2014.
- ↑ M. Heaulme, JP Chambon, R. Leyris, JC Molimard, CG Wermuth, K. Biziere: Biochemical characterization of the interaction of three pyridazinyl-GABA derivatives with the GABAA receptor site . In: Brain Research . tape 384 , no. 2 , October 1986, p. 224-231 , PMID 3022866 .
- ^ A b S. Ueno, J. Bracamontes, C. Zorumski, DS Weiss, JH Steinbach: Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor . In: The Journal of Neuroscience: The Official Journal of the Society for Neuroscience . tape 17 , no. 2 , January 15, 1997, p. 625-634 , PMID 8987785 .
- ↑ CJ Behrens, LP van den Boom, U. Heinemann: Effects of the GABA (A) receptor antagonists bicuculline and gabazine on stimulus-induced sharp wave-ripple complexes in adult rat hippocampus in vitro . In: The European Journal of Neuroscience . tape 25 , no. 7 , 2007, p. 2170-2181 , doi : 10.1111 / j.1460-9568.2007.05462.x , PMID 17419756 .
