Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2012/12/25 15:01:56」(JST)
[Wiki en表示]
Gabazine
|
Systematic (IUPAC) name |
4-[6-imino-3-(4-methoxyphenyl)pyridazin-1-yl] butanoic acid hydrobromide |
Clinical data |
Pregnancy cat. |
? |
Legal status |
? |
Identifiers |
CAS number |
104104-50-9 |
ATC code |
None |
PubChem |
CID 107895 |
ChemSpider |
4925141 Y |
ChEMBL |
CHEMBL303580 Y |
Chemical data |
Formula |
C15H18BrN3O3 |
Mol. mass |
368.226 |
SMILES
- [Br-].O=C(O)CCC[n+]2nc(c1ccc(OC)cc1)ccc2N
|
InChI
-
InChI=1S/C15H17N3O3.BrH/c1-21-12-6-4-11(5-7-12)13-8-9-14(16)18(17-13)10-2-3-15(19)20;/h4-9,16H,2-3,10H2,1H3,(H,19,20);1H Y
Key:GFZHNFOGCMEYTA-UHFFFAOYSA-N Y
|
Y (what is this?) (verify)
|
Gabazine (SR-95531) is a drug that acts as an antagonist at GABAA receptors. It is used in scientific research and has no role in medicine, as it would be expected to produce convulsions if used in humans.[1]
Gabazine binds to the GABA recognition site of the receptor-channel complex and acts as an allosteric inhibitor of channel opening.[2] The net effect is to reduce GABA-mediated synaptic inhibition by inhibiting chloride flux across the cell membrane, and thus inhibiting neuronal hyperpolarization. While phasic (synaptic) inhibition is gabazine-sensitive, tonic (extrasynaptic) inhibition is relatively gabazine-insensitive.[3]
References
- ^ Behrens, CJ; Van Den Boom, LP; Heinemann, U (2007). "Effects of the GABA(A) receptor antagonists bicuculline and gabazine on stimulus-induced sharp wave-ripple complexes in adult rat hippocampus in vitro". The European Journal of Neuroscience 25 (7): 2170–81. doi:10.1111/j.1460-9568.2007.05462.x. PMID 17419756.
- ^ Ueno, S; Bracamontes, J; Zorumski, C; Weiss, DS; Steinbach, JH (1997). "Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor". The Journal of neuroscience : the official journal of the Society for Neuroscience 17 (2): 625–34. PMID 8987785.
- ^ Yeung, JY; Canning, KJ; Zhu, G; Pennefather, P; MacDonald, JF; Orser, BA (2003). "Tonically activated GABAA receptors in hippocampal neurons are high-affinity, low-conductance sensors for extracellular GABA". Molecular Pharmacology 63 (1): 2–8. PMID 12488530.
GABAergics
|
|
Receptor
ligands |
GABAA
|
- Agonists: Main site: Bamaluzole
- Gaboxadol
- Ibotenic acid
- Isoguvacine
- Isonipecotic acid
- Muscimol (Amanita Muscaria)
- Progabide
- SL 75102
- Thiomuscimol
- Tolgabide; Positive allosteric modulators: Barbiturates
- Benzodiazepines
- Carbamates
- Chlormezanone
- Clomethiazole
- Ethanol (Alcohol)
- Etomidate
- Kavalactones (Kava)
- Loreclezole
- Metomidate
- Neuroactive steroids
- Nonbenzodiazepines (β-Carbolines, Cyclopyrrolones, Imidazopyridines, Pyrazolopyrimidines, etc.)
- Phenols
- Piperidinediones
- Propanidid
- Pyrazolopyridines
- Quinazolinones
- ROD-188
- Skullcap
- Stiripentol
- Valerenic acid (Valerian)
Note: See the GABAA receptor PAMs navbox for a full list of GABAA positive allosteric modulators.
- Antagonists: Main site: Bicuculline
- Gabazine
- Pitrazepin
- Quisqualamine; Negative allosteric modulators: α5IA
- Bilobalide
- Cicutoxin
- Cyclothiazide
- DMCM
- Flumazenil
- Flurothyl
- Furosemide
- Iomazenil (123I)
- L-655,708
- Oenanthotoxin
- Penicillin
- Pentylenetetrazol
- Picrotoxin
- PWZ-029
- Radequinil
- Ro15-4513
- Sarmazenil
- Suritozole
- Terbequinil
- Thujone
- Thiocolchicoside
- ZK-93426
|
|
GABAB
|
- Agonists: Main site: 1,4-Butanediol
- Baclofen
- GBL
- GHB
- GHV
- GVL
- Lesogaberan
- Phenibut
- Progabide
- SKF-97,541
- Tolgabide; Positive allosteric modulators: BHF-177
- BHFF
- BSPP
- CGP-7930
- GS-39783
Antagonists: Main site: CGP-35348
- Phaclofen
- Saclofen
- SCH-50911
|
|
GABAC
|
- Agonists: Main site: CACA
- CAMP
- GABOB
- N4-Chloroacetylcytosine arabinoside
- Progabide
- Tolgabide
Antagonists: Main site: Bilobalide
- TPMPA
|
|
|
Reuptake
inhibitors |
Plasmalemmal
|
GAT inhibitors
|
- CI-966
- Deramciclane
- EF-1502
- Gabaculine
- Guvacine
- Nipecotic acid
- NNC 05-2090
- SKF-89976A
- SNAP-5114
- Tiagabine
|
|
|
|
Enzyme
inhibitors |
Anabolism
|
|
|
Catabolism
|
GABA-T inhibitors
|
- 3-Hydrazinopropionic acid
- Aminooxyacetic acid
- Gabaculine
- Isoniazid
- Phenelzine
- Phenylethylidenehydrazine
- Sodium valproate
- Valnoctamide
- Valproate pivoxil
- Valproate semisodium (Divalproex sodium)
- Valproic acid
- Valpromide
- Vigabatrin
|
|
|
|
Others |
Precursors
|
|
|
Cofactors
|
- Vitamin B6 (pyridoxine
- pyridoxamine
- pyridoxal phosphate)
|
|
Others
|
- Gabapentin
- Hopantenic acid
- Picamilon
- Pregabalin
- L-Theanine
|
|
|
English Journal
- Differential Roles of GABAergic and Glycinergic Input on FM Selectivity in the Inferior Colliculus of the Pallid Bat.
- Williams AJ, Fuzessery ZM.Source1University of Wyoming.
- Journal of neurophysiology.J Neurophysiol.2011 Jul 20. [Epub ahead of print]
- Multiple mechanisms have been shown to shape FM selectivity within the central nucleus of the inferior colliculus (IC) in the pallid bat. Here we focus on the mechanisms associated with sideband inhibition. The relative arrival time of inhibition as compared to excitation can be used to predict FM r
- PMID 21775712
Japanese Journal
- 明期ラット海馬スライスにおいてカルバコール誘導β振動は出にくくなる(一般,ニューロコンピューティングの実装とシステム化,一般)
- 中司 弘樹,夏目 季代久
- 電子情報通信学会技術研究報告. NC, ニューロコンピューティング 110(246), 1-4, 2010-10-16
- … この差は、GABA_A阻害薬である、Gabazineによって消失した。 … しかし、Gabazineは、周波数など、他のパラメータには影響を及ぼさなかった。 …
- NAID 110008106473
Related Links
- Gabazine (SR-95531) is a drug that acts as an antagonist at GABAA receptors. It is used in scientific research and has no role in medicine, as it would be expected to produce convulsions if used in humans. Gabazine binds to the GABA ...
Related Pictures