GABA antagonist

GABA antagonists are drugs which inhibit the action of GABA. In general these drugs produce stimulant and convulsant effects, and are mainly used for counteracting overdose of sedative drugs.

Examples include Bicuculline and Metrazol, and the benzodiazepine GABA_A receptor antagonist Flumazenil. Also Thujone has properties of GABA_A receptor antagonist.

External links

MeSH GABA+antagonists

Neuromodulation

Types

Enzyme: Inducer • Inhibitor
Ion channel: Opener • Blocker
Receptor: Agonist • Antagonist • Positive allosteric modulator (PAM) • Negative allosteric modulator (NAM) • Inverse agonist
Transporter [Reuptake]: Enhancer (RE) • Inhibitor (RI) • Releaser (RA)
Miscellaneous: Precursor • Cofactor

Classes

Enzyme

see Enzyme inhibition

Ion channel

Calcium channel blocker (CCB) • Potassium channel blocker (PCB) • Sodium channel blocker (SCB) • Potassium channel opener (PCO)

Receptor &
transporter

BA/M

Adrenergic	Adrenergic receptor agonist (α, β (1, 2)) • Adrenergic receptor antagonist (α (1, 2), β) • Adrenergic reuptake inhibitor (ARI)

Dopaminergic	Dopamine receptor agonist • Dopamine receptor antagonist • Dopamine reuptake inhibitor (DRI)

Histaminergic	Histamine receptor agonist • Histamine receptor antagonist (H₁, H₂, H₃)

Serotonergic	Serotonin receptor agonist • Serotonin Receptor Antagonist (5-HT₃) • Serotonin reuptake inhibitor (SRI) • Serotonin reuptake enhancer (SRE)


GABAergic	GABA receptor agonist • GABA receptor antagonist • GABA reuptake inhibitor (GRI)

Glutamatergic	Glutamate receptor agonist (AMPA) • Glutamate receptor antagonist (NMDA)

Cholinergic

Acetylcholine receptor agonist (Muscarinic, Nicotinic) • Acetylcholine receptor antagonist (Muscarinic, Nicotinic (Ganglionic, Muscular))

Endocannabinoid

Cannabinoid receptor agonist • Cannabinoid receptor antagonist

Opioid

Opioid receptor agonist • Opioid receptor antagonist

Other

Adenosine reuptake inhibitor (AdoRI) • Angiotensin II receptor antagonist • Endothelin receptor antagonist • NK₁ receptor antagonist • Vasopressin receptor antagonist

Miscellaneous

Cofactor (see Enzyme cofactors) • Precursor (see Amino acids)

GABAergics

Receptor
ligands

GABA_A	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) * See Template:GABAAergics for a full list of GABA_A positive allosteric modulators. Antagonists: Main site: Bicuculline • Gabazine • Pitrazepin • Quisqualamine; Negative allosteric modulators: α5IA • Bilobalide • Cicutoxin • Cyclothiazide • DMCM • Flumazenil • Flurothyl • Furosemide • L-655,708 • Oenanthotoxin • Penicillin • Pentylenetetrazol • Picrotoxin • PWZ-029 • Ro15-4513 • Sarmazenil • Suritozole • Thujone (Absinthe) • Thiocolchicoside • ZK-93426

GABA_B	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

GABA_C	Agonists: Main site: CACA • CAMP • GABOB • N(4)-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

GAD inhibitors	Allylglycine

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	Glutamate • Glutamine

Cofactors	Vitamin B6 (pyridoxine, pyridoxamine, pyridoxal phosphate)

Others	Gabapentin • L-Theanine • Picamilon • Pregabalin