GABA-B Receptor Antagonists

Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.

Also Known As:

GABA-B Antagonists; GABA-B Receptor Antagonist; Antagonist, GABA-B Receptor; Antagonists, GABA-B; Antagonists, GABA-B Receptor; GABA B Antagonists; GABA B Receptor Antagonist; GABA B Receptor Antagonists; Receptor Antagonist, GABA-B; Receptor Antagonists, GABA-B

Networked: 49 relevant articles (2 outcomes, 4 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Chemical Actions and Uses
- Pharmacologic Actions: 160
  - Molecular Mechanisms of Pharmacological Action: 24
    - Neurotransmitter Agents: 13181
      - GABA Agents: 76
        GABA Antagonists: 133
        GABA-B Receptor Antagonists: 49
  - Physiological Effects of Drugs: 1
    - Neurotransmitter Agents: 13181
      - GABA Agents: 76
        GABA Antagonists: 133
        GABA-B Receptor Antagonists: 49

Experts

1.	Leung, L Stan: 3 articles (06/2012 - 05/2008)
2.	Koek, Wouter: 3 articles (10/2010 - 06/2005)
3.	Pearl, Phillip L: 2 articles (11/2021 - 10/2011)
4.	Theodore, William H: 2 articles (11/2021 - 10/2011)
5.	Mareš, Pavel: 2 articles (01/2019 - 12/2010)
6.	Boyce, Richard: 2 articles (06/2012 - 03/2010)
7.	Tsai, Min-Lan: 2 articles (06/2012 - 05/2008)
8.	Ayajiki, Kazuhide: 2 articles (09/2011 - 11/2009)
9.	Kobuchi, Shuhei: 2 articles (09/2011 - 11/2009)
10.	Matsumura, Yasuo: 2 articles (09/2011 - 11/2009)

Related Diseases

1.	Acute Kidney Injury (Acute Renal Failure) 11/25/2009 - "Intravenous injection of CGP52432 (0.1micromol/kg), a selective GABA(B) receptor antagonist, eliminated the preventive effect by GABA (50micromol/kg) on ischemic acute kidney injury. "
2.	succinic semialdehyde dehydrogenase deficiency 11/01/2021 - "We examined safety, tolerability, and efficacy of SGS-742, a γ-aminobutyric acid B (GABA-B) receptor antagonist, in patients with succinic semialdehyde dehydrogenase deficiency. " 11/01/2021 - "A Randomized Controlled Trial of SGS-742, a γ-aminobutyric acid B (GABA-B) Receptor Antagonist, for Succinic Semialdehyde Dehydrogenase Deficiency."
3.	Seizures (Absence Seizure) 03/01/2006 - "This study confirms the potential of GABA(B) antagonists in contrasting seizure absence in rodent models and suggests the application of drugs with a similar mechanism in humans. " 10/01/2011 - "These resemble absence seizures and are abolished by a GABA(B) receptor antagonist. " 12/01/2010 - "Thresholds for movements directly elicited by stimulation, for spike-and-wave type of AD, for clonic seizures accompanying this type of ADs and for transition into limbic type of AD were decreased by the 200mg/kg dose of a GABA-B receptor antagonist CGP35348 in all three age groups. " 05/01/2008 - "The aim of this study was to investigate the long-term alterations of synaptic transmission and seizure susceptibility in the hippocampus after early-life seizures induced by systemic injection of a GABA(B)-receptor antagonist CGP56999A in immature rats. " 06/25/2012 - "Seizure rats were given a single injection of GABA(B) receptor antagonist CGP56999A (1-1.2 mg/kg i.p.) on postnatal day (PND) 15, which induced multiple limbic seizures in 8h; control rats were given saline injection. "
4.	Absence Epilepsy (Childhood Absence Epilepsy) 08/01/2001 - "The aim of the present study was to examine the effects of three potent gamma-aminobutyric acid (GABA)B receptor antagonists CGP55845A, CGP62349 and CGP71982 (0.01 mg/kg) on the development of GHBL-induced absence epilepsy and in learning paradigms of active and passive avoidance tests in GHBL-treated mice and rats. " 11/02/2001 - "AMPA and GABA(B) receptor antagonists and their interaction in rats with a genetic form of absence epilepsy."
5.	Ischemia 03/01/2016 - "A total of 80 rats were randomly divided into four groups: A sham operation group, an ischemia group, an ON group and an ON group effectively inhibited by the GABA(B) receptor antagonist, CGP35384 (n=20/group). " 09/01/2011 - "Intravenous or intracerebroventricular treatment with 3-[[[(3,4-dichlorophenyl)methyl]amino]propyl] diethoxymethyl) phosphinic acid (CGP52432), a GABA(B) receptor antagonist, abolished the suppressive effects of intravenously applied GABA on enhanced renal sympathetic nerve activity during ischemia, leading to the elimination of the renoprotective effects of GABA. " 06/13/2007 - "While baclofen (500 microM), a GABA(B) receptor agonist, suppressed ischemia-induced glutamate release by 52%, GABA(B) receptor antagonist saclofen (500 microM) failed to produce a significant increase of glutamate release. "

Related Drugs and Biologics

1.	gamma-Aminobutyric Acid (GABA)
2.	Aminobutyrates (Aminobutyric Acid)
3.	(3-aminopropyl)(n-butyl)phosphinic acid
4.	Acids
5.	CGP 56999A
6.	Ethanol (Ethyl Alcohol)
7.	(+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid
8.	Baclofen
9.	GABA-B Receptor Agonists
10.	CGP 35348

Related Therapies and Procedures

1.	Intravenous Injections
2.	Induced Hypothermia
3.	Hypnosis (Mesmerism)