gabab

(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist that decreases GABA-induced IP3 (inositol trisphosphate) production with an IC50 of 37.9 μM. It is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.

(E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.GABAB receptor antagonist 1 is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.

Panadiplon (FG 10571) is a selective gamma-aminobutyric acid receptor agonist and partial agonist of 5GABAA, a benzodiazepine receptor, used in the treatment of anxiety disorders.Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors.

3-aminopropylphosphonic acid (3-APPA) is a phosphonic analog of GABA that acts as a partial agonist of GABAB receptors (IC50 = 1.5 μM in a radioligand binding assay).

COR659 is a GABAB positive allosteric modulator (PAM) . COR659 suppresses alcohol and chocolate self-administration in rats[1]. COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABAB receptor and an action at the cannabinoid CB1 receptor[3]. COR659 (0, 2.5, 5 and 10 mg/kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats[1].COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats[2]. Animal Model: Male sP and Wistar rats[1]. [1]. Paola Maccioni, et al. Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABA B and cannabinoid CB 1 receptors. Psychopharmacology (Berl). 2017 Sep;234(17):2525-2543. [2]. Francesca Ferlenghi, et al. The GABA B receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives. Eur J Pharm Sci. 2020 Dec 1;155:105544. [3]. Paola Maccioni, et al. Anti-addictive properties of COR659 - Additional pharmacological evidence and comparison with a series of novel analogues. Alcohol. 2019 Mar;75:55-66.

SSD114 is a novel GABAB receptor positive allosteric modulator.

SCH 50911 is (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid and is a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor (IC50: 1.1 μM). SCH 50911 antagonizes GABA(B) autoreceptors, increasi

CGP 36742 is a selective antagonist of the GABAB receptor that can penetrate the blood-brain barrier after peripheral administration (IC50: 32 μM). It is useful in the treatment of depression.

CGP 35348 is a selective antagonist of GABAB receptor (EC50 = 34 μM). CGP 35348 can be used in studies of neuromuscular coordination and spatial learning after neonatal brain damage in albino mice.

GS 39783 is a positive allosteric modulator (PAM) of GABABR, which reduces the motivational properties of alcohol and the conditioned reinforcement and conditional reward of psychostimulants.

rac-BHFF ((R,S)-BHFF) is potent and selective GABA B receptor positive allosteric modulator that increases the potency and efficacy of GABA ( > 15-fold and > 149% respectively). It exhibits anxiolytic activity in vivo and is orally active.

CGP52432 is a very potent antagonist of GABAB receptors (IC50 = 85 nM).

Saclofen is a sulfonic analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) that acts as a competitive antagonist of the GABAB receptor (IC50: 7.8 μM).1 This compound can be used to determine the functional roles for the GABAB receptor as

Phenibut hydrochloride (3-Amino-4-phenylbutyric acid hydrochloride) is a GABA mimetic that acts as an agonist at GABAB receptors, blocks α2δ subunit-containing voltage-gated calcium channels, stimulates dopamine receptors, and inhibits the actions of β-phenethylamine

GABAB receptor antagonist 5 (Compound 23) is a competitive antagonist of the GABAB receptor. It holds potential for research into neuropsychiatric disorders, including epilepsy, depression, and addiction.

GABAB receptor antagonist 4 (Compound 28) is a GABAB receptor antagonist that inhibits GABA-induced G protein activation by competitively binding to the orthosteric site of the GABAB receptor. This compound is useful for researching neurological disorders associated with GABAB receptors.

3 (example 3) acts as an antagonist to the GABAB receptor [1].

Lesogaberan is an effective and selective GABAB receptor agonist (EC50: 8.6 nM for human recombinant GABAB receptors). For rat brain GABAB and GABAA receptors, the binding affinity (Kis) is 5.1 nM and 1.4 μM, respectively.

Baclofen (Lioresal) is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing Baclofen acts as a gamma-aminobutyric acid (GABA) agonist specific for GABA-B receptors. It acts at spinal and supraspinal sites, reducing excitatory transmission.

Baclofen hydrochloride (4-amino-3-(4-chlorophenyl)butanoic acid hydron chloride) is a GAMMA-AMINOBUTYRIC ACID derivative that is a specific GABA-B RECEPTORS agonist. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.

Lesogaberan (AZD-3355) napadisylate is a potent and selective agonist of GABA B receptors, with an EC50 of 8.6 nM for human recombinant GABA B receptors. It has an affinity (Ki) of 5.1 nM for rat GABA B receptors and 1.4 μM for GABA A receptors, determined by displacement of [3H]GABA binding in brain membranes. Lesogaberan napadisylate exerts a peripheral mode of action, inhibiting transient lower esophageal sphincter relaxation.

GABA-BSA is a hapten-carrier protein conjugate formed by coupling GABA (γ1-aminobutyric acid) to bovine serum albumin (BSA). As a hapten, GABA alone cannot induce an immune response and must be conjugated to a large molecular protein to become a complete antigen with immunogenicity. GABA-BSA may be supplied as a lyophilized powder or as a solution. The solution is prepared in 0.01 M TBS (pH 7.4) buffer at a typical concentration of 1 mg/mL.

Inaperisone is a novel centrally acting muscle relaxant that inhibits the voiding reflex. Inaperisone may inhibit the voiding reflex by acting indirectly on GABAB receptors in the brainstem.

γ-Aminobutyric acid belongs to natural products and functions as an agonist of GABAA and GABAB receptors, possessing central sedative effects, cell permeability, and the ability to modulate neuronal excitability. This compound is used in neuroscience research and exhibits anxiolytic, anticonvulsant, and neuroprotective activities.