gabab

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.

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).

SSD114 is a novel GABAB receptor positive allosteric modulator.

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

(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.

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

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 (4-Aminobutyric acid) is the predominant inhibitory neurotransmitter in the central nervous system.

Phenibut (Aminophenylbutyric acid) is a central depressant and derivative of the naturally occurring inhibitory neurotransmitter γ-aminobutyric acid (GABA).

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).

Phosphorylethanolamine (O-Phosphorylethanolamine) is a phosphomonoester metabolite of the phospholipid metabolism. Phosphorylethanolamine is a precursor of phospholipid synthesis and a product of phospholipid breakdown. Phosphomonoesters are present at much higher levels in the brain than in other organs. In developing the brain, phosphomonoesters are normally elevated during the period of neuritic proliferation. This also coincides with the occurrence of normal programmed cell death and synaptic pruning in developing the brain. These findings are consistent with the role of phosphomonoesters in membrane biosynthesis. Phosphorylethanolamine shows a strong structural similarity to the inhibitory neurotransmitter, GABA, and the GABAB receptor partial agonist, 3-amino-propylphosphonic acid. Phosphorylethanolamine is a phosphomonoester which is decreased in post-mortem Alzheimer's disease (AD) brain.

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

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.

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.

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.

CMPPE is a positive allosteric modulator (PAM) of the GABAB receptor, which inhibits alcohol self-administration and relapse behavior in rats.

Inidascamine is a modulator of cholinergic, glutamatergic, and GABA_B receptors, which can be utilized in the study of schizophrenia.

CGP55845 hydrochloride is a potent and selective GABAB receptor antagonist with an IC50 of 6 nM, suitable for use in neurological research [1] [2].

2-Hydroxysaclofen is a GABAB receptor antagonist.