GABAB Receptors

GABAB receptors are metabotropic G-protein-coupled receptors responsible for mediating the inhibitory effects of GABA alongside ionotropic GABAA and GABAA receptors. They exist as heterodimers of GABAB1 and GABAB2 subunits, with both required for function.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
3618 Acamprosate calcium
GABA agonist and glutamatergic modulator
0796 (R)-Baclofen
Selective GABAB agonist. Active enantiomer of (RS)-Baclofen (Cat. No. 0417)
0417 (RS)-Baclofen
Selective GABAB agonist
0344 GABA
Endogenous agonist
3400 RuBi-GABA
Caged GABA; excitable by visible wavelength
4709 RuBi GABA trimethylphosphine
Caged GABA; inhibits neural activity
0379 SKF 97541
Extremely potent GABAB agonist

Antagonists

Cat No Product Name / Activity
1245 CGP 35348
Brain penetrant, selective GABAB antagonist
3219 CGP 36216 hydrochloride
GABAB antagonist; displays activity at presynaptic receptors
1247 CGP 46381
Brain penetrant, selective GABAB antagonist
1246 CGP 52432
Potent, selective GABAB antagonist
1088 CGP 54626 hydrochloride
Potent, selective GABAB antagonist
1248 CGP 55845 hydrochloride
Potent, selective GABAB antagonist
0245 2-Hydroxysaclofen
Selective GABAB antagonist, more potent than saclofen (Cat. No. 0246)
0178 Phaclofen
Weak, selective GABAB antagonist
0246 Saclofen
Selective GABAB antagonist
0984 SCH 50911
Selective, competitive, orally active GABAB antagonist

Modulators

Cat No Product Name / Activity
3313 rac BHFF
Potent, selective GABAB positive allosteric modulator
1514 CGP 13501
Positive modulator at GABAB receptors
1513 CGP 7930
Positive modulator at GABAB receptors
2001 GS 39783
Positive modulator at GABAB receptors

Other

Cat No Product Name / Activity
1814 N-ArachidonylGABA
Inhibits pain in vivo
0806 Gabapentin
Anticonvulsant. Increases brain GABA
0538 trans-4-Hydroxycrotonic acid
GHB receptor ligand
0386 3-Methyl-GABA
Activator of GABA amino-transferase
1811 Modafinil
Psychostimulant
0780 NCS-382
Antagonist of γ-hydroxybutyric acid
4579 Pentobarbital sodium salt
Enhances GABAergic activity
2687 Pentylenetetrazole
CNS stimulant
4578 Phenobarbital sodium salt
Enhances GABAergic activity
5518 UMB 68
GHB receptor ligand
2815 Valproic acid, sodium salt
Increases GABA levels; anticonvulsant
0808 Vigabatrin
GABA-T inhibitor
2625 Zonisamide
Anticonvulsant, modulates GABA neurotransmission

GABAB receptors are metabotropic G-protein-coupled receptors responsible for mediating the inhibitory effects of GABA alongside ionotropic GABAA and GABAA receptors. They exist as heterodimers of GABAB1 and GABAB2 subunits and the presence of both subunits is required for receptor function.

When GABAB1 is expressed alone it is non-functional and is not transported to the cell membrane. This subunit is responsible for binding GABA, and the GABAB2 subunit interacts with the G protein. The two subunits interact allosterically: GABAB1 increases coupling of GABAB2 to G proteins and GABAB2 increases agonist binding to GABAB1. GABAB receptors are coupled to Ca2+ and K+ channels.

External sources of pharmacological information for GABAB Receptors :

Literature for GABAB Receptors

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GABA Receptors

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GABAB Receptor Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
GABAB1 Human GABBR1 NM_021905 Q9UBS5
Mouse Gabbr1 NM_019439 Q9WV18
Rat Gabbr1 NM_031028 Q9Z0U4
GABAB2 Human GABBR2 NM_005458 O75899
Mouse Gabbr2 NM_001081141 Q80T41
Rat Gabbr2 NM_031802 O88871