GABA<sub>B1</sub> | GABA<sub>B</sub> receptors | IUPHAR/BPS Guide to PHARMACOLOGY

GABAB1

Target id: 240

Nomenclature: GABAB1

Family: GABAB receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for GABAB1 in GtoImmuPdb

Quaternary Structure: Complexes
GABAB receptor
Gene and Protein Information
class C G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 961 6p21.3 GABBR1 gamma-aminobutyric acid type B receptor subunit 1 10-11,21
Mouse 7 960 17B3 Gabbr1 gamma-aminobutyric acid (GABA) B receptor, 1
Rat 7 960 20p12 Gabbr1 gamma-aminobutyric acid type B receptor subunit 1
Previous and Unofficial Names
GABABR1 [14] | GPRC3A | GABA-B receptor 1 | GABABR1 | gamma-aminobutyric acid (GABA) B receptor 1 | gamma-aminobutyric acid (GABA) B receptor
Database Links
Specialist databases
GPCRDB gabr1_human (Hs), gabr1_mouse (Mm), gabr1_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands
GABA

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
lesogaberan Hs Agonist 8.1 pEC50 1
pEC50 8.1 (EC50 8x10-9 M) [1]
3-APPA Rn Agonist 5.6 pIC50 14
pIC50 5.6 [14]
CGP 47656 Hs Full agonist 4.8 – 5.0 pIC50 14
pIC50 4.8 – 5.0 [14]
GABA Rn Full agonist 4.5 – 4.6 pIC50 14
pIC50 4.5 – 4.6 [14]
(-)-baclofen Rn Full agonist 4.4 – 4.6 pIC50 14
pIC50 4.4 – 4.6 [14]
View species-specific agonist tables
Agonist Comments
The potency values displayed here are for ligand binding to the GABAB1 subunit only. For ligand binding data on the functional heterodimer of GABAB1 and GABAB2, see the GABAB data pages.

No evidence of any species difference.

The GABA binding site within this subunit is located in the large extracellular domain, the structure of which is similar to that of the mGlu receptor. Critical residues involved in agonist binding have been identified by molecular modeling and site directed mutagenesis [15]. It is proposed agonists act by stabilizing a closed state of this binding domain in GABAB1. In agreement with this proposal, locking this binding domain in a closed state by introduction of a cystein-bond, locks the receptor in a fully active state [16].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]CGP 71872 Rn Antagonist 9.0 pKd 14
pKd 9.0 [14]
[125I]CGP 64213 Rn Antagonist 8.9 pKd 14
pKd 8.9 [14]
CGP 56999A Rn Antagonist 9.1 – 9.2 pIC50 14
pIC50 9.1 – 9.2 [14]
CGP 62349 Rn Antagonist 8.8 – 9.0 pIC50 14
pIC50 8.8 – 9.0 [14]
CGP 54626A Rn Antagonist 8.7 – 8.8 pIC50 14
pIC50 8.7 – 8.8 [14]
CGP 64213 Rn Antagonist 8.5 – 8.6 pIC50 14
pIC50 8.5 – 8.6 [14]
CGP 71872 Rn Antagonist 8.3 – 8.4 pIC50 14
pIC50 8.3 – 8.4 [14]
SCH 50911 Rn Antagonist 6.4 pIC50 2
pIC50 6.4 [2]
CGP 35348 Rn Antagonist 4.6 – 4.8 pIC50 7,14
pIC50 4.6 – 4.8 [7,14]
2-hydroxy-saclofen Rn Antagonist 4.1 pIC50 14
pIC50 4.1 [14]
saclofen Rn Antagonist 3.4 – 3.5 pIC50 14
pIC50 3.4 – 3.5 [14]
Antagonist Comments
The potency values displayed here are for ligand binding to the GABAB1 subunit only. For ligand binding data on the functional heterodimer of GABAB1 and GABAB2, see the GABAB data pages.

So far no species difference have been noticed for the GABAB1 subunit.

These antagonists bind at the same site as agonists and likely prevent the formation of a closed state of the binding domain.
When measured on the GABAB1 subunit expressed alone, antagonist affinities were identical to those measured in the GABAB1 - GABAB2 heterodimer. This indicates that the GABAB2 subunit has no major effect on antagonist binding.
Allosteric Modulator Comments
Positive modulators for GABAB receptors exist but the indications are that they exert their actions via GABAB2 within the GABAB heterodimer. No evidence for any modulation of the GABAB1 receptor subunit exists.
Primary Transduction Mechanisms
Comments:  The GABAB2 subunit contains all the molecular determinants required for G protein recognition and activation by the heteromer[6,8,17]. However, GABAB1 is able to weakly couple to G proteins and to atypically modulate effector K+ channels in vivo in the absence of GABAB2. It is currently unclear whether the observed coupling is physiologically relevant or not.
References:  9
Tissue Distribution
All cerebral cortical layers, pyramidal cell layers of the hippocampus, granular cell layer of the dentate gyrus, medial habenula, medial geniculate nucleus, substantia nigra pars compacta, ventral tegmental area and several thalamic, amygdaloid and hypothalamic nuclei.
In the cerebellum: Purkinje cells > granular layer.
Neuronal but not glial cells.
Species:  Rat
Technique:  in situ hybridisation.
References:  14
Uterus, spleen, small intestine, lung > prostate, stomach, pancreas, kidney, heart, liver > skeletal muscle, testes.
Species:  Rat
Technique:  Immunohistochemistry.
References:  4
Thalamus, interpeduncular nucleus and medial habenula.
Species:  Rat
Technique:  Immunohistochemistry.
References:  18
Brain: neocortex, hippocampus, thalamus, cerebellum and habenula. Spinal cord: superficial layers of the dorsal horn and motor neurones in the deep layers of the ventral horn.
Species:  Rat
Technique:  Immunohistochemistry.
References:  5
Tissue Distribution Comments
There is a high degree of similarity between the distributions of the GABAB1 and GABAB2 subunits [13].
Expression Datasets

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assay Comments
No functional assays for the GABAB1 (in the absence of GABAB2) subunit have been described. Only where there is an intact heterodimer (GABAB1+ GABAB2) have any functional studies been reported. Structural modifications to GABAB1 + GABAB2 within the heterodimer can still allow functional responses to occur.
Physiological Consequences of Altering Gene Expression
Spontaneous seizure, Hyperalgesia, Hyperlocomotor activity, Cognitive deficits, Lack of responses to GABAB agonist administration eg. lack of muscle relaxation and hypothermia, down-regulation in GABAB2 subunit.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  25
The GABAB1 receptor knockout mice have disrupted pre- and postsynaptic GABAB receptor function. The mice appear normal at birth but later exhibit retarded growth, epilepsy and premature death.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  23
GABAB1 receptor knockout mice exhibit a complete loss of GABAB function and increased excitability in the CA3 region of hippocampal slices, leading to the development of complex generalised epilepsies.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  3
GABAB1 receptor knockout mice exhibit basal hypothermia and lack of GABAB receptor binding sites in brain membranes.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  24
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Gabbr1tm1Pngl Gabbr1tm1Pngl/Gabbr1tm1Pngl
involves: 129P2/OlaHsd * C57BL/6J
MGI:1860139  MP:0005402 abnormal action potential PMID: 11414794 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0005404 abnormal axon morphology PMID: 18206390 
Gabbr1tm2.1Bet Gabbr1tm2.1Bet/Gabbr1tm2.1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0001777 abnormal body temperature regulation PMID: 15493018 
Gabbr1tm2Bet|Tg(HCRT-cre)1Stak Gabbr1tm2Bet/Gabbr1tm2Bet,Tg(HCRT-cre)1Stak/0
involves: BALB/cA * C57BL/6 * DBA/1
MGI:1860139  MGI:3839421  MP:0002206 abnormal CNS synaptic transmission PMID: 19246384 
Gabbr1tm3Bet Gabbr1tm3Bet/Gabbr1tm3Bet
BALB/c-Gabbr1
MGI:1860139  MP:0002805 abnormal conditioned taste aversion behavior PMID: 16928868 
Gabbr1tm4Bet Gabbr1tm4Bet/Gabbr1tm4Bet
BALB/c-Gabbr1
MGI:1860139  MP:0002805 abnormal conditioned taste aversion behavior PMID: 16928868 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0003360 abnormal depression-related behavior PMID: 15706241 
Gabbr1+|Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1+
BALB/c-Gabbr1
MGI:1860139  MP:0002572 abnormal emotion/affect behavior PMID: 15706241 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0001927 abnormal estrous cycle PMID: 16682806 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0002910 abnormal excitatory postsynaptic currents PMID: 11498050 
Gabbr1tm3Bet Gabbr1tm3Bet/Gabbr1tm3Bet
BALB/c-Gabbr1
MGI:1860139  MP:0002910 abnormal excitatory postsynaptic currents PMID: 16701209 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0001406 abnormal gait PMID: 18206390 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0002945 abnormal inhibitory postsynaptic currents PMID: 11498050 
Gabbr1tm4Bet Gabbr1tm4Bet/Gabbr1tm4Bet
BALB/c-Gabbr1
MGI:1860139  MP:0002945 abnormal inhibitory postsynaptic currents PMID: 16701209 
Gabbr1tm2Bet|Tg(HCRT-cre)1Stak Gabbr1tm2Bet/Gabbr1tm2Bet,Tg(HCRT-cre)1Stak/0
involves: BALB/cA * C57BL/6 * DBA/1
MGI:1860139  MGI:3839421  MP:0002945 abnormal inhibitory postsynaptic currents PMID: 19246384 
Gabbr1tm1Pngl Gabbr1tm1Pngl/Gabbr1tm1Pngl
involves: 129P2/OlaHsd * C57BL/6J
MGI:1860139  MP:0002911 abnormal inhibitory postsynaptic potential PMID: 11414794 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0006404 abnormal lumbar dorsal root ganglion morphology PMID: 18206390 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0000920 abnormal myelination PMID: 18206390 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0003871 abnormal myelin sheath morphology PMID: 18206390 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0002272 abnormal nervous system electrophysiology PMID: 11498050 
Gabbr1tm1Pngl Gabbr1tm1Pngl/Gabbr1tm1Pngl
involves: 129P2/OlaHsd * C57BL/6J
MGI:1860139  MP:0002272 abnormal nervous system electrophysiology PMID: 11414794 
Gabbr1tm3Bet Gabbr1tm3Bet/Gabbr1tm3Bet
BALB/c-Gabbr1
MGI:1860139  MP:0001458 abnormal object recognition memory PMID: 16701209 
Gabbr1tm1Dgen Gabbr1tm1Dgen/Gabbr1tm1Dgen
involves: 129P2/OlaHsd * C57BL/6
MGI:1860139  MP:0001504 abnormal posture
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0002651 abnormal sciatic nerve PMID: 18206390 
Gabbr1tm2Bet|Tg(HCRT-cre)1Stak Gabbr1tm2Bet/Gabbr1tm2Bet,Tg(HCRT-cre)1Stak/0
involves: BALB/cA * C57BL/6 * DBA/1
MGI:1860139  MGI:3839421  MP:0001501 abnormal sleep pattern PMID: 19246384 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0002752 abnormal somatic nervous system morphology PMID: 18206390 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0003635 abnormal synaptic transmission PMID: 11498050 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0003216 absence seizures PMID: 11498050 
Gabbr1tm1Dgen Gabbr1tm1Dgen/Gabbr1tm1Dgen
involves: 129P2/OlaHsd * C57BL/6
MGI:1860139  MP:0008843 absent subcutaneous adipose tissue
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0001496 audiogenic seizures PMID: 11498050 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0003996 clonic seizures PMID: 11498050 
Gabbr1tm1Pngl Gabbr1tm1Pngl/Gabbr1tm1Pngl
involves: 129P2/OlaHsd * C57BL/6J
MGI:1860139  MP:0001262 decreased body weight PMID: 11414794 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0008874 decreased physiological sensitivity to xenobiotic PMID: 11498050 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0003998 decreased thermal nociceptive threshold PMID: 11498050  18206390 
Gabbr1tm1Dgen Gabbr1tm1Dgen/Gabbr1tm1Dgen
involves: 129P2/OlaHsd * C57BL/6
MGI:1860139  MP:0001429 dehydration
Gabbr1tm2.1Bet Gabbr1tm2.1Bet/Gabbr1tm2.1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0001399 hyperactivity PMID: 15493018 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0001399 hyperactivity PMID: 11498050 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0002738 hyperresponsive to tactile stimuli PMID: 11498050 
Gabbr1tm1Dgen Gabbr1tm1Dgen/Gabbr1tm1Dgen
involves: 129P2/OlaHsd * C57BL/6
MGI:1860139  MP:0001402 hypoactivity
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0005498 hyporesponsive to tactile stimuli PMID: 18206390 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0009747 impaired behavioral response to xenobiotic PMID: 11498050  15321743 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0004000 impaired passive avoidance behavior PMID: 11498050 
Gabbr1+|Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1+
BALB/c-Gabbr1
MGI:1860139  MP:0004000 impaired passive avoidance behavior PMID: 11498050 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0001363 increased anxiety-related response PMID: 15321743  15706241 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0001751 increased circulating luteinizing hormone level PMID: 16682806 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0005124 increased circulating prolactin level PMID: 16682806 
Gabbr1+|Gabbr1tm1Pngl Gabbr1tm1Pngl/Gabbr1+
involves: 129P2/OlaHsd * C57BL/6J
MGI:1860139  MP:0009141 increased prepulse inhibition PMID: 11414794 
Gabbr1Gt(KST229)Byg Gabbr1Gt(KST229)Byg/Gabbr1Gt(KST229)Byg
involves: 129P2/OlaHsd * C57BL/6
MGI:1860139  MP:0002058 neonatal lethality PMID: 11431694 
Gabbr1tm1Pngl Gabbr1tm1Pngl/Gabbr1tm1Pngl
involves: 129P2/OlaHsd * C57BL/6J
MGI:1860139  MP:0002082 postnatal lethality PMID: 11414794 
Gabbr1tm1Dgen Gabbr1tm1Dgen/Gabbr1tm1Dgen
involves: 129P2/OlaHsd * C57BL/6
MGI:1860139  MP:0002083 premature death
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0009017 prolonged estrus PMID: 16682806 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0001923 reduced female fertility PMID: 16682806 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0001473 reduced long term potentiation PMID: 16701209 
Gabbr1tm3Bet Gabbr1tm3Bet/Gabbr1tm3Bet
BALB/c-Gabbr1
MGI:1860139  MP:0001473 reduced long term potentiation PMID: 16701209 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0002064 seizures PMID: 11498050 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0009015 short proestrus PMID: 16682806 
Gabbr1tm1Pngl Gabbr1tm1Pngl/Gabbr1tm1Pngl
involves: 129P2/OlaHsd * C57BL/6J
MGI:1860139  MP:0000951 sporadic seizures PMID: 11414794 
Gabbr1tm1Bet Gabbr1tm1Bet/Gabbr1tm1Bet
BALB/c-Gabbr1
MGI:1860139  MP:0003997 tonic-clonic seizures PMID: 11498050 
Gabbr1tm1Pngl Gabbr1tm1Pngl/Gabbr1tm1Pngl
involves: 129P2/OlaHsd * C57BL/6J
MGI:1860139  MP:0003997 tonic-clonic seizures PMID: 11414794 
Gabbr1tm1Dgen Gabbr1tm1Dgen/Gabbr1tm1Dgen
involves: 129P2/OlaHsd * C57BL/6
MGI:1860139  MP:0000746 weakness
Biologically Significant Variants
Type:  Alternative promoters
Species:  Human
Description:  The GABAB1(a) and GABAB1(b) isoforms which differ in their extracellular N-terminal regions are generated by alternative promoters in the human GABAB1 gene.
References:  27
Type:  Splice variant
Species:  Rat
Description:  The GABAB1(c) isoform, which has a 93 bp insertion in the region encoding the 5th transmembrane domain compared to GABAB1(b), has been found to be widely expressed in various rat tissues.
References:  12,22
Type:  Splice variant
Species:  Rat
Description:  The GABAB1(d) isoform, which has an additional 566 bps at the C-terminal when compared to GABAB1(b), has been found to be widely expressed in various rat tissues.
References:  12
Type:  Splice variant
Species:  Rat
Description:  The GABAB1(f) isoform has been identified mainly in rat peripheral tissues. It differs from the GABAB1(a) isoform due to a 21 bp deletion in the coding sequence of the N-terminal and a 93 bp insertion in the coding sequence of the 2nd extracellular loop and the 5th transmembrane domain.
References:  28
Type:  Splice variant
Species:  Rat
Description:  The GABAB1(e) receptor isoform, containing only the ligand binding extracellular domain, has been found to be a minor isoform in the CNS but a major isoform in peripheral tissues.
References:  26
Type:  Splice variant
Species:  Rat
Description:  The GABAB1(h) isoform has been identified in the embryonic rat brain.
References:  20
Type:  Splice variant
Species:  Human
Description:  The GABAB1(h) isoform (originally named GABAB1(c) in human) differs from GABAB1(a) by a 186 bp sushi domain exon that is skipped by alternative splicing. GABAB1(h) has a higher expression in the fetal human brain than the adult.
References:  19
Type:  Splice variant
Species:  Rat
Description:  The GABAB1(g) isoform, which has a 124 bp insertion between exon 3 and exon 4 encoding a truncated receptor lacking the C-terminal, has been found in both the rat brain and periphery.
References:  29

References

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1. AstraZeneca. Lesogaberan (AZD3355). Accessed on 11/09/2014. Modified on 11/09/2014. astrazeneca.com, http://openinnovation.astrazeneca.com/what-we-offer/compound/azd3355-lesogaberan/

2. Bolser DC, Blythin DJ, Chapman RW, Egan RW, Hey JA, Rizzo C, Kuo SC, Kreutner W. (1995) The pharmacology of SCH 50911: a novel, orally-active GABA-beta receptorantagonist. J Pharmacol Exp Ther., 274: 1393-1398. [PMID:7562513]

3. Brown JT, Gill CH, Farmer CE, Lanneau C, Randall AD, Pangalos MN, Collingridge GL, Davies CH. (2003) Mechanisms contributing to the exacerbated epileptiform activity in hippocampal slices of GABAB1 receptor subunit knockout mice. Epilepsy Res, 57: 121-136. [PMID:15013053]

4. Calver AR, Medhurst AD, Robbins MJ, Charles KJ, Evans ML, Harrison DC, Stammers M, Hughes SA, Hervieu G, Couve A, Moss SJ, Middlemiss DN, Pangalos MN. (2000) The expression of GABA(B1) and GABA(B2) receptor subunits in the CNS differs from that in peripheral tissues. Neuroscience, 1000: 155-170. [PMID:10996466]

5. Charles KJ, Evans ML, Robbins MJ, Calver AR, Leslie RA, Pangalos MN. (2001) Comparative immunohistochemical localisation of GABA(B1a), GABA(B1b) andGABA(B2) subunits in rat brain, spinal cord and dorsal root ganglion. Neuroscience, 106: 447-467. [PMID:11591450]

6. Duthey B, Caudron S, Perroy J, Bettler B, Fagni L, Pin JP, Prezeau L. (2002) A single subunit (GB2) is required for G-protein activation by the heterodimeric GABA(B) receptor. J Biol Chem, 277: 3236-3241. [PMID:11711539]

7. Froestl W, Mickel SJ, von Sprecher G, Diel PJ, Hall RG, Maier L, Strub D, Melillo V, Baumann PA, Bernasconi R et al.. (1995) Phosphinic acid analogues of GABA. 2. Selective, orally active GABAB antagonists. J. Med. Chem., 38: 3313-3331. [PMID:7650685]

8. Galvez T, Duthey B, Kniazeff J, Blahos J, Rovelli G, Bettler B, Prezeau L, Pin JP. (2001) Allosteric interactions between GB1 and GB2 subunits are required for optimal GABA(B) receptor function. Embo J, 20: 2152-2159. [PMID:11331581]

9. Gassmann M, Shaban H, Vigot R, Sansig G, Haller C, Barbieri S, Humeau Y, Schuler V, Muller M, Kinzel B, Klebs K, Schmutz M, Froestl W, Heid J, Kelly PH, Gentry C, Jaton AL, van der Putten H, Mombereau C, Lecourtier L, Mosbacher J, Cryan JF, Fritschy JM, Luthi A, Kaupmann K, Bettler B. (2004) Redistribution of GABAB(1) protein and atypical GABAB responses in GABAB(2)-deficient mice. J Neurosci, 24: 6086-6097. [PMID:15240800]

10. Goei VL, Choi J, Ahn J, Bowlus CL, Raha-Chowdhury R, Gruen JR. (1998) Human gamma-aminobutyric acid B receptor gene: complementary DNA cloning, expression, chromosomal location, and genomic organization. Biol Psychiatry, 44: 659-666. [PMID:9798068]

11. Grifa A, Totaro A, Rommens JM, Carella M, Roetto A, Borgato L, Zelante L, Gasparini P. (1998) GABA (gamma-amino-butyric acid) neurotransmission: identification and fine mapping of the human GABAB receptor gene. Biochem Biophys Res Commun, 250: 240-245. [PMID:9753614]

12. Isomoto S, Kaibara M, Sakurai-Yamashita Y, Nagayama Y, Uezonzo Y, Yano K, Taniyama K. (1998) Cloning and tissue distribution of novel splice variants of the rat GABAB receptor. Biochem. Biophys. Res. Commun., 253: 10-15. [PMID:9875211]

13. Jones KA, Borowsky B, Tamm JA, Craig DA, Durkin MM, Dai M, Yao WJ, Johnson M, Gunwaldsen C, Huang LY, Tang C, Shen Q, Salon JA, Morse K, Laz T, Smith KE, Nagarathnam D, Noble SA, Branchek TA, Gerald C. (1998) GABAB receptors function as a heteromeric assembly of the subunits GABABR1 and GABABR2. Nature, 396: 674-679. [PMID:9872315]

14. Kaupmann K, Huggel K, Heid J, Flor PJ, Bischoff S, Mickel SJ, McMaster G, Angst C, Bittiger H, Froestl W, Bettler B. (1997) Expression cloning of GABAB receptors uncovers similarity to metabotropic glutamate receptors. Nature, 386: 239-246. [PMID:9069281]

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16. Kniazeff J, Saintot PP, Goudet C, Liu J, Charnet A, Guillon G, Pin JP. (2004) Locking the dimeric GABAB G-protein coupled receptor in its active state. J Neurosci, 24: 370-377. [PMID:14724235]

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Bernhard Bettler, Norman G. Bowery, John F. Cryan, Sam J. Enna, David H. Farb, Wolfgang Foestl, Klemens Kaupmann, Jean-Philippe Pin.
GABAB receptors: GABAB1. Last modified on 20/02/2018. Accessed on 19/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=240.