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GABAA receptor ρ1 subunit

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Target not currently curated in GtoImmuPdb

Target id: 420

Nomenclature: GABAA receptor ρ1 subunit

Family: GABAA receptors

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 4 479 6q15 GABRR1 gamma-aminobutyric acid type A receptor subunit rho1 2
Mouse 4 480 4 A5 Gabrr1 gamma-aminobutyric acid type A receptor subunit rho 1 5
Rat 4 480 5q21 Gabrr1 gamma-aminobutyric acid type A receptor subunit rho 1 1
Previous and Unofficial Names Click here for help
GABA(A) receptor subunit rho-1 | gamma-aminobutyric acid (GABA) A receptor, rho 1 | gamma-aminobutyric acid (GABA) C receptor, subunit rho 1 | gamma-aminobutyric acid (GABA) C receptor | gamma-aminobutyric acid type A receptor rho1 subunit | gamma-aminobutyric acid type A receptor rho 1 subunit
Database Links Click here for help
Alphafold P24046 (Hs), P56475 (Mm), P50572 (Rn)
CATH/Gene3D 2.70.170.10
ChEMBL Target CHEMBL3561 (Hs)
DrugBank Target P24046 (Hs)
Ensembl Gene ENSG00000146276 (Hs), ENSMUSG00000028280 (Mm), ENSRNOG00000007603 (Rn)
Entrez Gene 2569 (Hs), 14408 (Mm), 29694 (Rn)
Human Protein Atlas ENSG00000146276 (Hs)
KEGG Gene hsa:2569 (Hs), mmu:14408 (Mm), rno:29694 (Rn)
OMIM 137161 (Hs)
Pharos P24046 (Hs)
RefSeq Nucleotide NM_002042 (Hs), NM_008075 (Mm), NM_017291 (Rn)
RefSeq Protein NP_002033 (Hs), NP_032101 (Mm), NP_058987 (Rn)
UniProtKB P24046 (Hs), P56475 (Mm), P50572 (Rn)
Wikipedia GABRR1 (Hs)
Natural/Endogenous Ligands Click here for help
GABA

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
CACA Small molecule or natural product Rn Agonist 4.1 pEC50 4
⤷ pEC50 4.1 (EC50 7.4x10-5 M) [4]
(±)-cis-2-CAMP Small molecule or natural product Click here for species-specific activity table Hs Full agonist - -
⤷ [Binds to: GABA site]
5-Me-IAA Small molecule or natural product Click here for species-specific activity table Hs Full agonist - -
⤷ [Binds to: GABA site]
isoguvacine Small molecule or natural product Click here for species-specific activity table Hs Partial agonist - -
⤷ [Binds to: GABA site]
muscimol Small molecule or natural product Click here for species-specific activity table Hs Partial agonist - -
⤷ [Binds to: GABA site]
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
cis-3-ACPBPA Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
⤷ [Binds to: GABA site]
trans-3-ACPBPA Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
⤷ [Binds to: GABA site]
aza-THIP Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
⤷ [Binds to: GABA site]
isonipecotic acid Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist - -
⤷ [Binds to: GABA site]
piperidine-4-sulphonic acid Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
⤷ [Binds to: GABA site]
gaboxadol Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist - - 3
⤷ [Binds to: GABA site] [3]
TPMPA Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist - -
⤷ [Binds to: GABA site]
Channel Blockers
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Use-dependent Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
picrotoxin Small molecule or natural product Click here for species-specific activity table Hs - no - - - no
⤷
Not voltage dependent
TBPS Small molecule or natural product Click here for species-specific activity table Hs - no - - - no
⤷
Not voltage dependent

References

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1. Cutting GR, Curristin S, Zoghbi H, O'Hara B, Seldin MF, Uhl GR. (1992) Identification of a putative gamma-aminobutyric acid (GABA) receptor subunit rho2 cDNA and colocalization of the genes encoding rho2 (GABRR2) and rho1 (GABRR1) to human chromosome 6q14-q21 and mouse chromosome 4. Genomics, 12 (4): 801-6. [PMID:1315307]

2. Cutting GR, Lu L, O'Hara BF, Kasch LM, Montrose-Rafizadeh C, Donovan DM, Shimada S, Antonarakis SE, Guggino WB, Uhl GR. (1991) Cloning of the gamma-aminobutyric acid (GABA) rho 1 cDNA: a GABA receptor subunit highly expressed in the retina. Proc Natl Acad Sci USA, 88 (7): 2673-7. [PMID:1849271]

3. Krehan D, Frølund B, Ebert B, Nielsen B, Krogsgaard-Larsen P, Johnston GA, Chebib M. (2003) Aza-THIP and related analogues of THIP as GABA C antagonists. Bioorg Med Chem, 11 (23): 4891-6. [PMID:14604650]

4. Woodward RM, Polenzani L, Miledi R. (1993) Characterization of bicuculline/baclofen-insensitive (rho-like) gamma-aminobutyric acid receptors expressed in Xenopus oocytes. II. Pharmacology of gamma-aminobutyric acidA and gamma-aminobutyric acidB receptor agonists and antagonists. Mol Pharmacol, 43 (4): 609-25. [PMID:8386310]

5. Zhang D, Pan ZH, Zhang X, Brideau AD, Lipton SA. (1995) Cloning of a gamma-aminobutyric acid type C receptor subunit in rat retina with a methionine residue critical for picrotoxinin channel block. Proc Natl Acad Sci USA, 92 (25): 11756-60. [PMID:8524843]

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