GABA<sub>A</sub> receptor ρ1 subunit | GABA<sub>A</sub> receptors | IUPHAR/BPS Guide to PHARMACOLOGY

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GABAA receptor ρ1 subunit

Target not currently curated in GtoImmuPdb

Target id: 420

Nomenclature: GABAA receptor ρ1 subunit

Family: GABAA receptors

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Contents:

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 4 473 6q13-q16.3 GABRR1 gamma-aminobutyric acid type A receptor rho1 subunit 2
Mouse 4 474 4 A5 Gabrr1 gamma-aminobutyric acid (GABA) C receptor, subunit rho 1 4
Rat 4 474 5q21 Gabrr1 gamma-aminobutyric acid type A receptor rho 1 subunit 1
Previous and Unofficial Names
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
Database Links
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)
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
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 Value Parameter Reference
CACA Rn Agonist 4.1 pEC50 3
⤷ pEC50 4.1 (EC50 7.4x10-5 M) [3]
(±)-cis-2-CAMP Hs Full agonist - -
⤷ [Binds to: GABA site]
5-Me-IAA Hs Full agonist - -
⤷ [Binds to: GABA site]
isoguvacine Hs Partial agonist - -
⤷ [Binds to: GABA site]
muscimol 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 Hs Antagonist - -
⤷ [Binds to: GABA site]
trans-3-ACPBPA Hs Antagonist - -
⤷ [Binds to: GABA site]
aza-THIP Hs Antagonist - -
⤷ [Binds to: GABA site]
isonipecotic acid Hs Antagonist - -
⤷ [Binds to: GABA site]
piperidine-4-sulphonic acid Hs Antagonist - -
⤷ [Binds to: GABA site]
gaboxadol Hs Antagonist - -
⤷ [Binds to: GABA site]
TPMPA 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 Hs - no - - - no
⤷
Not voltage dependent
TBPS 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. U.S.A., 88 (7): 2673-7. [PMID:1849271]

3. 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]

4. 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. U.S.A., 92 (25): 11756-60. [PMID:8524843]

Contributors

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How to cite this page

Delia Belelli, Tim G. Hales, Jeremy J. Lambert, Bernhard Luscher, Richard Olsen, John A. Peters, Uwe Rudolph, Werner Sieghart.
GABAA receptors: GABAA receptor ρ1 subunit. Last modified on 21/03/2019. Accessed on 26/08/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=420.