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GAL1 receptor

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Target not currently curated in GtoImmuPdb

Target id: 243

Nomenclature: GAL1 receptor

Family: Galanin receptors

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 349 18q23 GALR1 galanin receptor 1 67
Mouse 7 348 18 55.78 cM Galr1 galanin receptor 1 38,98
Rat 7 346 18q12.3 Galr1 galanin receptor 1 15
Previous and Unofficial Names Click here for help
GALNR | GALNR1
Database Links Click here for help
Specialist databases
GPCRDB galr1_human (Hs), galr1_mouse (Mm), galr1_rat (Rn)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
galanin {Sp: Human} , galanin {Sp: Mouse, Rat}
galanin-like peptide {Sp: Human} , galanin-like peptide {Sp: Mouse} , galanin-like peptide {Sp: Rat}
Comments: Galanin is more potent than galanin-like peptide
Potency order of endogenous ligands (Human)
galanin (GAL, P22466) > galanin-like peptide (GALP, Q9UBC7)  [68]

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I][Tyr26]galanin (pig) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Agonist 9.5 – 10.7 pKd 15,20,22,71,85-86
pKd 9.5 – 10.7 (Kd 3x10-10 – 1.9x10-11 M) Two populations of binding sites have been identified in transfected cells with Kds of 0.3 and 0.019nM. [15,20,22,71,85-86]
[125I][Tyr26]galanin (rat/mouse) Peptide Ligand is labelled Ligand is radioactive Mm Agonist 9.9 pKd 98
pKd 9.9 (Kd 1.34x10-10 M) [98]
[125I][Tyr26]galanin (pig) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist 9.8 pKd 11
pKd 9.8 (Kd 1.5x10-10 M) [11]
[19Lys,26Leu]-galparan Peptide Rn Agonist 9.1 pKd 46
pKd 9.1 (Kd 7.1x10-10 M) [46]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Rn Full agonist 9.1 pKd 46
pKd 9.1 (Kd 7.4x10-10 M) [46]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Hs Full agonist 9.1 pKd 29
pKd 9.1 (Kd 8x10-10 M) [29]
[125I][Tyr26]galanin (human) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist 7.8 – 10.3 pKd 24
pKd 10.3 (Kd 4.89x10-11 M) High affinity receptors [24]
pKd 7.8 (Kd 1.47x10-8 M) Low affinity receptors [24]
galparan Peptide Rn Agonist 8.2 pKd 46
pKd 8.2 (Kd 6.4x10-9 M) [46]
galanin(1-13)amide Peptide Rn Agonist 6.9 pKd 46
pKd 6.9 (Kd 1.25x10-7 M) [46]
[2Ala]-galparan Peptide Rn Agonist 5.8 pKd 46
pKd 5.8 (Kd 1.585x10-6 M) [46]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Hs Full agonist 9.6 – 10.6 pKi 11,24,29
pKi 9.6 – 10.6 (Ki 2.3x10-10 – 2.5x10-11 M) [11,24,29]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Mm Full agonist 9.3 – 10.3 pKi 70,98
pKi 9.3 – 10.3 (Ki 4.6x10-10 – 4.7x10-11 M) [70,98]
galanin {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 9.1 – 10.5 pKi 11,24,29,82
pKi 9.1 – 10.5 (Ki 8x10-10 – 3.1x10-11 M) [11,24,29,82]
M617 Peptide Click here for species-specific activity table Hs Agonist 9.6 pKi 55
pKi 9.6 (Ki 2.3x10-10 M) [55]
M242 Peptide Click here for species-specific activity table Hs Agonist 9.6 pKi 82
pKi 9.6 (Ki 2.5x10-10 M) [82]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Rn Full agonist 9.0 – 10.1 pKi 15,86,94,96-97
pKi 9.0 – 10.1 (Ki 1x10-9 – 8x10-11 M) [15,86,94,96-97]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Rn Full agonist 9.1 – 10.0 pKi 15,71,85-86
pKi 9.1 – 10.0 (Ki 8.2x10-10 – 1x10-10 M) [15,71,85-86]
galanin {Sp: Human} Peptide Click here for species-specific activity table Rn Full agonist 9.2 – 9.9 pKi 15,86
pKi 9.2 – 9.9 (Ki 6x10-10 – 1.4x10-10 M) [15,86]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Hs Full agonist 8.8 – 10.1 pKi 11,29,53,55,78,81,88
pKi 8.8 – 10.1 (Ki 1.75x10-9 – 8x10-11 M) [11,29,53,55,78,81,88]
Gal-(K)4 Peptide Click here for species-specific activity table Hs Agonist 9.4 pKi 106
pKi 9.4 (Ki 4x10-10 M) [106]
Gal-B2-MPEG4 Peptide Click here for species-specific activity table Hs Agonist 9.3 pKi 106
pKi 9.3 (Ki 5x10-10 M) [106]
Gal-B2-C8 Peptide Click here for species-specific activity table Hs Agonist 9.1 pKi 106
pKi 9.1 (Ki 7x10-10 M) [106]
Gal-B2-dPEG24 Peptide Click here for species-specific activity table Hs Agonist 8.9 pKi 105
pKi 8.9 (Ki 1.3x10-9 M) [105]
Gal-B2-C10 Peptide Click here for species-specific activity table Hs Agonist 8.9 pKi 106
pKi 8.9 (Ki 1.3x10-9 M) [106]
Gal-B2-C12 Peptide Click here for species-specific activity table Hs Agonist 8.9 pKi 106
pKi 8.9 (Ki 1.4x10-9 M) [106]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Mm Agonist 8.7 – 9.0 pKi 70,98
pKi 8.7 – 9.0 (Ki 2.2x10-9 – 1.02x10-9 M) [70,98]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Hs Agonist 8.3 – 9.3 pKi 11,14,24,29
pKi 8.3 – 9.3 (Ki 5x10-9 – 5x10-10 M) [11,14,24,29]
Gal-B2-C14 Peptide Click here for species-specific activity table Hs Agonist 8.6 pKi 106
pKi 8.6 (Ki 2.6x10-9 M) [106]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Rn Agonist 8.1 – 9.0 pKi 15,71,85-86,94,96-97
pKi 8.1 – 9.0 (Ki 9x10-9 – 9.5x10-10 M) [15,71,85-86,94,96-97]
Gal-B2 Peptide Click here for species-specific activity table Hs Agonist 8.5 pKi 14
pKi 8.5 (Ki 3.5x10-9 M) [14]
Gal-B2-C18 Peptide Click here for species-specific activity table Hs Agonist 8.4 pKi 106
pKi 8.4 (Ki 4x10-9 M) [106]
galanin(1-15) Peptide Click here for species-specific activity table Rn Agonist 7.9 – 8.5 pKi 71,85
pKi 7.9 – 8.5 (Ki 1.15x10-8 – 3x10-9 M) [71,85]
galanin(7-29) (pig) Peptide Click here for species-specific activity table Hs Agonist 8.2 pKi 11
pKi 8.2 (Ki 6.76x10-9 M) [11]
galanin(2-29) (pig) Peptide Rn Full agonist 7.1 – 8.1 pKi 15,71
pKi 7.1 – 8.1 (Ki 8.25x10-8 – 7.14x10-9 M) [15,71]
galanin(7-29) (pig) Peptide Click here for species-specific activity table Rn Agonist 7.6 pKi 86
pKi 7.6 (Ki 2.455x10-8 M) [86]
J20 (galanin analogue) Peptide Click here for species-specific activity table Hs Agonist 7.6 pKi 79
pKi 7.6 (Ki 2.5x10-8 M) [79]
galanin(2-29) (pig) Peptide Click here for species-specific activity table Hs Full agonist 7.6 pKi 11
pKi 7.6 (Ki 2.63x10-8 M) [11]
galanin(2-29) (rat/mouse) Peptide Click here for species-specific activity table Mm Full agonist 7.1 – 8.0 pKi 70,98
pKi 7.1 – 8.0 (Ki 8.46x10-8 – 1.08x10-8 M) [70,98]
galanin(2-30) (human) Peptide Click here for species-specific activity table Hs Agonist 7.3 pKi 17
pKi 7.3 (Ki 5.2x10-8 M) [17]
M1151 Peptide Click here for species-specific activity table Hs Agonist 7.0 pKi 81
pKi 7.0 (Ki 9.86x10-8 M) [81]
J18 (galanin analogue) Peptide Click here for species-specific activity table Hs Agonist 6.9 pKi 79
pKi 6.9 (Ki 1.38x10-7 M) [79]
galanin(2-29) (rat/mouse) Peptide Click here for species-specific activity table Rn Full agonist 6.0 – 7.1 pKi 94,96-97
pKi 6.0 – 7.1 (Ki 1.1x10-6 – 8.5x10-8 M) [94,96-97]
[N-Me,des-Sar]Gal-B2 Peptide Click here for species-specific activity table Hs Agonist 6.4 pKi 77
pKi 6.4 (Ki 3.645x10-7 M) [77]
Gal-B5 Peptide Click here for species-specific activity table Hs Agonist 6.4 pKi 14
pKi 6.4 (Ki 3.87x10-7 M) [14]
M1145 Peptide Click here for species-specific activity table Hs Agonist 6.2 pKi 78
pKi 6.2 (Ki 5.87x10-7 M) [78]
galanin(D-Trp2) (pig) Peptide Click here for species-specific activity table Hs Agonist 6.2 pKi 11
pKi 6.2 (Ki 6.31x10-7 M) [11]
galanin(D-Trp2) (pig) Peptide Click here for species-specific activity table Rn Agonist 6.0 – 6.4 pKi 85-86
pKi 6.0 – 6.4 (Ki 1x10-6 – 4.074x10-7 M) [85-86]
galanin(3-29) (pig) Peptide Click here for species-specific activity table Rn Agonist <6.0 pKi 15,71,85-86
pKi <6.0 (Ki >1x10-6 M) [15,71,85-86]
galanin(3-29) (rat/mouse) Peptide Click here for species-specific activity table Rn Agonist <6.0 pKi 94,97
pKi <6.0 (Ki >1x10-6 M) [94,97]
galanin(10-29) (pig) Peptide Click here for species-specific activity table Rn Agonist <6.0 pKi 71
pKi <6.0 (Ki >1x10-6 M) [71]
galanin(3-29) (rat/mouse) Peptide Click here for species-specific activity table Mm Agonist <5.8 pKi 70
pKi <5.8 (Ki >1.65x10-6 M) [70]
galanin(10-29) (rat/mouse) Peptide Click here for species-specific activity table Mm Agonist <5.8 pKi 70
pKi <5.8 (Ki >1.67x10-6 M) [70]
M1153 Peptide Click here for species-specific activity table Hs Agonist 5.7 pKi 81
pKi 5.7 (Ki 1.89x10-6 M) [81]
M1152 Peptide Click here for species-specific activity table Hs Agonist 5.6 pKi 81
pKi 5.6 (Ki 2.37x10-6 M) [81]
galanin(3-29) (pig) Peptide Click here for species-specific activity table Hs Agonist <5.0 – 6.0 pKi 11,29
pKi <5.0 – 6.0 (Ki >1x10-5 – 1x10-6 M) [11,29]
galanin(2-11) Peptide Click here for species-specific activity table Hs Agonist <5.3 pKi 53
pKi <5.3 (Ki >5x10-6 M) [53]
galnon Small molecule or natural product Hs Agonist 4.9 pKi 5,87
pKi 4.9 (Ki 1.17x10-5 M) [5,87]
M1160 Peptide Click here for species-specific activity table Hs Agonist 4.8 pKi 80
pKi 4.8 (Ki 1.55x10-5 M) [80]
galmic Small molecule or natural product Hs Agonist 4.5 pKi 5,87
pKi 4.5 (Ki 3.42x10-5 M) [5,87]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Rn Full agonist 9.8 pEC50 68
pEC50 9.8 (EC50 1.6x10-10 M) [68]
galanin-like peptide {Sp: Pig} Peptide Click here for species-specific activity table Rn Agonist 7.5 pEC50 68
pEC50 7.5 (EC50 3x10-8 M) [68]
galanin {Sp: Human} Peptide Click here for species-specific activity table Rn Full agonist 10.1 – 10.2 pIC50 33,91
pIC50 10.1 – 10.2 (IC50 7x10-11 – 6x10-11 M) [33,91]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Rn Full agonist 10.1 – 10.2 pIC50 33,91
pIC50 10.1 – 10.2 (IC50 7x10-11 – 6x10-11 M) [33,91]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Hs Full agonist 9.9 pIC50 22
pIC50 9.9 (IC50 1.3x10-10 M) [22]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Hs Full agonist 9.8 – 9.9 pIC50 22,91
pIC50 9.8 – 9.9 (IC50 1.6x10-10 – 1.4x10-10 M) [22,91]
galanin(1-19) (human) Peptide Rn Agonist 9.8 pIC50 91
pIC50 9.8 (IC50 1.5x10-10 M) [91]
galanin {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 9.6 – 9.9 pIC50 22,49,91
pIC50 9.6 – 9.9 (IC50 2.7x10-10 – 1.3x10-10 M) [22,49,91]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Rn Agonist 9.6 pIC50 33,91
pIC50 9.6 (IC50 2.7x10-10 M) [33,91]
galanin(1-19) (human) Peptide Hs Agonist 9.5 pIC50 91
pIC50 9.5 (IC50 3.4x10-10 M) [91]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Rn Full agonist 8.9 – 10.0 pIC50 13,68
pIC50 8.9 – 10.0 (IC50 1.4x10-9 – 9.7x10-11 M) [13,68]
[Sar1, D-Ala12]galanin(1-16) Peptide Hs Agonist 9.4 pIC50 47
pIC50 9.4 (IC50 4x10-10 M) [47]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Hs Agonist 9.0 – 9.2 pIC50 22,91
pIC50 9.0 – 9.2 (IC50 1.01x10-9 – 6x10-10 M) [22,91]
galanin(1-11) Peptide Hs Agonist 9.0 pIC50 49
pIC50 9.0 (IC50 1.1x10-9 M) [49]
galanin(1-15) Peptide Click here for species-specific activity table Hs Agonist 8.8 pIC50 22
pIC50 8.8 (IC50 1.68x10-9 M) [22]
galanin-like peptide {Sp: Pig} Peptide Click here for species-specific activity table Rn Agonist 8.4 pIC50 68
pIC50 8.4 (IC50 4.3x10-9 M) [68]
galanin(2-29) (rat/mouse) Peptide Click here for species-specific activity table Rn Full agonist 8.1 pIC50 33,91
pIC50 8.1 (IC50 7.2x10-9 M) [33,91]
galanin(2-29) (rat/mouse) Peptide Click here for species-specific activity table Hs Full agonist 8.0 pIC50 91
pIC50 8.0 (IC50 1x10-8 M) [91]
galanin(2-29) (pig) Peptide Click here for species-specific activity table Hs Full agonist 7.5 pIC50 22
pIC50 7.5 (IC50 3.04x10-8 M) [22]
GALP(3-32) (human) Peptide Click here for species-specific activity table Hs Agonist 7.5 pIC50 44
pIC50 7.5 (IC50 3.3x10-8 M) [44]
galanin-like peptide {Sp: Rat} Peptide Click here for species-specific activity table Rn Agonist 7.3 pIC50 13
pIC50 7.3 (IC50 4.5x10-8 M) [13]
galanin-like peptide {Sp: Human} Peptide Click here for species-specific activity table Hs Agonist 7.1 pIC50 44
pIC50 7.1 (IC50 7.7x10-8 M) [44]
GALP(1-32) (human) Peptide Click here for species-specific activity table Hs Agonist 6.9 pIC50 44
pIC50 6.9 (IC50 1.29x10-7 M) [44]
galanin(2-11) Peptide Click here for species-specific activity table Hs Agonist 6.1 pIC50 49
pIC50 6.1 (IC50 8.79x10-7 M) [49]
galanin(3-29) (pig) Peptide Click here for species-specific activity table Hs Agonist <6.0 pIC50 22
pIC50 <6.0 (IC50 >1x10-6 M) [22]
galanin(3-29) (rat/mouse) Peptide Click here for species-specific activity table Hs Agonist <6.0 pIC50 91
pIC50 <6.0 (IC50 >1x10-6 M) [91]
galanin(3-29) (rat/mouse) Peptide Click here for species-specific activity table Rn Agonist <6.0 pIC50 33,91
pIC50 <6.0 (IC50 >1x10-6 M) [33,91]
alarin {Sp: Rat} Peptide Click here for species-specific activity table Rn Agonist <6.0 pIC50 13
pIC50 <6.0 (IC50 >1x10-6 M) [13]
View species-specific agonist tables
Agonist Comments
Rat and mouse galanin sequences are identical [54]. Binding affinity is lost with removal of amino acids 1 and 2 of galanin [11].
Galanin(D-Trp2) and galanin(2-29) both have higher binding affinity for GAL2 than GAL1 receptors [11].
Many different galanin analogues were trialled in [14] and [77]. The most active compounds are reported in the table above. The Ki values of other analogues are listed in these publications.

[94] and [24] have data for two types of radioligand binding assays; membrane binding and whole-cell binding assays.

NOTE that compounds with -ve log10 affinities <6 have no appreciable agonist function.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
M15 Peptide Click here for species-specific activity table Hs Antagonist 9.4 – 10.6 pKi 11,24,53
pKi 9.4 – 10.6 (Ki 4x10-10 – 2.7x10-11 M) [11,24,53]
M40 Peptide Click here for species-specific activity table Mm Antagonist 9.4 – 10.4 pKi 70,98
pKi 9.4 – 10.4 (Ki 4.3x10-10 – 4x10-11 M) [70,98]
M32 Peptide Click here for species-specific activity table Hs Antagonist 9.6 – 9.7 pKi 11,82
pKi 9.6 – 9.7 (Ki 2.6x10-10 – 1.8x10-10 M) [11,82]
C7 Peptide Click here for species-specific activity table Hs Antagonist 9.2 – 10.1 pKi 11,24
pKi 9.2 – 10.1 (Ki 6.9x10-10 – 8.2x10-11 M) [11,24]
M35 Peptide Click here for species-specific activity table Hs Antagonist 8.3 – 10.9 pKi 11,24,53
pKi 8.3 – 10.9 (Ki 4.8x10-9 – 1.2x10-11 M) [11,24,53]
M35 Peptide Click here for species-specific activity table Rn Antagonist 9.3 – 9.5 pKi 71,85-86
pKi 9.3 – 9.5 (Ki 4.6x10-10 – 3x10-10 M) [71,85-86]
M40 Peptide Click here for species-specific activity table Hs Antagonist 8.6 – 10.0 pKi 11,24,53
pKi 8.6 – 10.0 (Ki 2.4x10-9 – 1.1x10-10 M) [11,24,53]
M32 Peptide Click here for species-specific activity table Rn Antagonist 9.2 – 9.2 pKi 85-86
pKi 9.2 – 9.2 (Ki 6.8x10-10 – 6x10-10 M) [85-86]
C7 Peptide Click here for species-specific activity table Mm Antagonist 8.7 – 9.0 pKi 70,98
pKi 8.7 – 9.0 (Ki 2x10-9 – 9.6x10-10 M) [70,98]
C7 Peptide Click here for species-specific activity table Rn Antagonist 7.8 – 9.6 pKi 71,85-86
pKi 7.8 – 9.6 (Ki 1.6x10-8 – 2.8x10-10 M) [71,85-86]
M15 Peptide Click here for species-specific activity table Rn Antagonist 8.0 – 9.2 pKi 71,85-86,96
pKi 8.0 – 9.2 (Ki 1x10-8 – 6.5x10-10 M) [71,85-86,96]
M15 Peptide Click here for species-specific activity table Mm Antagonist 8.2 – 8.6 pKi 70,98
pKi 8.2 – 8.6 (Ki 6.3x10-9 – 2.24x10-9 M) [70,98]
M40 Peptide Click here for species-specific activity table Rn Antagonist 7.9 – 8.4 pKi 71,85-86
pKi 7.9 – 8.4 (Ki 1.13x10-8 – 4x10-9 M) [71,85-86]
M871 Peptide Click here for species-specific activity table Hs Antagonist 6.4 pKi 88
pKi 6.4 (Ki 4.2x10-7 M) [88]
Sch 202596 Small molecule or natural product Hs Antagonist 5.8 pKi 16
pKi 5.8 (Ki 1.7x10-6 M) [16]
GalR3ant Small molecule or natural product Hs Antagonist <5.0 pKi 52
pKi <5.0 (Ki >1x10-5 M) [52]
M35 Peptide Click here for species-specific activity table Rn Antagonist 11.0 pIC50 33,91
pIC50 11.0 (IC50 1x10-11 M) [33,91]
M35 Peptide Click here for species-specific activity table Hs Antagonist 10.4 pIC50 91
pIC50 10.4 (IC50 4x10-11 M) [91]
M40 Peptide Click here for species-specific activity table Hs Antagonist 9.3 pIC50 91
pIC50 9.3 (IC50 5x10-10 M) [91]
M40 Peptide Click here for species-specific activity table Rn Antagonist 9.1 pIC50 33,91
pIC50 9.1 (IC50 9x10-10 M) [33,91]
M15 Peptide Click here for species-specific activity table Rn Antagonist 9.0 pIC50 33,91
pIC50 9.0 (IC50 1x10-9 M) [33,91]
M15 Peptide Click here for species-specific activity table Hs Antagonist 8.8 – 8.8 pIC50 22,91
pIC50 8.8 – 8.8 (IC50 1.5x10-9 – 1.46x10-9 M) [22,91]
C7 Peptide Click here for species-specific activity table Hs Antagonist 8.2 – 9.0 pIC50 22,91
pIC50 8.2 – 9.0 (IC50 6.3x10-9 – 1.04x10-9 M) [22,91]
C7 Peptide Click here for species-specific activity table Rn Antagonist 8.3 pIC50 33,91
pIC50 8.3 (IC50 4.9x10-9 M) [33,91]
dithiipin-1,1,4,4-tetroxide analogue 7 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.7 pIC50 84
pIC50 6.7 (IC50 1.9x10-7 M) [84]
2,3-dihydro-1,4-dithiin-1,1,4,4-tetroxide Small molecule or natural product Hs Antagonist 5.6 pIC50 84
pIC50 5.6 (IC50 2.7x10-6 M) [84]
View species-specific antagonist tables
Antagonist Comments
In [84] a series of compounds was tested. The IC50 values for two of the analogues at the human GAL1 receptor are reported in the table above. Analogue 7 is reported as the first non-peptidic sub-micromolar antagonist to human GAL1 receptor.
GalR3ant displays receptor selectivity for GAL3 receptor, with low affinity for GAL1 and GAL2 receptors [53].
[24] has radioligand binding data for both membrane and whole-cell based assays.
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Adenylyl cyclase inhibition
Potassium channel
Comments:  Stimulation of GAL1 receptor transfected cells inhibits forskolin-stimulated cAMP production in a pertussis toxin-sensitive manner [24,29,71,85]. GAL1 receptor activation opens G-protein-regulated inwardly rectifying K+ (GIRK) channels [86] and stimulates pertussis-toxin sensitive MAPK activity, which is inhibited by expression of the C-terminus of β-adrenergic receptor kinase (which specifically inhibits G-βγ signalling). This demonstrates that GAL1 receptor couples to a Gi/βγ signalling pathway to mediate MAPK activation [95] (reviewed in [45]).
References:  7,29,71,86
Tissue Distribution Click here for help
Bowes melanoma cell line > small intestine and fetal brain. None in colon adenocarcinoma cell line (HT29) or human liver.
Species:  Human
Technique:  Northern blot.
References:  29
Low expression. In periphery, most abundant in heart, small intestine, prostate, testes; in central nervous system, most abundant in cerebral cortex, amygdala, substantia nigra (not detectable in cerebellum).
Species:  Human
Technique:  RT-PCR.
References:  91
GAL1 receptor expressed in human gastrointestinal tract from oesophagus to rectum: largest amount in duodenum and least amount in gastric fundus.
Species:  Human
Technique:  RT-PCR.
References:  51
GAL1 receptor mRNA in > 20% of all lumbar 4 and 5 dorsal root ganglion neuron profiles, mainly small and medium sized neurons; almost all expressed CGRP mRNA. GAL1 receptor mRNA levels were transiently down-regulated by inflammation and more strongly by peripheral nerve injury
Species:  Rat
Technique:  In situ hybridisation.
References:  104
Bed nucleus of the accessory olfactory tract > Hypothalamic paraventricular nucleus (lateral magnocellular); thalamic paraventricular nucleus; subiculum (ventral); lateral parabrachial nucleus > supraoptic nucleus; dorsomedial nucleus; thalamic central medial nucleus; paracentral nucleus; CA1 (ventral region); medial (anteroventral) amygdala > insular cortex (granular); lateral septum (dorsal, ventral regions); bed nucleus of stria terminalis; medial preoptic area; anterior medial preoptic nucleus; medial preoptic nucleus; hypothalamic paraventricular nucleus (medial parvocellular); lateroanterior hypothalamic nucleus; ventromedial nucleus (ventrolateral region); lateral habenula; anterior cortical amygdala; basolmedial amygdala; amygdaloid piriform transition; posterior cortical nucleus; locus coeruleus; pontine reticular formation > taenia tecta (anterior region); septohippocampal nucleus; lateral preoptic area; subfornical organ; anterior hypothalamic area; lateral hypothalamus (tuberal region); mammillary nuclei; posterior hypothalamic area; anterodorsal thalamic nucleus; intermediodorsal nucleus; zona incerta; subincertal nucleus; precommissural nucleus; entorhinal cortex; medial amygdala (anterodorsal); central nucleus of the amygdala; ventral tegmental area; central grey; lateral substantia nigra.
Species:  Rat
Technique:  In situ hybridisat