Nomenclature: GAL2 receptor

Family: Galanin receptors

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Contents

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 387 17q25.3 GALR2 galanin receptor 2
Mouse 7 371 11 E2 Galr2 galanin receptor 2
Rat 7 372 10q32.3 Galr2 galanin receptor 2
Previous and Unofficial Names
Galanin-2 receptor
GALNR2
GAL2-R
GALR-2
galanin receptor 2
galanin receptor type 2
mGalR
gal2
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
PhosphoSitePlus
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Natural/Endogenous Ligands
galanin {Sp: Human} , galanin {Sp: Mouse, Rat}
galanin-like peptide {Sp: Human} , galanin-like peptide {Sp: Mouse} , galanin-like peptide {Sp: Rat}
Rank order of potency (Human)
galanin-like peptide (GALP, Q9UBC7) ≥ galanin (GAL, P22466)  [39]
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I][Tyr26]galanin (pig) Hs Agonist 9.92 pKd 17
pKd 9.92 (Kd 1.2x10-10 M) [17]
[125I][Tyr26]galanin (human) Hs Agonist 9.51 – 9.62 pKd 5-6,25
pKd 9.51 – 9.62 (Kd 3.1x10-10 – 2.4x10-10 M) [5-6,25]
[125I][Tyr26]galanin (human) Mm Agonist 9.33 pKd 40
pKd 9.33 (Kd 4.7x10-10 M) [40]
[125I][Tyr26]galanin (human) Rn Agonist 9.23 pKd 59
pKd 9.23 (Kd 5.9x10-10 M) [59]
[125I][Tyr26]galanin (pig) Rn Agonist 8.4 – 9.89 pKd 12,18,52,59
pKd 8.4 – 9.89 (Kd 4x10-9 – 1.3x10-10 M) [12,18,52,59]
galmic Rn Agonist <5.0 pKd 3,31
pKd <5.0 (Kd >1x10-5 M) [3,31]
galanin(1-15) Rn Agonist 9.15 pKi 51
pKi 9.15 (Ki 7x10-10 M) [51]
galanin {Sp: Pig} Rn Full agonist 8.98 – 9.3 pKi 51-52
pKi 8.98 – 9.3 (Ki 1.05x10-9 – 5x10-10 M) [51-52]
galanin(1-20) (human) Hs Agonist 9.11 pKi 5
pKi 9.11 (Ki 7.8x10-10 M) [5]
galanin(2–29) (rat/mouse) Hs Full agonist 9.04 pKi 5
pKi 9.04 (Ki 9.1x10-10 M) [5]
galanin {Sp: Pig} Hs Full agonist 9.02 pKi 6
pKi 9.02 (Ki 9.5x10-10 M) [6]
galanin {Sp: Human} Hs Full agonist 8.63 – 9.07 pKi 5-6,46
pKi 8.63 – 9.07 (Ki 2.34x10-9 – 8.6x10-10 M) [5-6,46]
galanin {Sp: Mouse, Rat} Rn Full agonist 8.25 – 9.25 pKi 31,40,52,58-60
pKi 8.25 – 9.25 (Ki 5.6x10-9 – 5.6x10-10 M) [31,40,52,58-60]
galanin {Sp: Mouse, Rat} Hs Full agonist 8.53 – 8.81 pKi 5-6,34,42,45,53
pKi 8.53 – 8.81 (Ki 2.98x10-9 – 1.54x10-9 M) [5-6,34,42,45,53]
galanin {Sp: Human} Rn Full agonist 8.6 pKi 52
pKi 8.6 (Ki 2.51x10-9 M) [52]
galanin(7-29) (pig) Rn Agonist 8.6 pKi 5
pKi 8.6 (Ki 2.51x10-9 M) [5]
galanin(2-29) (pig) Hs Full agonist 8.54 pKi 6
pKi 8.54 (Ki 2.88x10-9 M) [6]
galanin(1-15) Hs Agonist 8.46 pKi 5
pKi 8.46 (Ki 3.5x10-9 M) [5]
galanin {Sp: Mouse, Rat} Mm Full agonist 8.41 pKi 40
pKi 8.41 (Ki 3.9x10-9 M) [40]
galanin(2-30) (human) Hs Full agonist 8.0 – 8.74 pKi 5,11
pKi 8.0 – 8.74 (Ki 1x10-8 – 1.8x10-9 M) [5,11]
galanin(1-16) (rat/mouse/pig) Hs Agonist 7.89 – 8.8 pKi 5-6,8
pKi 7.89 – 8.8 (Ki 1.3x10-8 – 1.6x10-9 M) [5-6,8]
galanin(1-19) (rat/mouse) Rn Agonist 8.33 pKi 60
pKi 8.33 (Ki 4.7x10-9 M) [60]
galanin(1-16) (rat/mouse/pig) Rn Agonist 7.89 – 8.74 pKi 40,51-52,58-60
pKi 7.89 – 8.74 (Ki 1.3x10-8 – 1.8x10-9 M) [40,51-52,58-60]
J20 (galanin analogue) Hs Agonist 8.31 pKi 43
pKi 8.31 (Ki 4.9x10-9 M) [43]
galanin(7-29) (pig) Hs Full agonist 8.31 pKi 6
pKi 8.31 (Ki 4.9x10-9 M) [6]
M1153 Hs Agonist 8.3 pKi 45
pKi 8.3 (Ki 4.98x10-9 M) [45]
M617 Hs Agonist 8.24 pKi 34
pKi 8.24 (Ki 5.71x10-9 M) [34]
M242 Hs Agonist 8.23 pKi 46
pKi 8.23 (Ki 5.84x10-9 M) [46]
galanin(1-12) Hs Agonist 8.19 pKi 5
pKi 8.19 (Ki 6.4x10-9 M) [5]
M1145 Hs Full agonist 8.18 pKi 42
pKi 8.18 (Ki 6.55x10-9 M) [42]
galanin(2–29) (rat/mouse) Mm Full agonist 8.17 pKi 40
pKi 8.17 (Ki 6.8x10-9 M) [40]
[D-Trp2]galanin-(1–29) Rn Full agonist 8.15 pKi 51
pKi 8.15 (Ki 7x10-9 M) [51]
galanin(2–29) (rat/mouse) Rn Full agonist 7.25 – 8.72 pKi 40,58-60
pKi 7.25 – 8.72 (Ki 5.6x10-8 – 1.9x10-9 M) [40,58-60]
galanin(1-16) (rat/mouse/pig) Mm Agonist 7.93 pKi 40
pKi 7.93 (Ki 1.18x10-8 M) [40]
Gal-B2-dPEG24 Hs Agonist 7.87 pKi 66
pKi 7.87 (Ki 1.35x10-8 M) [66]
galanin(D-Trp2) (pig) Rn Agonist 7.56 – 8.15 pKi 51-52
pKi 7.56 – 8.15 (Ki 2.754x10-8 – 7x10-9 M) [51-52]
Gal-B2-C10 Hs Agonist 7.84 pKi 67
pKi 7.84 (Ki 1.44x10-8 M) [67]
Gal-B2-C8 Hs Agonist 7.83 pKi 67
pKi 7.83 (Ki 1.49x10-8 M) [67]
Gal-B2-C18 Hs Agonist 7.82 pKi 67
pKi 7.82 (Ki 1.5x10-8 M) [67]
Gal-B2-C12 Hs Agonist 7.79 pKi 67
pKi 7.79 (Ki 1.61x10-8 M) [67]
galanin(2-11) Hs Agonist 7.78 pKi 42
pKi 7.78 (Ki 1.66x10-8 M) [42]
Gal-B2-C14 Hs Agonist 7.74 pKi 67
pKi 7.74 (Ki 1.82x10-8 M) [67]
J18 (galanin analogue) Hs Agonist 7.7 pKi 43
pKi 7.7 (Ki 2x10-8 M) [43]
[N-Me,des-Sar]Gal-B2 Hs Agonist 7.69 pKi 41
pKi 7.69 (Ki 2.02x10-8 M) [41]
Gal-B2-MPEG4 Hs Agonist 7.69 pKi 67
pKi 7.69 (Ki 2.05x10-8 M) [67]
Gal-(K)4 Hs Agonist 7.62 pKi 67
pKi 7.62 (Ki 2.4x10-8 M) [67]
M1151 Hs Agonist 7.54 pKi 45
pKi 7.54 (Ki 2.89x10-8 M) [45]
M1160 Hs Agonist 7.48 pKi 44
pKi 7.48 (Ki 3.33x10-8 M) [44]
M1152 Hs Agonist 7.44 pKi 45
pKi 7.44 (Ki 3.64x10-8 M) [45]
Gal-B5 Hs Agonist 7.32 pKi 8
pKi 7.32 (Ki 4.8x10-8 M) [8]
Gal-B2 Hs Agonist 7.29 pKi 8
pKi 7.29 (Ki 5.15x10-8 M) [8]
Gal-R2-dPEG24 Hs Agonist 7.22 pKi 66
pKi 7.22 (Ki 6.04x10-8 M) [66]
galanin(2-11) Rn Agonist 7.06 pKi 30
pKi 7.06 (Ki 8.8x10-8 M) [30]
galanin(D-Trp2) (pig) Hs Agonist 6.7 pKi 6
pKi 6.7 (Ki 1.995x10-7 M) [6]
galanin (10-29) (rat/mouse) Hs Agonist <6.15 pKi 5
pKi <6.15 (Ki >7x10-7 M) [5]
galanin(1-10) Hs Agonist <6.15 pKi 5
pKi <6.15 (Ki >7x10-7 M) [5]
galanin(9-25) (rat/mouse) Hs Agonist <6.15 pKi 5
pKi <6.15 (Ki >7x10-7 M) [5]
galanin(3-29) (rat/mouse) Hs Agonist <6.15 pKi 5
pKi <6.15 (Ki >7x10-7 M) [5]
galanin(5-29) (rat/mouse) Hs Agonist <6.15 pKi 5
pKi <6.15 (Ki >7x10-7 M) [5]
galanin(9-29) (rat/mouse) Hs Agonist <6.15 pKi 5
pKi <6.15 (Ki >7x10-7 M) [5]
galanin(3-30) (human) Hs Agonist <6.15 pKi 5
pKi <6.15 (Ki >7x10-7 M) [5]
GMAP(1-41) {Sp: Pig} Rn Agonist <6.08 pKi 59
pKi <6.08 (Ki >8.4x10-7 M) [59]
galanin(3-29) (pig) Hs Agonist <6.0 pKi 6
pKi <6.0 (Ki >1x10-6 M) [6]
galanin(3-29) (pig) Rn Agonist <6.0 pKi 51-52
pKi <6.0 (Ki >1x10-6 M) [51-52]
GMAP(44-59) {Sp: Pig} Rn Agonist <6.0 pKi 60
pKi <6.0 (Ki >1x10-6 M) [60]
(D-Thr6, D-Trp8,9)galanin(1-15)ol Rn Agonist <5.9 pKi 59
pKi <5.9 (Ki >1.25x10-6 M) [59]
galanin(3-29) (rat/mouse) Rn Agonist 5.51 – 6.0 pKi 40,58,60
pKi 5.51 – 6.0 (Ki 3.125x10-6 – 1x10-6 M) [40,58,60]
galanin (10-29) (rat/mouse) Mm Agonist <5.73 pKi 40
pKi <5.73 (Ki >1.86x10-6 M) [40]
galanin(3-29) (rat/mouse) Mm Agonist <5.66 pKi 40
pKi <5.66 (Ki >2.2x10-6 M) [40]
galnon Rn Agonist 4.47 pKi 3,31
pKi 4.47 (Ki 3.41x10-5 M) [3,31]
galanin(1-15) Hs Agonist 9.14 pEC50 17
pEC50 9.14 (EC50 7.2x10-10 M) [17]
galanin-like peptide {Sp: Pig} Rn Agonist 8.62 pEC50 39
pEC50 8.62 (EC50 2.4x10-9 M) [39]
galanin {Sp: Human} Hs Full agonist 7.91 – 9.15 pEC50 6,17
pEC50 7.91 – 9.15 (EC50 1.23x10-8 – 7.1x10-10 M) [6,17]
galanin(1-16) (rat/mouse/pig) Hs Agonist 7.26 – 9.38 pEC50 6,17
pEC50 7.26 – 9.38 (EC50 5.495x10-8 – 4.2x10-10 M) [6,17]
galanin {Sp: Mouse, Rat} Rn Full agonist 8.28 pEC50 39
pEC50 8.28 (EC50 5.2x10-9 M) [39]
galanin(2-29) (pig) Hs Full agonist 7.62 – 8.93 pEC50 6,17
pEC50 7.62 – 8.93 (EC50 2.399x10-8 – 1.17x10-9 M) [6,17]
galanin {Sp: Pig} Hs Full agonist 8.09 pEC50 6
pEC50 8.09 (EC50 8.12x10-9 M) [6]
galanin {Sp: Pig} Rn Full agonist 7.74 pEC50 51
pEC50 7.74 (EC50 1.8x10-8 M) [51]
galanin(7-29) (pig) Hs Agonist 7.46 pEC50 6
pEC50 7.46 (EC50 3.467x10-8 M) [6]
galanin(1-15) Rn Agonist 7.19 pEC50 51
pEC50 7.19 (EC50 6.5x10-8 M) [51]
galanin(1-16) (rat/mouse/pig) Rn Agonist 7.03 pEC50 51
pEC50 7.03 (EC50 9.4x10-8 M) [51]
galanin(D-Trp2) (pig) Rn Agonist 6.82 pEC50 51
pEC50 6.82 (EC50 1.5x10-7 M) [51]
galanin(D-Trp2) (pig) Hs Agonist 6.47 pEC50 6
pEC50 6.47 (EC50 3.388x10-7 M) [6]
galanin(3-29) (pig) Hs Agonist <6.0 pEC50 6
pEC50 <6.0 (EC50 >1x10-6 M) [6]
galanin(3-29) (pig) Rn Agonist <6.0 pEC50 51
pEC50 <6.0 (EC50 >1x10-6 M) [51]
galanin(10-29) (pig) Hs Agonist <6.0 pEC50 17
pEC50 <6.0 (EC50 >1x10-6 M) [17]
galanin-like peptide {Sp: Pig} Rn Agonist 9.62 pIC50 39
pIC50 9.62 (IC50 2.4x10-10 M) [39]
galanin {Sp: Pig} Hs Full agonist 9.46 pIC50 17
pIC50 9.46 (IC50 3.5x10-10 M) [17]
galanin {Sp: Pig} Rn Full agonist 9.34 – 9.43 pIC50 18,22
pIC50 9.34 – 9.43 (IC50 4.6x10-10 – 3.7x10-10 M) [18,22]
galanin {Sp: Human} Hs Full agonist 9.29 pIC50 17
pIC50 9.29 (IC50 5.1x10-10 M) [17]
galanin {Sp: Mouse, Rat} Rn Full agonist 8.72 – 9.32 pIC50 7,18,39
pIC50 8.72 – 9.32 (IC50 1.9x10-9 – 4.8x10-10 M) [7,18,39]
galanin {Sp: Human} Rn Full agonist 8.6 – 9.0 pIC50 18,22,29
pIC50 8.6 – 9.0 (IC50 2.5x10-9 – 1x10-9 M) [18,22,29]
galanin(1-11) Rn Agonist 8.78 pIC50 29
pIC50 8.78 (IC50 1.65x10-9 M) [29]
[Sar1, D-Ala12]galanin(1-16) Rn Agonist 8.76 pIC50 29
pIC50 8.76 (IC50 1.74x10-9 M) [29]
galanin(2-11) Rn Agonist 8.75 pIC50 29
pIC50 8.75 (IC50 1.76x10-9 M) [29]
galanin(2-29) (pig) Hs Full agonist 8.73 – 8.74 pIC50 17-18
pIC50 8.73 – 8.74 (IC50 1.87x10-9 – 1.8x10-9 M) [17-18]
galanin {Sp: Mouse, Rat} Hs Full agonist 7.93 – 9.47 pIC50 6,17
pIC50 9.47 (IC50 3.4x10-10 M) [17]
pIC50 7.93 – 9.12 (IC50 1.175x10-8 – 7.6x10-10 M) [6,17]
galanin(1-16) (rat/mouse/pig) Hs Agonist 8.66 pIC50 17
pIC50 8.66 (IC50 2.17x10-9 M) [17]
galanin(1-15) Hs Agonist 8.61 pIC50 17
pIC50 8.61 (IC50 2.47x10-9 M) [17]
galanin(2–29) (rat/mouse) Rn Full agonist 8.54 pIC50 22
pIC50 8.54 (IC50 2.9x10-9 M) [22]
galanin(1-16) (rat/mouse/pig) Rn Agonist 7.88 – 8.52 pIC50 18,22
pIC50 7.88 – 8.52 (IC50 1.32x10-8 – 3x10-9 M) [18,22]
galanin(1-15) Rn Agonist 8.13 pIC50 18
pIC50 8.13 (IC50 7.4x10-9 M) [18]
GALP(3-32) (human) Hs Agonist 7.82 pIC50 26
pIC50 7.82 (IC50 1.5x10-8 M) [26]
galanin-like peptide {Sp: Human} Hs Agonist 7.55 – 7.73 pIC50 7,26
pIC50 7.55 – 7.73 (IC50 2.8x10-8 – 1.87x10-8 M) [7,26]
GALP(1-32) (human) Hs Agonist 7.16 pIC50 26
pIC50 7.16 (IC50 6.9x10-8 M) [26]
alarin {Sp: Rat} Rn Agonist <6.0 pIC50 7
pIC50 <6.0 (IC50 >1x10-6 M) [7]
galanin(3-29) (rat/mouse) Rn Agonist <6.0 pIC50 22
pIC50 <6.0 (IC50 >1x10-6 M) [22]
galanin(3-29) (pig) Hs Agonist <6.0 pIC50 17-18
pIC50 <6.0 (IC50 >1x10-6 M) [17-18]
galanin(10-29) (pig) Rn Agonist 6.0 pIC50 18
pIC50 6.0 (IC50 1x10-6 M) [18]
View species-specific agonist tables
Agonist Comments
Binding affinity is lost with removal of amino acids 1 and 2 of galanin [6]. Galanin(D-Trp2) has a higher binding affinity for GAL2 receptor than GAL1 receptor.
In [58], affinities are given for both membrane binding assays and whole cell binding assays. Two populations of binding sites (larger population of low affinity/ smaller population of higher affinity) are identified in [18].

In [8] and [41] many different galanin analogues were trialled. The most active compounds are reported here. The Ki values of other analogues are listed in these publications. In [47] a series of 2,4,6-triaminopyridimines analogs were tested and found to have IC50 values in the range 300-100nM.

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 Affinity Units Reference
M32 Rn Antagonist 9.1 – 9.22 pKi 51-52
pKi 9.1 – 9.22 (Ki 7.9x10-10 – 6x10-10 M) [51-52]
M15 Am Antagonist 8.97 pKi 6
pKi 8.97 (Ki 1.07x10-9 M) [6]
C7 Hs Antagonist 8.7 – 9.2 pKi 5-6
pKi 8.7 – 9.2 (Ki 2x10-9 – 6.3x10-10 M) [5-6]
M15 Mm Antagonist 8.85 pKi 40
pKi 8.85 (Ki 1.4x10-9 M) [40]
M32 Hs Antagonist 8.66 – 8.84 pKi 6,46
pKi 8.66 – 8.84 (Ki 2.18x10-9 – 1.45x10-9 M) [6,46]
M35 Hs Antagonist 8.71 – 8.74 pKi 5-6
pKi 8.71 – 8.74 (Ki 1.95x10-9 – 1.8x10-9 M) [5-6]
M35 Rn Antagonist 8.09 – 9.22 pKi 31,40,51-52,59
pKi 8.09 – 9.22 (Ki 8.2x10-9 – 6x10-10 M) [31,40,51-52,59]
M40 Hs Antagonist 8.39 – 8.82 pKi 5-6
pKi 8.39 – 8.82 (Ki 4.07x10-9 – 1.5x10-9 M) [5-6]
M40 Mm Antagonist 8.55 pKi 40
pKi 8.55 (Ki 2.8x10-9 M) [40]
C7 Rn Antagonist 7.72 – 9.25 pKi 40,51-52,59
pKi 7.72 – 9.25 (Ki 1.9x10-8 – 5.6x10-10 M) [40,51-52,59]
M40 Rn Antagonist 7.74 – 9.15 pKi 31,40,51-52,59-60
pKi 7.74 – 9.15 (Ki 1.8x10-8 – 7x10-10 M) [31,40,51-52,59-60]
M15 Rn Antagonist 7.8 – 9.0 pKi 31,40,51-52,59-60
pKi 7.8 – 9.0 (Ki 1.57x10-8 – 1x10-9 M) [31,40,51-52,59-60]
M35 Mm Antagonist 8.31 pKi 40
pKi 8.31 (Ki 4.9x10-9 M) [40]
M871 Hs Antagonist 7.88 pKi 53
pKi 7.88 (Ki 1.31x10-8 M) [53]
C7 Mm Antagonist 7.85 pKi 40
pKi 7.85 (Ki 1.4x10-8 M) [40]
SNAP 398299 Hs Antagonist <6.0 pKi 56
pKi <6.0 (Ki >1x10-6 M) [56]
SNAP 37889 Hs Antagonist <5.0 pKi 56
pKi <5.0 (Ki >1x10-5 M) [56]
GalR3ant Rn Antagonist <5.0 pKi 31