GAL<sub>2</sub> receptor | Galanin receptors | IUPHAR/BPS Guide to PHARMACOLOGY

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GAL2 receptor

Target not currently curated in GtoImmuPdb

Target id: 244

Nomenclature: GAL2 receptor

Family: Galanin receptors

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

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
GALNR2
Database Links
Specialist databases
GPCRDB galr2_human (Hs), galr2_mouse (Mm), galr2_rat (Rn)
Other databases
ChEMBL Target CHEMBL3176 (Hs), CHEMBL5577 (Rn)
Ensembl Gene ENSG00000182687 (Hs), ENSMUSG00000020793 (Mm), ENSRNOG00000009407 (Rn)
Entrez Gene 8811 (Hs), 14428 (Mm), 29234 (Rn)
Human Protein Atlas ENSG00000182687 (Hs)
KEGG Gene hsa:8811 (Hs), mmu:14428 (Mm), rno:29234 (Rn)
OMIM 603691 (Hs)
RefSeq Nucleotide NM_003857 (Hs), NM_010254 (Mm), NM_019172 (Rn)
RefSeq Protein NP_003848 (Hs), NP_034384 (Mm), NP_062045 (Rn)
UniProtKB O43603 (Hs), O88854 (Mm), O08726 (Rn)
Wikipedia GALR2 (Hs)
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}
[125I][Tyr26]galanin (human)
Potency order of endogenous ligands (Human)
galanin-like peptide (GALP, Q9UBC7) ≥ galanin (GAL, P22466)  [39]

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
[125I][Tyr26]galanin (pig) Hs Agonist 9.5 – 9.9 pKd 6,17
⤷ pKd 9.9 (Kd 1.2x10-10 M) [17]
pKd 9.5 (Kd 3.1x10-10 M) [6]
[125I][Tyr26]galanin (human) Hs Agonist 9.5 – 9.6 pKd 5,25
⤷ pKd 9.5 – 9.6 (Kd 3.1x10-10 – 2.4x10-10 M) [5,25]
[125I][Tyr26]galanin (human) Mm Agonist 9.3 pKd 40
⤷ pKd 9.3 (Kd 4.7x10-10 M) [40]
[125I][Tyr26]galanin (human) Rn Agonist 9.2 pKd 59
⤷ pKd 9.2 (Kd 5.9x10-10 M) [59]
[125I][Tyr26]galanin (pig) Rn Agonist 8.4 – 9.9 pKd 12,18,52,59
⤷ pKd 8.4 – 9.9 (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 9.1 pKi 51
⤷ pKi 9.1 (Ki 7x10-10 M) [51]
galanin {Sp: Pig} Rn Full agonist 9.0 – 9.3 pKi 51-52
⤷ pKi 9.0 – 9.3 (Ki 1.05x10-9 – 5x10-10 M) [51-52]
galanin(1-20) (human) Hs Agonist 9.1 pKi 5
⤷ pKi 9.1 (Ki 7.8x10-10 M) [5]
galanin(2-29) (rat/mouse) Hs Full agonist 9.0 pKi 5
⤷ pKi 9.0 (Ki 9.1x10-10 M) [5]
galanin {Sp: Pig} Hs Full agonist 9.0 pKi 6
⤷ pKi 9.0 (Ki 9.5x10-10 M) [6]
galanin {Sp: Human} Hs Full agonist 8.6 – 9.1 pKi 5-6,46
⤷ pKi 8.6 – 9.1 (Ki 2.34x10-9 – 8.6x10-10 M) [5-6,46]
galanin {Sp: Mouse, Rat} Rn Full agonist 8.3 – 9.3 pKi 31,40,52,58-60
⤷ pKi 8.3 – 9.3 (Ki 5.6x10-9 – 5.6x10-10 M) [31,40,52,58-60]
galanin {Sp: Mouse, Rat} Hs Full agonist 8.5 – 8.8 pKi 5-6,34,42,45,53
⤷ pKi 8.5 – 8.8 (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 8.5 pKi 6
⤷ pKi 8.5 (Ki 2.88x10-9 M) [6]
galanin(1-15) Hs Agonist 8.5 pKi 5
⤷ pKi 8.5 (Ki 3.5x10-9 M) [5]
galanin {Sp: Mouse, Rat} Mm Full agonist 8.4 pKi 40
⤷ pKi 8.4 (Ki 3.9x10-9 M) [40]
galanin(2-30) (human) Hs Full agonist 8.0 – 8.7 pKi 5,11
⤷ pKi 8.0 – 8.7 (Ki 1x10-8 – 1.8x10-9 M) [5,11]
galanin(1-16) (rat/mouse/pig) Hs Agonist 7.9 – 8.8 pKi 5-6,8
⤷ pKi 7.9 – 8.8 (Ki 1.3x10-8 – 1.6x10-9 M) [5-6,8]
galanin(1-19) (rat/mouse) Rn Agonist 8.3 pKi 60
⤷ pKi 8.3 (Ki 4.7x10-9 M) [60]
galanin(1-16) (rat/mouse/pig) Rn Agonist 7.9 – 8.7 pKi 40,51-52,58-60
⤷ pKi 7.9 – 8.7 (Ki 1.3x10-8 – 1.8x10-9 M) [40,51-52,58-60]
J20 (galanin analogue) Hs Agonist 8.3 pKi 43
⤷ pKi 8.3 (Ki 4.9x10-9 M) [43]
galanin(7-29) (pig) Hs Full agonist 8.3 pKi 6
⤷ pKi 8.3 (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 8.2 pKi 34
⤷ pKi 8.2 (Ki 5.71x10-9 M) [34]
M242 Hs Agonist 8.2 pKi 46
⤷ pKi 8.2 (Ki 5.84x10-9 M) [46]
galanin(1-12) Hs Agonist 8.2 pKi 5
⤷ pKi 8.2 (Ki 6.4x10-9 M) [5]
M1145 Hs Full agonist 8.2 pKi 42
⤷ pKi 8.2 (Ki 6.55x10-9 M) [42]
galanin(2-29) (rat/mouse) Mm Full agonist 8.2 pKi 40
⤷ pKi 8.2 (Ki 6.8x10-9 M) [40]
[D-Trp2]galanin-(1-29) Rn Full agonist 8.1 pKi 51
⤷ pKi 8.1 (Ki 7x10-9 M) [51]
galanin(2-29) (rat/mouse) Rn Full agonist 7.3 – 8.7 pKi 40,58-60
⤷ pKi 7.3 – 8.7 (Ki 5.6x10-8 – 1.9x10-9 M) [40,58-60]
galanin(1-16) (rat/mouse/pig) Mm Agonist 7.9 pKi 40
⤷ pKi 7.9 (Ki 1.18x10-8 M) [40]
Gal-B2-dPEG24 Hs Agonist 7.9 pKi 67
⤷ pKi 7.9 (Ki 1.35x10-8 M) [67]
galanin(D-Trp2) (pig) Rn Agonist 7.6 – 8.1 pKi 51-52
⤷ pKi 7.6 – 8.1 (Ki 2.754x10-8 – 7x10-9 M) [51-52]
Gal-B2-C10 Hs Agonist 7.8 pKi 68
⤷ pKi 7.8 (Ki 1.44x10-8 M) [68]
Gal-B2-C8 Hs Agonist 7.8 pKi 68
⤷ pKi 7.8 (Ki 1.49x10-8 M) [68]
Gal-B2-C18 Hs Agonist 7.8 pKi 68
⤷ pKi 7.8 (Ki 1.5x10-8 M) [68]
Gal-B2-C12 Hs Agonist 7.8 pKi 68
⤷ pKi 7.8 (Ki 1.61x10-8 M) [68]
galanin(2-11) Hs Agonist 7.8 pKi 42
⤷ pKi 7.8 (Ki 1.66x10-8 M) [42]
Gal-B2-C14 Hs Agonist 7.7 pKi 68
⤷ pKi 7.7 (Ki 1.82x10-8 M) [68]
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 7.7 pKi 41
⤷ pKi 7.7 (Ki 2.02x10-8 M) [41]
Gal-B2-MPEG4 Hs Agonist 7.7 pKi 68
⤷ pKi 7.7 (Ki 2.05x10-8 M) [68]
Gal-(K)4 Hs Agonist 7.6 pKi 68
⤷ pKi 7.6 (Ki 2.4x10-8 M) [68]
M1151 Hs Agonist 7.5 pKi 45
⤷ pKi 7.5 (Ki 2.89x10-8 M) [45]
M1160 Hs Agonist 7.5 pKi 44
⤷ pKi 7.5 (Ki 3.33x10-8 M) [44]
M1152 Hs Agonist 7.4 pKi 45
⤷ pKi 7.4 (Ki 3.64x10-8 M) [45]
Gal-B5 Hs Agonist 7.3 pKi 8
⤷ pKi 7.3 (Ki 4.8x10-8 M) [8]
Gal-B2 Hs Agonist 7.3 pKi 8
⤷ pKi 7.3 (Ki 5.15x10-8 M) [8]
Gal-R2-dPEG24 Hs Agonist 7.2 pKi 67
⤷ pKi 7.2 (Ki 6.04x10-8 M) [67]
galanin(2-11) Rn Agonist 7.1 pKi 30
⤷ pKi 7.1 (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(3-29) (rat/mouse) Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(10-29) (rat/mouse) Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(5-29) (rat/mouse) Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(9-29) (rat/mouse) Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(9-25) (rat/mouse) Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(3-30) (human) Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(1-10) Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
GMAP(1-41) {Sp: Pig} Rn Agonist <6.1 pKi 59
⤷ pKi <6.1 (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 5.5 – 6.0 pKi 40,58,60
⤷ pKi 5.5 – 6.0 (Ki 3.125x10-6 – 1x10-6 M) [40,58,60]
galanin(10-29) (rat/mouse) Mm Agonist <5.7 pKi 40
⤷ pKi <5.7 (Ki >1.86x10-6 M) [40]
galanin(3-29) (rat/mouse) Mm Agonist <5.7 pKi 40
⤷ pKi <5.7 (Ki >2.2x10-6 M) [40]
galnon Rn Agonist 4.5 pKi 3,31
⤷ pKi 4.5 (Ki 3.41x10-5 M) [3,31]
galanin(1-15) Hs Agonist 9.1 pEC50 17
⤷ pEC50 9.1 (EC50 7.2x10-10 M) [17]
galanin-like peptide {Sp: Pig} Rn Agonist 8.6 pEC50 39
⤷ pEC50 8.6 (EC50 2.4x10-9 M) [39]
galanin {Sp: Human} Hs Full agonist 7.9 – 9.1 pEC50 6,17
⤷ pEC50 7.9 – 9.1 (EC50 1.23x10-8 – 7.1x10-10 M) [6,17]
galanin(1-16) (rat/mouse/pig) Hs Agonist 7.3 – 9.4 pEC50 6,17
⤷ pEC50 7.3 – 9.4 (EC50 5.495x10-8 – 4.2x10-10 M) [6,17]
galanin {Sp: Mouse, Rat} Rn Full agonist 8.3 pEC50 39
⤷ pEC50 8.3 (EC50 5.2x10-9 M) [39]
galanin(2-29) (pig) Hs Full agonist 7.6 – 8.9 pEC50 6,17
⤷ pEC50 7.6 – 8.9 (EC50 2.399x10-8 – 1.17x10-9 M) [6,17]
galanin {Sp: Pig} Hs Full agonist 8.1 pEC50 6
⤷ pEC50 8.1 (EC50 8.12x10-9 M) [6]
galanin {Sp: Pig} Rn Full agonist 7.7 pEC50 51
⤷ pEC50 7.7 (EC50 1.8x10-8 M) [51]
galanin(7-29) (pig) Hs Agonist 7.5 pEC50 6
⤷ pEC50 7.5 (EC50 3.467x10-8 M) [6]
galanin(1-15) Rn Agonist 7.2 pEC50 51
⤷ pEC50 7.2 (EC50 6.5x10-8 M) [51]
galanin(1-16) (rat/mouse/pig) Rn Agonist 7.0 pEC50 51
⤷ pEC50 7.0 (EC50 9.4x10-8 M) [51]
galanin(D-Trp2) (pig) Rn Agonist 6.8 pEC50 51
⤷ pEC50 6.8 (EC50 1.5x10-7 M) [51]
galanin(D-Trp2) (pig) Hs Agonist 6.5 pEC50 6
⤷ pEC50 6.5 (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 9.6 pIC50 39
⤷ pIC50 9.6 (IC50 2.4x10-10 M) [39]
galanin {Sp: Pig} Hs Full agonist 9.5 pIC50 17
⤷ pIC50 9.5 (IC50 3.5x10-10 M) [17]
galanin {Sp: Pig} Rn Full agonist 9.3 – 9.4 pIC50 18,22
⤷ pIC50 9.3 – 9.4 (IC50 4.6x10-10 – 3.7x10-10 M) [18,22]
galanin {Sp: Human} Hs Full agonist 9.3 pIC50 17
⤷ pIC50 9.3 (IC50 5.1x10-10 M) [17]
galanin {Sp: Mouse, Rat} Rn Full agonist 8.7 – 9.3 pIC50 7,18,39
⤷ pIC50 8.7 – 9.3 (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 8.8 pIC50 29
⤷ pIC50 8.8 (IC50 1.65x10-9 M) [29]
[Sar1, D-Ala12]galanin(1-16) Rn Agonist 8.8 pIC50 29
⤷ pIC50 8.8 (IC50 1.74x10-9 M) [29]
galanin(2-11) Rn Agonist 8.8 pIC50 29
⤷ pIC50 8.8 (IC50 1.76x10-9 M) [29]
galanin(2-29) (pig) Hs Full agonist 8.7 – 8.7 pIC50 17-18
⤷ pIC50 8.7 – 8.7 (IC50 1.87x10-9 – 1.8x10-9 M) [17-18]
galanin {Sp: Mouse, Rat} Hs Full agonist 7.9 – 9.5 pIC50 6,17
⤷ pIC50 9.5 (IC50 3.4x10-10 M) [17]
pIC50 7.9 – 9.1 (IC50 1.175x10-8 – 7.6x10-10 M) [6,17]
galanin(1-16) (rat/mouse/pig) Hs Agonist 8.7 pIC50 17
⤷ pIC50 8.7 (IC50 2.17x10-9 M) [17]
galanin(1-15) Hs Agonist 8.6 pIC50 17
⤷ pIC50 8.6 (IC50 2.47x10-9 M) [17]
galanin(2-29) (rat/mouse) Rn Full agonist 8.5 pIC50 22
⤷ pIC50 8.5 (IC50 2.9x10-9 M) [22]
galanin(1-16) (rat/mouse/pig) Rn Agonist 7.9 – 8.5 pIC50 18,22
⤷ pIC50 7.9 – 8.5 (IC50 1.32x10-8 – 3x10-9 M) [18,22]
galanin(1-15) Rn Agonist 8.1 pIC50 18
⤷ pIC50 8.1 (IC50 7.4x10-9 M) [18]
GALP(3-32) (human) Hs Agonist 7.8 pIC50 26
⤷ pIC50 7.8 (IC50 1.5x10-8 M) [26]
galanin-like peptide {Sp: Human} Hs Agonist 7.6 – 7.7 pIC50 7,26
⤷ pIC50 7.6 – 7.7 (IC50 2.8x10-8 – 1.87x10-8 M) [7,26]
GALP(1-32) (human) Hs Agonist 7.2 pIC50 26
⤷ pIC50 7.2 (IC50 6.9x10-8 M) [26]
galanin(5-29) (pig) Rn Agonist 6.7 pIC50 63
⤷ pIC50 6.7 (IC50 2x10-7 M) [63]
galanin(3-29) (pig) Hs Agonist <6.0 pIC50 17-18
⤷ pIC50 <6.0 (IC50 >1x10-6 M) [17-18]
galanin(3-29) (rat/mouse) Rn Agonist <6.0 pIC50 22
⤷ pIC50 <6.0 (IC50 >1x10-6 M) [22]
galanin(10-29) (pig) Rn Agonist 6.0 pIC50 18
⤷ pIC50 6.0 (IC50 1x10-6 M) [18]
alarin {Sp: Rat} Rn Agonist <6.0 pIC50 7
⤷ pIC50 <6.0 (IC50 >1x10-6 M) [7]
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 Value Parameter Reference
M15 Am Antagonist 9.0 pKi 6
⤷ pKi 9.0 (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 8.9 pKi 40
⤷ pKi 8.9 (Ki 1.4x10-9 M) [40]
M32 Hs Antagonist 8.7 – 8.8 pKi 6,46
⤷ pKi 8.7 – 8.8 (Ki 2.18x10-9 – 1.45x10-9 M) [6,46]
M35 Hs Antagonist 8.7 – 8.7 pKi 5-6
⤷ pKi 8.7 – 8.7 (Ki 1.95x10-9 – 1.8x10-9 M) [5-6]
M35 Rn Antagonist 8.1 – 9.2 pKi 31,40,51-52,59
⤷ pKi 8.1 – 9.2 (Ki 8.2x10-9 – 6x10-10 M) [31,40,51-52,59]
M40 Hs Antagonist 8.4 – 8.8 pKi 5-6
⤷ pKi 8.4 – 8.8 (Ki 4.07x10-9 – 1.5x10-9 M) [5-6]
M32 Rn Antagonist 7.9 – 9.2 pKi 51-52
⤷ pKi 9.1 – 9.2 (Ki 7.9x10-10 – 6x10-10 M) [51-52]
pKi 7.9 (Ki 1.3x10-8 M) [51]
M40