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

Gene and Protein Information
Previous and Unofficial Names
Database Links
Natural/Endogenous Ligands
Rank order lists
Agonists
Antagonists
Allosteric Modulators
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
Physiological Consequences of Altering Gene Expression
Phenotypes, Alleles and Disease Models
Gene Expression and Pathophysiology
Biologically Significant Variants
References
Contributors
How to cite this page

Gene and Protein Information
class A G protein-coupled receptor
Species	TM	AA	Chromosomal Location	Gene Symbol	Gene Name	Reference
Human	7	387	17q25.1	GALR2	galanin receptor 2
Mouse	7	371	11 81.1 cM	Galr2	galanin receptor 2
Rat	7	372	10q32.1	Galr2	galanin receptor 2

Previous and Unofficial Names
GALNR2

Previous and Unofficial Names

GALNR2

Database Links
Specialist databases
GPCRdb	galr2_human (Hs), galr2_mouse (Mm), galr2_rat (Rn)
Other databases
Alphafold	O43603 (Hs), O88854 (Mm), O08726 (Rn)
ChEMBL Target	CHEMBL3176 (Hs), CHEMBL5577 (Rn)
Ensembl Gene	ENSG00000182687 (Hs), ENSMUSG00000020793 (Mm), ENSRNOG00000061733 (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)
Pharos	O43603 (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}
spexin-1 {Sp: Human}

Potency order of endogenous ligands (Human)
galanin-like peptide (GALP, Q9UBC7) ≥ galanin (GAL, P22466) [41]

Potency order of endogenous ligands (Human)

galanin-like peptide (GALP, Q9UBC7) ≥ galanin (GAL, P22466) [41]

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Agonists

Key to terms and symbols

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Ligand		Sp.	Action	Value	Parameter	Reference
[¹²⁵I][Tyr²⁶]galanin (pig)		Hs	Agonist	9.5 – 9.9	pK_d	6,17
⤷	pK_d 9.9 (K_d 1.2x10^-10 M) [17] pK_d 9.5 (K_d 3.1x10^-10 M) [6]
[¹²⁵I][Tyr²⁶]galanin (human)		Hs	Agonist	9.5 – 9.6	pK_d	5,26
⤷	pK_d 9.5 – 9.6 (K_d 3.1x10^-10 – 2.4x10^-10 M) [5,26]
[¹²⁵I][Tyr²⁶]galanin (human)		Mm	Agonist	9.3	pK_d	42
⤷	pK_d 9.3 (K_d 4.7x10^-10 M) [42]
[¹²⁵I][Tyr²⁶]galanin (human)		Rn	Agonist	9.2	pK_d	61
⤷	pK_d 9.2 (K_d 5.9x10^-10 M) [61]
[¹²⁵I][Tyr²⁶]galanin (pig)		Rn	Agonist	8.4 – 9.9	pK_d	12,18,54,61
⤷	pK_d 8.4 – 9.9 (K_d 4x10^-9 – 1.3x10^-10 M) [12,18,54,61]
galmic		Rn	Agonist	<5.0	pK_d	3,33
⤷	pK_d <5.0 (K_d >1x10^-5 M) [3,33]
galanin(1-15)		Rn	Agonist	9.1	pK_i	53
⤷	pK_i 9.1 (K_i 7x10^-10 M) [53]
galanin {Sp: Pig}		Rn	Full agonist	9.0 – 9.3	pK_i	53-54
⤷	pK_i 9.0 – 9.3 (K_i 1.05x10^-9 – 5x10^-10 M) [53-54]
galanin(1-20) (human)		Hs	Agonist	9.1	pK_i	5
⤷	pK_i 9.1 (K_i 7.8x10^-10 M) [5]
galanin(2-29) (rat/mouse)		Hs	Full agonist	9.0	pK_i	5
⤷	pK_i 9.0 (K_i 9.1x10^-10 M) [5]
galanin {Sp: Pig}		Hs	Full agonist	9.0	pK_i	6
⤷	pK_i 9.0 (K_i 9.5x10^-10 M) [6]
galanin {Sp: Human}		Hs	Full agonist	8.6 – 9.1	pK_i	5-6,48
⤷	pK_i 8.6 – 9.1 (K_i 2.34x10^-9 – 8.6x10^-10 M) [5-6,48]
galanin {Sp: Mouse, Rat}		Rn	Full agonist	8.3 – 9.3	pK_i	33,42,54,60-62
⤷	pK_i 8.3 – 9.3 (K_i 5.6x10^-9 – 5.6x10^-10 M) [33,42,54,60-62]
galanin {Sp: Mouse, Rat}		Hs	Full agonist	8.5 – 8.8	pK_i	5-6,36,44,47,55
⤷	pK_i 8.5 – 8.8 (K_i 2.98x10^-9 – 1.54x10^-9 M) [5-6,36,44,47,55]
galanin {Sp: Human}		Rn	Full agonist	8.6	pK_i	54
⤷	pK_i 8.6 (K_i 2.51x10^-9 M) [54]
galanin(7-29) (pig)		Rn	Agonist	8.6	pK_i	5
⤷	pK_i 8.6 (K_i 2.51x10^-9 M) [5]
galanin(2-29) (pig)		Hs	Full agonist	8.5	pK_i	6
⤷	pK_i 8.5 (K_i 2.88x10^-9 M) [6]
galanin(1-15)		Hs	Agonist	8.5	pK_i	5
⤷	pK_i 8.5 (K_i 3.5x10^-9 M) [5]
galanin {Sp: Mouse, Rat}		Mm	Full agonist	8.4	pK_i	42
⤷	pK_i 8.4 (K_i 3.9x10^-9 M) [42]
galanin(2-30) (human)		Hs	Full agonist	8.0 – 8.7	pK_i	5,11
⤷	pK_i 8.0 – 8.7 (K_i 1x10^-8 – 1.8x10^-9 M) [5,11]
galanin(1-16) (rat/mouse/pig)		Hs	Agonist	7.9 – 8.8	pK_i	5-6,8
⤷	pK_i 7.9 – 8.8 (K_i 1.3x10^-8 – 1.6x10^-9 M) [5-6,8]
galanin(1-19) (rat/mouse)		Rn	Agonist	8.3	pK_i	62
⤷	pK_i 8.3 (K_i 4.7x10^-9 M) [62]
galanin(1-16) (rat/mouse/pig)		Rn	Agonist	7.9 – 8.7	pK_i	42,53-54,60-62
⤷	pK_i 7.9 – 8.7 (K_i 1.3x10^-8 – 1.8x10^-9 M) [42,53-54,60-62]
J20 (galanin analogue)		Hs	Agonist	8.3	pK_i	45
⤷	pK_i 8.3 (K_i 4.9x10^-9 M) [45]
galanin(7-29) (pig)		Hs	Full agonist	8.3	pK_i	6
⤷	pK_i 8.3 (K_i 4.9x10^-9 M) [6]
M1153		Hs	Agonist	8.3	pK_i	47
⤷	pK_i 8.3 (K_i 4.98x10^-9 M) [47]
M617		Hs	Agonist	8.2	pK_i	36
⤷	pK_i 8.2 (K_i 5.71x10^-9 M) [36]
M242		Hs	Agonist	8.2	pK_i	48
⤷	pK_i 8.2 (K_i 5.84x10^-9 M) [48]
galanin(1-12)		Hs	Agonist	8.2	pK_i	5
⤷	pK_i 8.2 (K_i 6.4x10^-9 M) [5]
M1145		Hs	Full agonist	8.2	pK_i	44
⤷	pK_i 8.2 (K_i 6.55x10^-9 M) [44]
galanin(2-29) (rat/mouse)		Mm	Full agonist	8.2	pK_i	42
⤷	pK_i 8.2 (K_i 6.8x10^-9 M) [42]
[D-Trp²]galanin-(1-29)		Rn	Full agonist	8.1	pK_i	53
⤷	pK_i 8.1 (K_i 7x10^-9 M) [53]
galanin(2-29) (rat/mouse)		Rn	Full agonist	7.3 – 8.7	pK_i	42,60-62
⤷	pK_i 7.3 – 8.7 (K_i 5.6x10^-8 – 1.9x10^-9 M) [42,60-62]
galanin(1-16) (rat/mouse/pig)		Mm	Agonist	7.9	pK_i	42
⤷	pK_i 7.9 (K_i 1.18x10^-8 M) [42]
Gal-B2-dPEG₂₄		Hs	Agonist	7.9	pK_i	69
⤷	pK_i 7.9 (K_i 1.35x10^-8 M) [69]
galanin(D-Trp²) (pig)		Rn	Agonist	7.6 – 8.1	pK_i	53-54
⤷	pK_i 7.6 – 8.1 (K_i 2.754x10^-8 – 7x10^-9 M) [53-54]
Gal-B2-C₁₀		Hs	Agonist	7.8	pK_i	70
⤷	pK_i 7.8 (K_i 1.44x10^-8 M) [70]
Gal-B2-C₈		Hs	Agonist	7.8	pK_i	70
⤷	pK_i 7.8 (K_i 1.49x10^-8 M) [70]
Gal-B2-C₁₈		Hs	Agonist	7.8	pK_i	70
⤷	pK_i 7.8 (K_i 1.5x10^-8 M) [70]
Gal-B2-C₁₂		Hs	Agonist	7.8	pK_i	70
⤷	pK_i 7.8 (K_i 1.61x10^-8 M) [70]
galanin(2-11)		Hs	Agonist	7.8	pK_i	44
⤷	pK_i 7.8 (K_i 1.66x10^-8 M) [44]
Gal-B2-C₁₄		Hs	Agonist	7.7	pK_i	70
⤷	pK_i 7.7 (K_i 1.82x10^-8 M) [70]
J18 (galanin analogue)		Hs	Agonist	7.7	pK_i	45
⤷	pK_i 7.7 (K_i 2x10^-8 M) [45]
[N-Me,des-Sar]Gal-B2		Hs	Agonist	7.7	pK_i	43
⤷	pK_i 7.7 (K_i 2.02x10^-8 M) [43]
Gal-B2-MPEG₄		Hs	Agonist	7.7	pK_i	70
⤷	pK_i 7.7 (K_i 2.05x10^-8 M) [70]
Gal-(K)4		Hs	Agonist	7.6	pK_i	70
⤷	pK_i 7.6 (K_i 2.4x10^-8 M) [70]
M1151		Hs	Agonist	7.5	pK_i	47
⤷	pK_i 7.5 (K_i 2.89x10^-8 M) [47]
M1160		Hs	Agonist	7.5	pK_i	46
⤷	pK_i 7.5 (K_i 3.33x10^-8 M) [46]
M1152		Hs	Agonist	7.4	pK_i	47
⤷	pK_i 7.4 (K_i 3.64x10^-8 M) [47]
Gal-B5		Hs	Agonist	7.3	pK_i	8
⤷	pK_i 7.3 (K_i 4.8x10^-8 M) [8]
Gal-B2		Hs	Agonist	7.3	pK_i	8
⤷	pK_i 7.3 (K_i 5.15x10^-8 M) [8]
Gal-R2-dPEG₂₄		Hs	Agonist	7.2	pK_i	69
⤷	pK_i 7.2 (K_i 6.04x10^-8 M) [69]
galanin(2-11)		Rn	Agonist	7.1	pK_i	32
⤷	pK_i 7.1 (K_i 8.8x10^-8 M) [32]
galanin(D-Trp²) (pig)		Hs	Agonist	6.7	pK_i	6
⤷	pK_i 6.7 (K_i 1.995x10^-7 M) [6]
galanin(3-29) (rat/mouse)		Hs	Agonist	<6.2	pK_i	5
⤷	pK_i <6.2 (K_i >7x10^-7 M) [5]
galanin(10-29) (rat/mouse)		Hs	Agonist	<6.2	pK_i	5
⤷	pK_i <6.2 (K_i >7x10^-7 M) [5]
galanin(5-29) (rat/mouse)		Hs	Agonist	<6.2	pK_i	5
⤷	pK_i <6.2 (K_i >7x10^-7 M) [5]
galanin(9-29) (rat/mouse)		Hs	Agonist	<6.2	pK_i	5
⤷	pK_i <6.2 (K_i >7x10^-7 M) [5]
galanin(9-25) (rat/mouse)		Hs	Agonist	<6.2	pK_i	5
⤷	pK_i <6.2 (K_i >7x10^-7 M) [5]
galanin(3-30) (human)		Hs	Agonist	<6.2	pK_i	5
⤷	pK_i <6.2 (K_i >7x10^-7 M) [5]
galanin(1-10)		Hs	Agonist	<6.2	pK_i	5
⤷	pK_i <6.2 (K_i >7x10^-7 M) [5]
GMAP(1-41) {Sp: Pig}		Rn	Agonist	<6.1	pK_i	61
⤷	pK_i <6.1 (K_i >8.4x10^-7 M) [61]
galanin(3-29) (pig)		Hs	Agonist	<6.0	pK_i	6
⤷	pK_i <6.0 (K_i >1x10^-6 M) [6]
galanin(3-29) (pig)		Rn	Agonist	<6.0	pK_i	53-54
⤷	pK_i <6.0 (K_i >1x10^-6 M) [53-54]
GMAP(44-59) {Sp: Pig}		Rn	Agonist	<6.0	pK_i	62
⤷	pK_i <6.0 (K_i >1x10^-6 M) [62]
(D-Thr⁶, D-Trp^8,9)galanin(1-15)ol		Rn	Agonist	<5.9	pK_i	61
⤷	pK_i <5.9 (K_i >1.25x10^-6 M) [61]
galanin(3-29) (rat/mouse)		Rn	Agonist	5.5 – 6.0	pK_i	42,60,62
⤷	pK_i 5.5 – 6.0 (K_i 3.125x10^-6 – 1x10^-6 M) [42,60,62]
galanin(10-29) (rat/mouse)		Mm	Agonist	<5.7	pK_i	42
⤷	pK_i <5.7 (K_i >1.86x10^-6 M) [42]
galanin(3-29) (rat/mouse)		Mm	Agonist	<5.7	pK_i	42
⤷	pK_i <5.7 (K_i >2.2x10^-6 M) [42]
galnon		Rn	Agonist	4.5	pK_i	3,33
⤷	pK_i 4.5 (K_i 3.41x10^-5 M) [3,33]
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	41
⤷	pEC₅₀ 8.6 (EC₅₀ 2.4x10^-9 M) [41]
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	41
⤷	pEC₅₀ 8.3 (EC₅₀ 5.2x10^-9 M) [41]
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	53
⤷	pEC₅₀ 7.7 (EC₅₀ 1.8x10^-8 M) [53]
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	53
⤷	pEC₅₀ 7.2 (EC₅₀ 6.5x10^-8 M) [53]
Qu-SPX		Hs	Agonist	7.1	pEC₅₀	30
⤷	pEC₅₀ 7.1 (EC₅₀ 8.71x10^-8 M) [30] Description: SRE-luc reporter activation in HEK293 Gqi cells expressing hGAL₃ receptor.
galanin(1-16) (rat/mouse/pig)		Rn	Agonist	7.0	pEC₅₀	53
⤷	pEC₅₀ 7.0 (EC₅₀ 9.4x10^-8 M) [53]
galanin(D-Trp²) (pig)		Rn	Agonist	6.8	pEC₅₀	53
⤷	pEC₅₀ 6.8 (EC₅₀ 1.5x10^-7 M) [53]
spexin-1 {Sp: Human}		Hs	Agonist	6.8	pEC₅₀	25
⤷	pEC₅₀ 6.8 (EC₅₀ 1.61x10^-7 M) [25] Description: Determined by measuring SRE-luc activity in HEK293-Gqi cells expressing hGALR2.
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	53
⤷	pEC₅₀ <6.0 (EC₅₀ >1x10^-6 M) [53]
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	41
⤷	pIC₅₀ 9.6 (IC₅₀ 2.4x10^-10 M) [41]
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	7,18,41
⤷	pIC₅₀ 8.7 – 9.3 (IC₅₀ 1.9x10^-9 – 4.8x10^-10 M) [7,18,41]
galanin {Sp: Human}		Rn	Full agonist	8.6 – 9.0	pIC₅₀	18,22,31
⤷	pIC₅₀ 8.6 – 9.0 (IC₅₀ 2.5x10^-9 – 1x10^-9 M) [18,22,31]
galanin(1-11)		Rn	Agonist	8.8	pIC₅₀	31
⤷	pIC₅₀ 8.8 (IC₅₀ 1.65x10^-9 M) [31]
[Sar¹, D-Ala¹²]galanin(1-16)		Rn	Agonist	8.8	pIC₅₀	31
⤷	pIC₅₀ 8.8 (IC₅₀ 1.74x10^-9 M) [31]
galanin(2-11)		Rn	Agonist	8.8	pIC₅₀	31
⤷	pIC₅₀ 8.8 (IC₅₀ 1.76x10^-9 M) [31]
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	27
⤷	pIC₅₀ 7.8 (IC₅₀ 1.5x10^-8 M) [27]
galanin-like peptide {Sp: Human}		Hs	Agonist	7.6 – 7.7	pIC₅₀	7,27
⤷	pIC₅₀ 7.6 – 7.7 (IC₅₀ 2.8x10^-8 – 1.87x10^-8 M) [7,27]
GALP(1-32) (human)		Hs	Agonist	7.2	pIC₅₀	27
⤷	pIC₅₀ 7.2 (IC₅₀ 6.9x10^-8 M) [27]
galanin(5-29) (pig)		Rn	Agonist	6.7	pIC₅₀	65
⤷	pIC₅₀ 6.7 (IC₅₀ 2x10^-7 M) [65]
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]
[¹²⁵I]spexin-1		Hs	Agonist	-	-	25
⤷	[25]

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 [60], 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 [43] many different galanin analogues were trialled. The most active compounds are reported here. The K_i values of other analogues are listed in these publications. In [49] 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

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Ligand		Sp.	Action	Value	Parameter	Reference
M15		Am	Antagonist	9.0	pK_i	6
⤷	pK_i 9.0 (K_i 1.07x10^-9 M) [6]
C7		Hs	Antagonist	8.7 – 9.2	pK_i	5-6
⤷	pK_i 8.7 – 9.2 (K_i 2x10^-9 – 6.3x10^-10 M) [5-6]
M15		Mm	Antagonist	8.9	pK_i	42
⤷	pK_i 8.9 (K_i 1.4x10^-9 M) [42]
M32		Hs	Antagonist	8.7 – 8.8	pK_i	6,48
⤷	pK_i 8.7 – 8.8 (K_i 2.18x10^-9 – 1.45x10^-9 M) [6,48]
M35		Hs	Antagonist	8.7 – 8.7	pK_i	5-6
⤷	pK_i 8.7 – 8.7 (K_i 1.95x10^-9 – 1.8x10^-9 M) [5-6]
M35		Rn	Antagonist	8.1 – 9.2	pK_i	33,42,53-54,61
⤷	pK_i 8.1 – 9.2 (K_i 8.2x10^-9 – 6x10^-10 M) [33,42,53-54,61]
M40		Hs	Antagonist	8.4 – 8.8	pK_i	5-6
⤷	pK_i 8.4 – 8.8 (K_i 4.07x10^-9 – 1.5x10^-9 M) [5-6]
M32		Rn	Antagonist	7.9 – 9.2	pK_i	53-54
⤷	pK_i 9.1 – 9.2 (K_i 7.9x10^-10 – 6x10^-10 M) [53-54] pK_i 7.9 (K_i 1.3x10^-8 M) [53]
M40		Mm	Antagonist	8.6	pK_i	42
⤷	pK_i 8.6 (K_i 2.8x10^-9 M) [42]
C7		Rn	Antagonist	7.7 – 9.3	pK_i	42,53-54,61
⤷	pK_i 7.7 – 9.3 (K_i 1.9x10^-8 – 5.6x10^-10 M) [42,53-54,61]
M40		Rn	Antagonist	7.7 – 9.1	pK_i	33,42,53-54,61-62
⤷	pK_i 7.7 – 9.1 (K_i 1.8x10^-8 – 7x10^-10 M) [33,42,53-54,61-62]
M15		Rn	Antagonist	7.8 – 9.0	pK_i	33,42,53-54,61-62
⤷	pK_i 7.8 – 9.0 (K_i 1.57x10^-8 – 1x10^-9 M) [33,42,53-54,61-62]
M35		Mm	Antagonist	8.3	pK_i	42
⤷	pK_i 8.3 (K_i 4.9x10^-9 M) [42]
M871		Hs	Antagonist	7.9	pK_i	55
⤷	pK_i 7.9 (K_i 1.31x10^-8 M) [55]
C7		Mm	Antagonist	7.8	pK_i	42
⤷	pK_i 7.8 (K_i 1.4x10^-8 M) [42]
SNAP 398299		Hs	Antagonist	<6.0	pK_i	58
⤷	pK_i <6.0 (K_i >1x10^-6 M) [58]
SNAP 37889		Hs	Antagonist	<5.0	pK_i	58
⤷	pK_i <5.0 (K_i >1x10^-5 M) [58]
GalR3ant		Rn	Antagonist	<5.0	pK_i	33
⤷	pK_i <5.0 (K_i >1x10^-5 M) [33]
M15		Hs	Antagonist	8.0 – 9.2	pEC₅₀	5-6,17
⤷	pEC₅₀ 8.0 – 9.2 (EC₅₀ 9.12x10^-9 – 6.5x10^-10 M) [5-6,17]
C7		Rn	Antagonist	8.5	pEC₅₀	53
⤷	pEC₅₀ 8.5 (EC₅₀ 3x10^-9 M) [53]
M35		Hs	Antagonist	7.9 – 9.1	pEC₅₀	6,17
⤷	pEC₅₀ 7.9 – 9.1 (EC₅₀ 1.38x10^-8 – 7.2x10^-10 M) [6,17]
M32		Hs	Antagonist	7.8 – 8.4	pEC₅₀	6,17
⤷	pEC₅₀ 7.8 – 8.4 (EC₅₀ 1.413x10^-8 – 4.23x10^-9 M) [6,17]
C7		Hs	Antagonist	8.0	pEC₅₀	6
⤷	pEC₅₀ 8.0 (EC₅₀ 9.33x10^-9 M) [6]
M40		Hs	Antagonist	7.8	pEC₅₀	6
⤷	pEC₅₀ 7.8 (EC₅₀ 1.621x10^-8 M) [6]
M40		Rn	Antagonist	7.6	pEC₅₀	53
⤷	pEC₅₀ 7.6 (EC₅₀ 2.8x10^-8 M) [53]
M35		Rn	Antagonist	7.5	pEC₅₀	53
⤷	pEC₅₀ 7.5 (EC₅₀ 2.9x10^-8 M) [53]
M15		Rn	Antagonist	6.5	pEC₅₀	53
⤷	pEC₅₀ 6.5 (EC₅₀ 3x10^-7 M) [53]
M35		Rn	Antagonist	8.6 – 9.4	pIC₅₀	18,22
⤷	pIC₅₀ 8.6 – 9.4 (IC₅₀ 2.8x10^-9 – 4.3x10^-10 M) [18,22]
M40		Rn	Antagonist	8.6 – 8.7	pIC₅₀	18,22
⤷	pIC₅₀ 8.6 – 8.7 (IC₅₀ 2.7x10^-9 – 1.9x10^-9 M) [18,22]
M15		Hs	Antagonist	8.4	pIC₅₀	17
⤷	pIC₅₀ 8.4 (IC₅₀ 4.02x10^-9 M) [17]
C7		Hs	Antagonist	8.1	pIC₅₀	17
⤷	pIC₅₀ 8.1 (IC₅₀ 8.39x10^-9 M) [17]
C7		Rn	Antagonist	7.6 – 8.4	pIC₅₀	18,22
⤷	pIC₅₀ 7.6 – 8.4 (IC₅₀ 2.3x10^-8 – 3.6x10^-9 M) [18,22]
M15		Rn	Antagonist	7.6 – 8.3	pIC₅₀	18,22
⤷	pIC₅₀ 7.6 – 8.3 (IC₅₀ 2.8x10^-8 – 4.8x10^-9 M) [18,22]
dithiipin-1,1,4,4-tetroxide analogue 7		Hs	Antagonist	<4.5	pIC₅₀	51
⤷	pIC₅₀ <4.5 (IC₅₀ >3x10^-5 M) [51]

View species-specific antagonist tables

Antagonist Comments

GalR3ant displays receptor selectivity for GAL₃ receptor, with low affinity for GAL₁ and GAL₂ receptors [33].
In [51], a series of compounds was tested, and the IC₅₀ value for human GAL₂ receptor is reported above. Analogue 7 is reported as the first non-peptide sub-micromolar antagonist to human GAL₁ receptor.

Allosteric Modulators

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Ligand											Sp.	Action	Value	Parameter	Reference
CYM2503											Rn	Positive	9.2	pEC₅₀	34
⤷	pEC₅₀ 9.2 (EC₅₀ 6.9x10^-10 M) [34] Description: Potentiation of galanin-induced IP1 accumulation in vitro.

Allosteric Modulator Comments

CYM2503, a putative GalR2-positive allosteric modulator, does not by itself stimulate IP1 production in HEK293 stably expressing the rat GAL₂ receptor in the absence of galanin. CYM2503 does however potentiate the effect of 100nM galanin (i.e. galanin alone EC₅₀ = 300nM; galanin+CYM2503 EC₅₀ = 690nM) and shifts the galanin concentration-response curve to the left (EC₅₀ shifted by 50.4 fold with 100μM CYM2503; 12.5 fold with 10μM CYM2503 and 0.7 fold with 1μM CYM2503) [34]. The results with CYM2503 suggest that the GAL₂ receptor is a plausible target for the development of novel anticonvulsant drug therapy.

Primary Transduction Mechanisms
Transducer	Effector/Response
G_q/G₁₁ family	Phospholipase C stimulation
Comments: The most commonly reported pathway involves phospholipase C activation, which increases insoitol phosphate hydrolysis, mediating the release of Ca²⁺ into the cytoplasm from intracellular stores and opening Ca²⁺-dependent chloride channels [6,12,17-18,42,53,63]. These GAL₂ receptor-mediated intracellular effects are not affected by pertussis toxin, suggesting that GAL₂ receptor acts via G_q/G₁₁-type G-proteins (reviewed in [28]).
References: 6,12,17-18,42,53,63

Secondary Transduction Mechanisms
Transducer	Effector/Response
G_i/G_o family G₁₂/G₁₃ family	Adenylyl cyclase inhibition Other - See Comments
Comments: The ability of GAL₂ receptor to signal via other G proteins is somewhat controversial (reviewed in [28]). Several studies demonstrate no alterations in forskolin-stimulated cAMP accumulation following galanin exposure [16,42,53]; whereas several other studies demonstrate at least some inhibition of forskolin-stimulated cAMP accumulation, although less than reported for GAL₁ receptor, which is inhibited by pertussis toxin [12,17,61,63]. In addition, GAL₂ receptor activation inhibits cyclic-AMP-responsive element-binding protein [1]. There is also evidence that GAL₂ receptor is coupled to a G_o-type G-protein, which activates mitogen-activated protein kinase (MAPK) in a pertussis toxin-sensitive, PKC (protein kinase C)-dependent fashion [12,20-21]; although it may also proceed via PKC-independent pathways [63]. Another proposed signalling pathway for GAL₂ receptor is via functional coupling to a G₁₂/G₁₃ G-protein and activation of RhoA in small cell lung cancer cells [63]. In non-tumour cells, galanin enhances neuronal survival, mediated via the Akt-signalling pathway, leading to suppression of caspase-3 and capase-9 activity, likely via GAL₂ receptor stimulation [13,68]; whereas in the tumour cell line (PC12), galanin mediates apoptotic cell death via GAL₂ receptor, by inhibition of the PI3K/Akt pathway [59]. GAL₂ receptor has been demonstrated to be internalised following incubation with galanin in a GAL₂-EGFP (enhanced green fluorescent protein)-transfected PC12 cell line (derived from phaeochromocytoma of rat adrenal medulla) [66-67] (reviewed in [28]).
References: 12,17,61

Tissue Distribution

Small intestine and colon. Not detected in whole brain, amygdala, caudate nucleus, corpus callosum, hippocampus, substantia nigra, subthalamic nucleus, thalamus, cerebellum, cerebral cortex, medulla, spinal cord, occipital lobe, frontal lobe, temporal lobe, putamen, heart, placenta, lung, liver, skeletal muscle, kidney, pancreas, spleen, thymus, prostate, testes, ovary, peripheral blood leukocytes.

Species:	Human
Technique:	Northern blot.
References:	5

High levels in GH3 pituitary cell line, anterior pituitary, whole brain, hypothalamus, gut tissues; lower levels in spleen, lung, skeletal muscle, heart, kidney, liver, testis.

Species:	Rat
Technique:	Ribonuclease protection analysis.
References:	18

About 25% normal dorsal root ganglia in lumbar spine were GAL₂ receptor mRNA positive. Strong increase in GAL₂ receptor mRNA neuron profiles after peripheral tissue inflammation and long-lasting decrease after axotomy.

Species:	Rat
Technique:	In situ hybridisation.
References:	56

Granule cell layer of dentate gyrus.

Species:	Rat
Technique:	In situ hybridisation.
References:	42

Following facial nerve injury, GAL₂ receptor mRNA expression is increased in the ipsilateral facial nucleus (at 3 & 7 days post facial nerve injury).

Species:	Rat
Technique:	In situ hybridisation.
References:	9

Highest levels – hippocampus (including dentate gyus) and hypothalamic nuclei (supraoptic, retrochiasmic, arcuate, lateral mammillary nuclei) > paraventricular nuclei>>anterior hypothalamic area, lateral hypothalamic area, preoptic area). Lower levels – amygdala and piriform cortex. Detected in brain stem, anterodorsal thalamic nucleus, Purkinje cells of cerebellum, anterior pituitary (not posterior pituitary).

Species:	Rat
Technique:	In situ hybridisation.
References:	18

Brain, lung, heart, spleen, kidney > skeletal muscle, liver, testis.

Species:	Rat
Technique:	Northern blot.
References:	53

Kidney, testis, skeletal muscle, liver > brain, heart, spleen, lung.

Species:	Rat
Technique:	Northern blot.
References:	61

Uterus, RIN m5F cells (rat insulinoma cell line) > large intestine, stomach > lung, prostate, vas deferens, ovary. Minimal to none in heart, kidney, liver, skeletal muscle, testes, pancreas.

Species:	Rat
Technique:	Northern blot.
References:	22

Expression Datasets

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays

Measurement of intracellular Ca²⁺ in rat GAL₂ receptor-transfected CHO cells.

Species:	Rat
Tissue:	CHO cells transfected with rat GAL₂ receptor.
Response measured:	Increase in intracellular free Ca²⁺.
References:	53

Rat galanin causes concentration dependent inhibition of forskolin-stimulated cAMP production.

Species:	Rat
Tissue:	COS-1 cells.
Response measured:	Measurement of forskolin-stimulated cAMP production in rat GAL₂ receptor transfected COS-1 cells.
References:	61

Measurement of inositol phosphate accumulation in rat GAL2-transfected CHO cells following application of porcine galanin.

Species:	Rat
Tissue:	CHO cells transfected with rat GAL₂ receptor.
Response measured:	Inositol phosphate accumulation.
References:	12,53

Measurement of inward currents in Xenopus oocytes injected with rat GAL₂ receptor mRNA following application of porcine galanin (100-1000nM).

Species:	Rat
Tissue:	Xenopus oocytes.
Response measured:	Activation of rapid inward currents (most likely mediated by endogenous calcium-activated Cl^- currents from the resulting increase in intracellular free Ca²⁺)
References:	53

Measurement of inositol phosphate levels in rat GAL₂ receptor-transfected HEK 293 cells.

Species:	Rat
Tissue:	HEK293 cell line transfected with rat GAL₂ receptor.
Response measured:	Stimulation of inositol phosphate accumulation, which isinsensitive to pertussis toxin.
References:	18

Inhibition of forskolin-stimulated cAMP production by 30% (compared to 70% in GAL₁ receptor-transfected CHO cells)

Species:	Rat
Tissue:	CHO cells.
Response measured:	Measurement of forskolin-stimulated cAMP production in rat GAL₂ receptor-transfected CHO cells.
References:	12

Galanin stimulates MAPK activity, which is inhibited by pretreatment with pertussis toxin and also with the protein kinase C (PKC) inhibitor, bis[indolylmaleimide I] and PKC depletion. Galanin-stimulated MAPK activity is not affected by β-ARKct expression, suggesting that the pathway was not mediated via the βγ subunit of G_i.

Species:	Rat
Tissue:	CHO cells.
Response measured:	Measurement of MAPK (mitogen-activated protein kinase) activity in GAL₂ receptor-transfected CHO cells.
References:	12

Human galanin causes a concentration-dependent decrease in forskolin-stimulated intracellular cAMP levels in human GAL₂ receptor-transfected HEK293 cells.

Species:	Human
Tissue:	HEK293 cells.
Response measured:	Measurement of forskolin-stimulated intracellular cAMP levels.
References:	17,63

Human galanin caused a concentration-dependent increase in transient intracellular Ca²⁺ levels in human GAL₂ receptor-transfected HEK293 cells.

Species:	Human
Tissue:	HEK293 cells.
Response measured:	Measurement of intracellular Ca2+ levels
References:	17

Galanin stimulates inositol phosphate accumulation in rat GAL₂ receptor-transfected COS-7 cells. This response is not affected by pertussis toxin.

Species:	Rat
Tissue:	COS-7 cells.
Response measured:	Measurement of inositol phosphate levels.
References:	42

Galanin stimulates inositol phosphate accumulation in mouse GAL₂ receptor transfected COS-7. This response is not affected by pertussis toxin.

Species:	Mouse
Tissue:	COS-7 cells.
Response measured:	Measurement of inositol phosphate levels.
References:	42

Human galanin (10-1000nM) activates rapid inward currents in Xenopus oocytes injected with human GAL₂ receptor mRNA

Species:	Human
Tissue:	Xenopus oocytes.
Response measured:	Measurement of inward currents in Xenopus oocytes.
References:	6

Galanin led to the formation of actin stress fibres in Swiss 3T3 fibroblast cells expressing the human GAL₂ receptor, which is likely mediated via G₁₂/G₁₃ protein family.

Species:	Human
Tissue:	Swiss 3T3 fibroblast cell line.
Response measured:	Measurement of Rho-dependent stress fibre formation.
References:	63

Human galanin caused a concentration-dependent increase in intracellular inositol phosphate levels in human GAL₂ receptor-transfected HEK293 cells.

Species:	Human
Tissue:	HEK293 cells.
Response measured:	Measurement of inositol phosphate levels.
References:	17

Glutamate increases phosphorylation of Akt in wild-type hippocampal cultures, which is significantly attenuated in GAL₂ receptor knockout cultures, suggesting that it is mediated via GAL₂ receptor.

Species:	Mouse
Tissue:	Hippocampal tissue.
Response measured:	Measurement of Akt phosphorylation.
References:	15

Galanin down-regulates phosphorylation of Akt and Bad in GAL₂ receptor-transfected PC12 cells, suggesting that GAL₂ receptor-mediated signalling leads to inhibition of the PI3K/Akt pathway, which in turn leads to caspase-dependent apoptotic cell death.

Species:	Rat
Tissue:	PC12 cell line (derived from phaeochromocytoma of rat adrenal medulla).
Response measured:	Measurement of phosphorylation of Akt and Bad.
References:	59

Galanin (100nM) stimulates increased intracellular Ca²⁺ in human GAL₂ receptor-transfected CHO cells. Galanin also increases Ca²⁺ release In GAL₂ receptor-expressing H69 cells, which is not blocked by pretreatment with pertussis toxin, suggesting it is mediated via a G_q/G₁₁ pathway. Galanin stimulates ERK activity in GAL₂ receptor-expressing H69 cells. This ERK stimulation is nearly abolished by pretreatment with staurosporine, indicating participation of serine/threonine kinases e.g. PKC isozymes, although the activation is not altered by pretreatment with the PKC inhibitor, bisindolylmaleimide I (GF10903X), suggesting that galanin-dependent ERK activation can proceed through alternative pathways independent of PKC.

Species:	Human
Tissue:	CHO cells, H69 cells (small cell lung cancer cell line).
Response measured:	Measurement of intracellular Ca²⁺ and measurement of ERK activation.
References:	6,63

Galanin stimulates inositol phosphate accumulation in human GAL₂ receptor-transfected CHO and COS-7 cells. Pertussis toxin does not alter the galanin-induced inositol phosphate accumulation in COS-7 cells.

Species:	Human
Tissue:	CHO cells, COS-7 cells.
Response measured:	Measurement of inositol phosphate levels.
References:	6,63

Galanin(1-29), which is a high affinity agonist for both GAL₁ receptor and GAL₂ receptor, and galanin (2-11), a GAL₂ receptor agonist, significantly reduce CREB phosphorylation induced by high-frequency trans stimulation, suggesting GAL₂ receptor may be involved.

Species:	Mouse
Tissue:	Hippocampal tissue.
Response measured:	Measurement of LTP-induced CREB phosphorylation in the dentate gyrus of mice.
References:	1

Galanin demonstrates neuroprotective effects against A-beta (β-amyloid) on basal forebrain neurons, which is replicated by the GAL₂ receptor agonist, galanin(2-11) (AR-M1896), suggesting that the effect is mediated via GAL₂ receptor. Further studies demonstrate that galanin reverses A-beta-induced inhibition of Akt phosphorylation (a pro-survival pathway), blocks the cleavage of capase-3, and attenuates cleavage of capase-9. It is likely this effect is also mediated via GAL₂ receptor.

Species:	Rat
Tissue:	Rat basal forebrain
Response measured:	Measurement of phosphorylation of Akt (serine/threonine kinase), and cleavage of caspase-3 and capase-9 levels in rat basal forebrain neurons.
References:	13

GAL₂ receptor is internalised in a dose dependent manner after incubation with galanin in GAL₂ receptor-EGFP (enhanced green fluorescent protein)-transfected PC12 cells. In addition, galanin and GALP (which preferentially binds to ₂ receptor) increase ERK phosphorylation in PC12 cells, which is inhibited by the protein kinase C (PKC)- specific inhibitor, GF, and pertussis toxin, suggesting that galanin-induced ERK phosphorylation involves activation of G_o proteins.

Species:	Rat
Tissue:	PC12 cell line (derived from phaeochromocytoma of rat adrenal medulla).
Response measured:	Measurement of receptor internalisation and ERK phosphorylation.
References:	20,66-67

Galanin rapidly activates ERK1 in wild-type but not GAL₂ receptor knockout mice.

Species:	Mouse
Tissue:	Dorsal root ganglion from wildtype and GAL₂ receptor knockout mice.
Response measured:	Measurement of ERK phosphorylation.
References:	21

Physiological Functions

Galanin analogue J18 (which is selective for Galr2) has antidepressant-like effects in mouse models of depression (forced swin and tail suspension tests) at low dose (<0.5mg/kg). This antidepressant-like effect is abbrogated by galanin antagonist M35.

Species:	Mouse
Tissue:	In vivo.
References:	45

Galanin, acting via GAL₂ receptor, induces myometrial contraction.

Species:	Rat
Tissue:	Myometrium.
References:	40

In the Morris water maze, galanin significantly retards spatial acquisition without affecting swim speed or performance in the visible platform test, which appears to be mediated via GAL₂ receptor (in areas where most of the galanin is present in noradrenergic terminals).

Species:	Rat
Tissue:	Hippocampal formation.
References:	50

Low dose galanin has a nociceptive role at the spinal cord level mediated by GAL₂ receptors^†.

Species:	Rat
Tissue:	Spinal cord.
References:	31

Galanin mediates neurite extension in adult sensory neurons (dorsal root ganglion) via GAL₂ receptor in a PKC-dependent manner.

Species:	Mouse
Tissue:	Dorsal root ganglion.
References:	37

GAL₂ receptor appears to control the excitability and Ca²⁺ entry in a large population of nociceptive neurons, which would increase excitability and enhance intracellular Ca²⁺ signalling, which would enhance sensory transmission.

Species:	Rat
Tissue:	Dorsal root ganglion neurons.
References:	24

In the dentate gyrus, galanin acting via GAL₂ receptor inhibits seizures, promotes viability of hilar interneurons and stimulates seizure-induced neurogenesis (from studies with a 50% reduction of GAL₂ receptor binding, achieved by continuous infusion of complemenatry peptide nucleic acid antisense oligonucleotide into dentate gyrus.

Species:	Rat
Tissue:	In vivo.
References:	39

Peripheral galanin appears to have an excitatory role in inflammatory pain (induced by capsaicin) likely mediated by peripheral GAL₂ receptor.

Species:	Rat
Tissue:	In vivo/intraplantar injections of capsaicin.
References:	23

GAL₂ receptor agonist blocked induction of LTP in the dentate gyrus, and caused a transient reduction in the maintenance phase of LTP. GAL₂ receptor may also be involved in reducing the level of LTP-mediated phosphorylation of CREB in the dentate gyrus granule cells.

Species:	Mouse
Tissue:	In vivo/brain.
References:	1

GAL₂ receptor inhibits cell proliferation and mediates apoptosis in SH-SY5Y neuroblastoma cells.

Species:	Human
Tissue:	SH-SY5Y neuroblastoma cells.
References:	4

Physiological Functions Comments

^† Note that in this study [31], the effects were investigated using the GAL₂ receptor agonist, AR-M1896, which has subsequently been demonstrated to bind with high affinity to GAL₃ receptor. This suggests that the effects may also be mediated via GAL₃ receptor.

Physiological Consequences of Altering Gene Expression

Mice with GAL₂ receptor knockout (C57BL/6 background) were tested in a variety of anxiety- and depressive-like tests. Mice with GAL₂ receptor knockout exhibited a more persistent depressive-like phenotype in the learned helplessness paradigm and increased immobility in the tail suspension test; but showed similar levels of anxiety-like behaviour compared to wildtype in the elevated plus maze, open field and light-dark transfer test.

Species:	Mouse
Tissue:	In vivo/brain.
Technique:	Gene knock-outs.
References:	35

GAL₂ receptor knockout mice do not exhibit antidepressant-like effects of GAL₂ receptor analogue J18 observed in receptor intact mice.

Species:	Mouse
Tissue:	In vivo
Technique:	Gene knockouts.
References:	45

GAL₂ receptor knockout mice were tested for basic motor and sensory function, feeding behaviour, reproduction, mood, learning and memory, and seizure susceptibility. GAL₂ receptor knockout mice were indistinguishable from wildtype mice in these tests.

Species:	Mouse
Tissue:	Brain.
Technique:	Gene knock-outs.
References:	19

GAL₂ receptor knockout mice demonstrated a 15% decrease in CGRP expressing neuronal profiles in the adult dorsal root ganglia, associated with marked deficits in neuropathic and inflammatory pain behaviours. They also demonstrated one third reduction in neurite outgrowth from cultured dorsal root ganglion neurons.

Species:	Mouse
Tissue:	Dorsal root ganglion.
Technique:	Gene knock-outs.
References:	21

Mice with GAL₂ receptor knockout (129AS1/SvlmJ line) were tested in tests of general health, cognitive behaviour and anxiety-like behaviour. Mice with GAL₂ receptor knockout demonstrated an anxiogenic-like phenotype on the elevated plus maze, but not in several other measures of anxeity-like behaviour. In addition, there was no siginificant differences from wildtype in terms of gnereal health or cognitive behaviour (Morris water maze, trace cued and contextual fear conditioning).

Species:	Mouse
Tissue:	In vivo.
Technique:	Gene knock-outs.
References:	2

GAL₂ receptor knockout mice were tested for hippocampal neuronal survival following glutamate-induced hippocampal damage. The protective role played by galanin for glutamate-induced hippocampal damage is abolished in GAL₂ receptor knockout mice.

Species:	Mouse
Tissue:	Hippocampal culture.
Technique:	Gene knock-outs.
References:	15

The role of GAL₂ receptor in status epilepticus was investigated by intrahippocampal infusion of anti-GAL₂ receptor peptide-nucleic acid antisense. Focal downregulation of GAL₂ receptor in the hippocampus significantly increased the severity of perforant path stimulation-induced status epilepticus and led to milder injury to hilar interneurons and potentiated seizure-induced hippocampal damage.

Species:	Rat
Tissue:	Hippocampus.
Technique:	Peptide nucleic acid antisense methodology.
References:	38

Mice with GAL₂ receptor knockout were tested for pain thresholds, and development and trophic effects of galanin. After 1 week post sciatic nerve transection, there were 16-20% fewer neurons in intact contralateral dorsal root ganglia of GAL₂ receptor knockout mice. Compared to wildtype mice, GAL₂ receptor knockout mice showed similar onset and duration of hyperalgia in the injured paw, and similar recovery from spinal nerve ligation-cause allodynia.

Species:	Mouse
Tissue:	In vivo/sciatic nerve/dorsal root ganglion.
Technique:	Gene knock-outs.
References:	52

Mice with GAL₂ receptor knockout were tested for disease severity in the experimental autoimmune encephalitis (EAE) model of multiple sclerosis. GAL₂ receptor knockout increases disease severity in this mouse model.

Species:	Mouse
Tissue:	In vivo.
Technique:	Gene knock-outs.
References:	64

Mice with GAL₂ receptor knockout were tested for amyloid induced cell death. Mice with GAL₂ receptor knockout demonstrated significantly greater cell death following amyloid than wildtype controls.

Species:	None
Tissue:	In vivo.
Technique:	Gene knock-outs.
References:	14

GAL₂ receptor-overexpressing mice were assessed in various tests of anxiety- and depressive-like behaviour, including the Porsolt forced swim test, the open field, elevated plus maze, passive avoidance test. GAL₂ receptor-overexpressing mice demonstrated decreased immobility in the forced swim test (indicative of antidepressive-like behaviour and/or increased stress resistance), but no difference in anxiety-like behaviour, motor activity levels, emotional learning or memory behaviours.

Species:	Mouse
Tissue:	In vivo.
Technique:	Gene over-expression.
References:	29

Phenotypes, Alleles and Disease Models

Mouse data from MGI

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Allele	Composition & genetic background	Accession	Phenotype Id	Phenotype	Reference
Galr2^tm1Dgen	Galr2^tm1Dgen/Galr2^tm1Dgen B6.129-Galr2	MGI:1337018	MP:0001022	abnormal L5 dorsal root ganglion morphology	PMID: 16487144
Galr2^{Gt(OST105469)Lex}	Galr2^{Gt(OST105469)Lex}/Galr2^{Gt(OST105469)Lex} involves: 129S5/SvEvBrd * C57BL/6J	MGI:1337018	MP:0005017	decreased B cell number
Galr2^{Gt(OST105469)Lex}	Galr2^{Gt(OST105469)Lex}/Galr2^{Gt(OST105469)Lex} involves: 129S5/SvEvBrd * C57BL/6J	MGI:1337018	MP:0002757	decreased vertical activity
Galr2^{Gt(OST105469)Lex}	Galr2^{Gt(OST105469)Lex}/Galr2^{Gt(OST105469)Lex} involves: 129S5/SvEvBrd * C57BL/6J	MGI:1337018	MP:0005015	increased T cell number
Galr2^tm1Dgen	Galr2^tm1Dgen/Galr2^tm1Dgen B6.129-Galr2	MGI:1337018	MP:0001973	increased thermal nociceptive threshold	PMID: 16487144

Gene Expression and Pathophysiology Comments
GAL₂ receptor is a candidate biomarker for colon cancer, with GAL₂ receptor hypermethylation showing a sensitvity of 85% and specificity of 95% [10].

Biologically Significant Variant Comments

Linkage and mapping studies suggest that the 17q chromosomal region contains a gene (or genes) that contributes to the genetic aetiology of obesity (particularly visceral adiposity). One candidate gene in this region is the GAL₂ receptor, although there is little evidence of an association between polymorphisms of GAL₂ receptor and obesity [57].

References

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