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BB2 receptor

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Target not currently curated in GtoImmuPdb

Target id: 39

Nomenclature: BB2 receptor

Family: Bombesin receptors

Contents:

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 7 384 Xp22.2 GRPR gastrin releasing peptide receptor 10,71
Mouse 7 384 X 75.63 cM Grpr gastrin releasing peptide receptor 5,16,59
Rat 7 384 Xq14 Grpr gastrin releasing peptide receptor 4
Gene and Protein Information Comments
Phylogenetic analysis of the BB2 receptor is described in [3].
Previous and Unofficial Names Click here for help
GRP-R | BB2 | GRP-preferring bombesin receptor | Gastrin-releasing peptide receptor | gastrin-releasing peptide receptor
Database Links Click here for help
Specialist databases
GPCRdb grpr_human (Hs), grpr_mouse (Mm), grpr_rat (Rn)
Other databases
Alphafold P30550 (Hs), P21729 (Mm), P52500 (Rn)
ChEMBL Target CHEMBL4959 (Hs), CHEMBL3596 (Mm), CHEMBL4280 (Rn)
Ensembl Gene ENSG00000126010 (Hs), ENSMUSG00000031364 (Mm), ENSRNOG00000004124 (Rn)
Entrez Gene 2925 (Hs), 14829 (Mm), 24938 (Rn)
Human Protein Atlas ENSG00000126010 (Hs)
KEGG Gene hsa:2925 (Hs), mmu:14829 (Mm), rno:24938 (Rn)
OMIM 305670 (Hs)
Pharos P30550 (Hs)
RefSeq Nucleotide NM_005314 (Hs), NM_008177 (Mm), NM_012706 (Rn)
RefSeq Protein NP_005305 (Hs), NP_032203 (Mm), NP_036838 (Rn)
UniProtKB P30550 (Hs), P21729 (Mm), P52500 (Rn)
Wikipedia GRPR (Hs)
Natural/Endogenous Ligands Click here for help
gastrin releasing peptide(14-27) (human)
GRP-(18-27) {Sp: Human, Pig} , GRP-(18-27) {Sp: Mouse, Rat}
neuromedin B {Sp: Human, Mouse, Rat, Pig}
neuromedin C
Comments: Gastrin-releasing peptide is the endogenous agonist with the greatest potency

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I][Tyr4]bombesin Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.2 pKd 6
⤷ pKd 8.2 (Kd 6.31x10-9 M) [6]
[D-Tyr6,β-Ala11,N-Me-Ala13,Nle14]bombesin-(6-14) Peptide Hs Agonist 9.5 pKi 24
⤷ pKi 9.5 [24]
[Phe13]bombesin Peptide Click here for species-specific activity table Rn Full agonist 9.1 pKi 26,40
⤷ pKi 9.1 (Ki 7.7x10-10 M) [26,40]
gastrin-releasing peptide {Sp: Human} Peptide Mm Full agonist 8.6 – 8.9 pKi 26
⤷ pKi 8.6 – 8.9 (Ki 2.5x10-9 – 1.24x10-9 M) [26]
ranatensin Peptide Click here for species-specific activity table Rn Full agonist 8.7 pKi 26,40
⤷ pKi 8.7 (Ki 2x10-9 M) [26,40]
bombesin Peptide Mm Full agonist 8.2 – 9.1 pKi 6
⤷ pKi 8.2 – 9.1 (Ki 6.8x10-9 – 9x10-10 M) [6]
bombesin Peptide Click here for species-specific activity table Rn Full agonist 8.4 pKi 6
⤷ pKi 8.4 (Ki 4.1x10-9 M) [6]
litorin Peptide Click here for species-specific activity table Rn Full agonist 8.2 pKi 26,40
⤷ pKi 8.2 (Ki 6x10-9 M) [26,40]
[Phe13]bombesin Peptide Hs Full agonist 7.6 – 8.7 pKi 53
⤷ pKi 7.6 – 8.7 (Ki 2.8x10-8 – 1.8x10-9 M) [53]
bombesin Peptide Click here for species-specific activity table Hs Full agonist 7.4 – 8.9 pKi 6,53
⤷ pKi 7.4 – 8.9 (Ki 4.4x10-8 – 1.4x10-9 M) [6,53]
[D-Phe6,β-Ala11,Phe13,Nle14]bombesin-(6-14) Peptide Click here for species-specific activity table Hs Full agonist 7.8 – 8.0 pKi 24,53
⤷ pKi 7.8 – 8.0 (Ki 1.5x10-8 – 1x10-8 M) [24,53]
gastrin-releasing peptide {Sp: Human} Peptide Click here for species-specific activity table Rn Full agonist 7.7 pKi 6,40
⤷ pKi 7.7 (Ki 1.8x10-8 M) [6,40]
neuromedin C Peptide Rn Full agonist 7.7 pKi 26,40
⤷ pKi 7.7 (Ki 2x10-8 M) [26,40]
Rhodei-litorin Peptide Click here for species-specific activity table Rn Full agonist 7.5 pKi 26,40
⤷ pKi 7.5 (Ki 3.1x10-8 M) [26,40]
gastrin-releasing peptide {Sp: Human} Peptide Ligand is endogenous in the given species Hs Full agonist 6.3 – 8.2 pKi 6,53,68
⤷ pKi 6.3 – 8.2 (Ki 4.53x10-7 – 6.2x10-9 M) [6,53,68]
neuromedin B {Sp: Human, Mouse, Rat, Pig} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 6.4 – 8.1 pKi 6,53
⤷ pKi 6.4 – 8.1 (Ki 4.37x10-7 – 7.4x10-9 M) [6,53]
neuromedin B {Sp: Human, Mouse, Rat, Pig} Peptide Mm Full agonist 6.6 – 7.4 pKi 6
⤷ pKi 6.6 – 7.4 (Ki 2.3x10-7 – 4.2x10-8 M) [6]
phyllolitorin Peptide Click here for species-specific activity table Rn Full agonist 6.6 pKi 26,40
⤷ pKi 6.6 (Ki 2.4x10-7 M) [26,40]
neuromedin B {Sp: Human, Mouse, Rat, Pig} Peptide Rn Full agonist 6.6 pKi 53
⤷ pKi 6.6 (Ki 2.48x10-7 M) [53]
[Leu8]-phyllolitorin Peptide Click here for species-specific activity table Rn Full agonist 6.4 pKi 26,40
⤷ pKi 6.4 (Ki 4.2x10-7 M) [26,40]
[D-Phe6,β-Ala11,Phe13,Nle14]bombesin-(6-14) Peptide Click here for species-specific activity table Hs Full agonist 10.1 – 10.3 pIC50 68
⤷ pIC50 10.1 – 10.3 (IC50 8.5x10-11 – 4.8x10-11 M) [68]
bombesin Peptide Click here for species-specific activity table Hs Agonist 9.8 – 10.1 pIC50 68
⤷ pIC50 9.8 – 10.1 (IC50 1.7x10-10 – 7x10-11 M) [68]
gastrin-releasing peptide {Sp: Human} Peptide Hs Full agonist 9.9 – 10.0 pIC50 17
⤷ pIC50 9.9 – 10.0 (IC50 1.2x10-10 – 1.1x10-10 M) [17]
neuromedin C Peptide Ligand is endogenous in the given species Hs Full agonist 9.9 pIC50 68
⤷ pIC50 9.9 (IC50 1.4x10-10 M) [68]
gastrin releasing peptide(14-27) (human) Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 9.7 – 9.8 pIC50 68
⤷ pIC50 9.7 – 9.8 (IC50 1.9x10-10 – 1.7x10-10 M) [68]
(D-Ala11]bombesin Peptide Hs Full agonist 9.1 – 9.3 pIC50 68
⤷ pIC50 9.1 – 9.3 (IC50 7.1x10-10 – 5.4x10-10 M) [68]
ranatensin Peptide Click here for species-specific activity table Rn Full agonist 9.0 pIC50 68
⤷ pIC50 9.0 (IC50 1.08x10-9 M) [68]
litorin Peptide Hs Agonist 8.6 – 9.3 pIC50 68
⤷ pIC50 8.6 – 9.3 (IC50 2.69x10-9 – 5.4x10-10 M) [68]
[Leu14]bombesin Peptide Hs Agonist 8.9 pIC50 68
⤷ pIC50 8.9 (IC50 1.32x10-9 M) [68]
litorin Peptide Click here for species-specific activity table Rn Full agonist 8.8 pIC50 68
⤷ pIC50 8.8 (IC50 1.66x10-9 M) [68]
ranatensin Peptide Click here for species-specific activity table Hs Full agonist 8.5 – 8.6 pIC50 68
⤷ pIC50 8.5 – 8.6 (IC50 3.16x10-9 – 2.24x10-9 M) [68]
neuromedin B (1-30) (human) Peptide Click here for species-specific activity table Hs Full agonist 7.7 – 7.8 pIC50 68
⤷ pIC50 7.7 – 7.8 (IC50 1.82x10-8 – 1.531x10-8 M) [68]
Rhodei-litorin Peptide Click here for species-specific activity table Rn Full agonist 7.6 pIC50 68
⤷ pIC50 7.6 (IC50 2.32x10-8 M) [68]
neuromedin B {Sp: Human, Mouse, Rat, Pig} Peptide Click here for species-specific activity table Hs Full agonist 7.4 – 7.5 pIC50 17,68
⤷ pIC50 7.4 – 7.5 (IC50 3.8x10-8 – 3.01x10-8 M) [17,68]
neuromedin C Peptide Rn Full agonist 7.3 pIC50 68
⤷ pIC50 7.3 (IC50 4.9x10-8 M) [68]
[Leu8]-phyllolitorin Peptide Click here for species-specific activity table Rn Full agonist 6.9 pIC50 68
⤷ pIC50 6.9 (IC50 1.2x10-7 M) [68]
Rhodei-litorin Peptide Click here for species-specific activity table Hs Full agonist 6.7 – 7.0 pIC50 68
⤷ pIC50 6.7 – 7.0 (IC50 1.9x10-7 – 1.1x10-7 M) [68]
phyllolitorin Peptide Click here for species-specific activity table Rn Full agonist 6.7 pIC50 68
⤷ pIC50 6.7 (IC50 1.9x10-7 M) [68]
[Leu8]-phyllolitorin Peptide Click here for species-specific activity table Hs Full agonist 6.3 – 6.4 pIC50 68
⤷ pIC50 6.3 – 6.4 (IC50 5.24x10-7 – 3.72x10-7 M) [68]
phyllolitorin Peptide Click here for species-specific activity table Hs Full agonist <5.5 pIC50 68
⤷ pIC50 <5.5 (IC50 >3x10-6 M) [68]
MK-5046 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist <5.0 pIC50 46
⤷ pIC50 <5.0 (IC50 >1x10-5 M) [46]
[125I]GRP (human) Peptide Ligand is labelled Ligand is radioactive Hs Full agonist - -
⤷
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
[125I][D-Tyr6]bombesin-(6-13)-methyl ester Peptide Ligand is labelled Ligand is radioactive Mm Antagonist 9.3 pKd 39
⤷ pKd 9.3 (Kd 5.3x10-10 M) [39]
[125I][D-Tyr6]bombesin-(6-13)-methyl ester Peptide Ligand is labelled Ligand is radioactive Rn Antagonist 9.0 pKd 39
⤷ pKd 9.0 (Kd 1.1x10-9 M) [39]
[D-Phe6, Leu13, Cpa14,ψ13-14]bombesin-(6-14) Peptide Primary target of this compound Click here for species-specific activity table Hs Antagonist 9.8 pKi 17
⤷ pKi 9.8 [17]
PD 176252 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 9.0 pKi 2
⤷ pKi 9.0 (Ki 1x10-9 M) [2]
[D-Phe6]bombesin(6-13)propylamide Peptide Rn Antagonist 8.2 pKi 26
⤷ pKi 8.2 (Ki 6x10-9 M) [26]
[Leu14, ψ 13-14)]bombesin Peptide Hs Antagonist 8.1 pKi 6
⤷ pKi 8.1 (Ki 7.7x10-9 M) [6]
[D-Phe6]bombesin(6-13)methyl ester Peptide Rn Antagonist 8.0 pKi 26
⤷ pKi 8.0 (Ki 1x10-8 M) [26]
PD 168368 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 – 7.8 pKi 53
⤷ pKi 7.5 – 7.8 (Ki 3x10-8 – 1.5x10-8 M) [53]
[D-Phe6, Leu13, Cpa14,ψ13-14]bombesin-(6-14) Peptide Rn Antagonist 7.4 pKi 26
⤷ pKi 7.4 (Ki 4.2x10-8 M) [26]
D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Nal-NH2 Peptide Click here for species-specific activity table Hs Antagonist 6.7 – 6.8 pKi 53
⤷ pKi 6.7 – 6.8 (Ki 2.16x10-7 – 1.7x10-7 M) [53]
AM-37 Small molecule or natural product Hs Antagonist 5.8 pKi 45
⤷ pKi 5.8 (Ki 1.4x10-6 M) [45]
Description: Measuring inhibition of specific [125]I-BA1 binding to hBB2 receptor in vitro.
D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Nal-NH2 Peptide Click here for species-specific activity table Rn Antagonist <5.0 pKi 26
⤷ pKi <5.0 (Ki >1x10-5 M) [26]
[D-Phe6]bombesin(6-13)methyl ester Peptide Hs Antagonist <5.0 pKi 53
⤷ pKi <5.0 (Ki >1x10-5 M) [53]
[D-Phe12]bombesin Peptide Rn Antagonist 5.0 pKi 26
⤷ pKi 5.0 (Ki 1x10-5 M) [26]
[D-Pro4,D-Trp7,9,10]substance P (4-11) Peptide Rn Antagonist <5.0 pKi 26
⤷ pKi <5.0 (Ki >1x10-5 M) [26]
[D-Arg1,D-Trp7,9,Leu11]substance P Peptide Rn Antagonist 4.9 pKi 26
⤷ pKi 4.9 (Ki 1.13x10-5 M) [26]
[(3-Ph-Pr6), His7,D-Ala11,D-Pro13,ψ13-14),Phe14]bombesin-(6-14) Peptide Mm Antagonist 12.0 pIC50 33
⤷ pIC50 12.0 (IC50 1x10-12 M) [33]
JMV641 Peptide Primary target of this compound Mm Antagonist 9.3 pIC50 66
⤷ pIC50 9.3 (IC50 4.6x10-10 M) [66]
[(3-Ph-Pr6), His7,D-Ala11,D-Pro13,ψ13-14),Phe14]bombesin-(6-14) Peptide Hs Antagonist 9.2 pIC50 17,33
⤷ pIC50 9.2 [17,33]
[D-Phe6]bombesin(6-13)propylamide Peptide Hs Antagonist 8.6 – 9.4 pIC50 17
⤷ pIC50 8.6 – 9.4 (IC50 2.63x10-9 – 3.9x10-10 M) [17]
JMV594 Peptide Primary target of this compound Mm Antagonist 8.9 pIC50 36,66
⤷ pIC50 8.9 [36,66]
[D-Phe6, Leu13, Cpa14,ψ13-14]bombesin-(6-14) Peptide Click here for species-specific activity table Hs Antagonist 8.9 – 8.9 pIC50 17
⤷ pIC50 8.9 – 8.9 (IC50 1.35x10-9 – 1.23x10-9 M) [17]
[D-Tpi6, Leu13 ψ(CH2NH)-Leu14]bombesin-(6-14) Peptide Hs Antagonist 8.8 – 8.9 pIC50 17
⤷ pIC50 8.9 [17]
pIC50 8.8 – 8.9 (IC50 1.58x10-9 – 1.32x10-9 M) [17]
[D-Phe6]bombesin(6-13)methyl ester Peptide Hs Antagonist 8.4 – 9.1 pIC50 17
⤷ pIC50 8.4 – 9.1 (IC50 3.98x10-9 – 8.9x10-10 M) [17]
Ac-GRP-(20-26)-methylester Peptide Hs Antagonist 8.7 pIC50 17
⤷ pIC50 8.7 [17]
Ac-GRP-(20-26)-methylester Peptide Mm Antagonist 8.4 pIC50 22
⤷ pIC50 8.4 [22]
BAY86-7548 Peptide Ligand is labelled Ligand is radioactive Hs Antagonist 8.1 – 8.6 pIC50 30-31,37-38,68
⤷ pIC50 8.6 (IC50 2.51x10-9 M) [31,68]
pIC50 8.1 (IC50 7.9x10-9 M) [30,37-38]
[Leu14, ψ 13-14)]bombesin Peptide Hs Antagonist 8.1 – 8.1 pIC50 17
⤷ pIC50 8.1 – 8.1 (IC50 8.12x10-9 – 7.7x10-9 M) [17]
[D-Phe6, Stat13, Leu14}Bn(6-14) Peptide Hs Antagonist 8.1 pIC50 38
⤷ pIC50 8.1 (IC50 7.94x10-9 M) [38]
[D-Tpi6, Leu13 ψ(CH2NH)-Leu14]bombesin-(6-14) Peptide Mm Antagonist 8.0 pIC50 50
⤷ pIC50 8.0 [50]
PD 176252 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.7 – 6.8 pIC50 17
⤷ pIC50 6.7 – 6.8 (IC50 2.13x10-7 – 1.7x10-7 M) [17]
pIC50 6.7 – 6.8 (IC50 2.13x10-7 – 1.7x10-7 M) [17]
kuwanon H Small molecule or natural product Mm Antagonist 6.5 pIC50 44
⤷ pIC50 6.5 [44]
[D-Arg1,D-Trp7,9,Leu11]substance P Peptide Hs Antagonist 5.8 – 6.1 pIC50 17
⤷ pIC50 5.8 – 6.1 (IC50 1.78x10-6 – 7.94x10-7 M) [17]
PD 168368 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.8 – 5.9 pIC50 17
⤷ pIC50 5.8 – 5.9 (IC50 1.738x10-6 – 1.172x10-6 M) [17]
D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Nal-NH2 Peptide Click here for species-specific activity table Hs Antagonist 5.3 – 5.6 pIC50 17
⤷ pIC50 5.3 – 5.6 (IC50 4.57x10-6 – 2.46x10-6 M) [17]
pIC50 5.3 – 5.6 (IC50 4.57x10-6 – 2.46x10-6 M) [17]
D-Nal,Cys,Tyr,D-Trp,Orn,Val,Cys,Nal-NH2 Peptide Click here for species-specific activity table Hs Antagonist 5.0 – 5.5 pIC50 17
⤷ pIC50 5.0 – 5.5 (IC50 1x10-5 – 3.47x10-6 M) [17]
[D-Pro4,D-Trp7,9,10]substance P (4-11) Peptide Hs Antagonist 5.0 – 5.4 pIC50 17
⤷ pIC50 5.0 – 5.4 (IC50 1x10-5 – 3.8x10-6 M) [17]
bantag-1 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.0 – 5.4 pIC50 19,46
⤷ pIC50 5.0 – 5.4 (IC50 1x10-5 – 4.4x10-6 M) [19,46]
View species-specific antagonist tables
Antagonist Comments
A number of studies show significant species variation in antagonist activity with some analogues functioning as partial agonists/ full agonists in some species [70].
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
Phospholipase A2 stimulation
Phospholipase D stimulation
Comments:  Receptor activation also results in stimulation of Na/H antiport, activation of numerous tyrosine kinases and transactivation of the EGFR receptor in various tumors.
References:  14,35,47,52,57,60
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
G protein (identity unknown) Adenylyl cyclase stimulation
Phospholipase A2 stimulation
Phospholipase D stimulation
References:  7,11,15
Tissue Distribution Click here for help
Highly expressed in pancreas. Also expressed in stomach, adrenal cortex and brain.
Species:  Human
Technique:  Ribonuclease protection assay, northern blot
References:  10
Brain (hypothalamus), pancreatic acinar cells, and fibroblasts.
Species:  Mouse
Technique:  Northern Blot, Sequencing analysis
References:  5
Expression Datasets Click here for help

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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 Click here for help
Calcium-dependant chloride currents in Xenopus oocytes injected with RNA for the human BB2 receptor could be measured in response to GRP and blocked by the BB2-specific inhibitor [D-phe]BN(6-13).
Species:  Human
Tissue:  Xenopus oocytes.
Response measured:  Production of chloride currents, blocked by a specific BB2 antagonist.
References:  10
Measurement of CREB (cAMP response element binding protein) phosphorylation and transactivation in the HuTu b80 duodenal cancer cell line.
Species:  Human
Tissue:  HuTu 80 cells.
Response measured:  CREB phosphorylation.
References:  49
Measurement of Prostaglandin synthase 2 (PGS-2) mRNA and protein in Swiss 3T3 cells containing native BB2 receptors.
Species:  Mouse
Tissue:  Swiss 3T3 cells.
Response measured:  Induction of PGS-2 expression.
References:  21
Measurement of phospholipase C activation- HUMAN, RAT and MOUSE.
Species:  Human
Tissue:  HuTu 80 cells (human),Swiss 3t3 cells (mouse), AR42J cells (rat).
Response measured:  [3H]inositol phosphate formation.
References:  17,39,44,66,68
Measurement of tyrosine kinase activity (formation p125FAK, p-paxillin)- HUMAN, RAT and MOUSE.
Species:  Human
Tissue:  HuTu 80 cells,Swiss 3t3 cells, lung cancer cells, AR42J cells.
Response measured:  Phosphorylation of FAK (tyrosine 125) and paxillin.
References:  34,51,74
Physiological Functions Click here for help
Hypothermia.
Species:  Rat
Tissue:  In vivo.
References:  8,65,67
GRP was found to be an anti-convulsant in seizure-prone DBA/2 mice. This may be due to increased GABAergic function in the hippocampus.
Species:  Mouse
Tissue:  In vivo.
References:  1
Increase in extracellular GABA levels in the rat hippocampus.
Species:  Rat
Tissue:  In vivo.
References:  1
Receptor activation suppresses food intake by increasing postingestive negative feedback, not by decreasing the palatability of the food.
Species:  Rat
Tissue:  in vivo.
References:  28,61
GRP is a neurotransmitter regulating pancreatic secretion- PIG and DOG
Species:  Pig
Tissue:  In vivo.
References:  23,25,27
CNS BB2 receptor activation affects GI function (suppresses gastric acid/pepsin secretion, gastrin/histamine release, increases bicarbonate/mucous release and stimulates vagally mediated contractions). These effects are also observed in dogs.
Species:  Rat
Tissue:  In vivo.
References:  41,62-64
BB2 receptor activation in lumbosacral spinal cord is essential for ejaculations in males.
Species:  Rat
Tissue:  In vivo.
References:  29,54
GRP is the modulatory neurotransmitter of the descending phase of the peristaltic reflex.
Species:  Rat
Tissue:  Colon.
References:  18
GRP regulates gastric acid secretion/gastrin release through BB2 receptor on antral G cells and D cells.
Species:  Mouse
Tissue:  Isolated perfused stomach.
References:  55-56
BB2 receptor activation affects lymphoid and neutrophil function (inhibits lymphocyte chemotaxis, leukocyte cytotoxicity and leukocyte chemoattractant activity).
Species:  Mouse
Tissue:  Isolated lymphocytes and neutrophils.
References:  12-13,42-43
Physiological Consequences of Altering Gene Expression Click here for help
BB2 receptor knockout mice show poor tumour differentiation, suggesting the BB2 receptor has a role in regulating tumour morphology.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  9
BB2 receptor knockout mice fail to suppress glucose intake following bombesin and gastrin-releasing peptide administration. The knockout mice ate more food at each meal, although total daily food consumption was the same as the wild-type mice. This suggests the involvement of the BB2 receptor in a meal-related satiety signal.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  32
In a social preference test, female BB2 receptor knockout mice showed a reduced preference towards the socially dominant male mice. However, in a similar test using anaesthetized males as the target the knockouts showed increased investigatory behaviour. It is suggested these behavioural changes may be due to altered GABAergic function in the BB2 knockout mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  73
BB2 receptor knockout mice show no gross abnormalities, however they do not suppress glucose intake upon bombesin administration, as wild-type mice do.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  20
BB2 receptor knockout mice show decreased inhibition of the principal neurons by the interneurons, enhanced long-term potentiation and greater and more persistent long-term fear memory. This suggests that the GRP signaling pathway serves as an inhibitory feedback constraint on learned fear.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  58
BB2 receptor knockout mice exhibit altered social behavior.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  72-73
BB2 receptor knockout mice altered insulin secretion by activation of the autonomic nerves.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  48
Intracerebroventricular administration of gastrin-releasing peptide (GRP) causes hypothermia in wild-type mice, which is not seen in BB2 receptor knockout mice. This suggests this receptor subtype is involved in body temperature regulation. The BB2 receptor knockout mice also showed increased locomotor activity during the dark period and abnormal social behaviour.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  69
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Grprtm1Jfb Grprtm1Jfb/Y
involves: 129X1/SvJ * C57BL/6J		 MGI:95836  MP:0005449 abnormal food intake PMID: 9501238 
Grprtm1Wada Grprtm1Wada/Y
involves: 129P2/OlaHsd * C57BL/6J		 MGI:95836  MP:0003638 abnormal response/metabolism to endogenous compounds PMID: 9345264 
Grprtm1Wada Grprtm1Wada/Y
involves: 129P2/OlaHsd * C57BL/6J		 MGI:95836  MP:0001360 abnormal social investigation PMID: 9345264 
Grprtm1Wada Grprtm1Wada/Y
involves: 129P2/OlaHsd * C57BL/6J		 MGI:95836  MP:0001399 hyperactivity PMID: 9345264 
Grprtm1Jfb Grprtm1Jfb/Grprtm1Jfb
involves: 129X1/SvJ * C57BL/6J		 MGI:95836  MP:0002169 no abnormal phenotype detected PMID: 9501238 
Biologically Significant Variant Comments
It is predicted that glycosylation of aa 20 may occur in humans and that glycosylation of aa 5, 20 and 24 may occur in both rat and mouse.

References

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74. Zachary I, Gil J, Lehmann W, Sinnett-Smith J, Rozengurt E. (1991) Bombesin, vasopressin, and endothelin rapidly stimulate tyrosine phosphorylation in intact Swiss 3T3 cells. Proc Natl Acad Sci USA, 88 (11): 4577-81. [PMID:1647010]

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