Nomenclature: secretin receptor

Family: Glucagon receptor family

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

Contents

Gene and Protein Information
class B G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 440 2q14.1 SCTR secretin receptor 1,11,13
Mouse 7 337 1 E2.3 Sctr secretin receptor
Rat 7 449 13 Sctr secretin receptor 9
Previous and Unofficial Names
MGC93381
SCT-R
6530402O03Rik
Database Links
ChEMBL Target
DrugBank 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
secretin {Sp: Rat} , secretin {Sp: Human} , secretin {Sp: Mouse}
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]secretin (pig) Rn Full agonist 7.7 – 9.2 pKd 9
pKd 7.7 – 9.2 [9]
[Bpa6,Tyr10]secretin-27 (rat) Rn Full agonist 7.6 pKd 4
pKd 7.6 [4]
secretin {Sp: Pig} Rn Full agonist 8.0 – 9.0 pKi 9
pKi 8.0 – 9.0 [9]
secretin {Sp: Rat} Rn Full agonist 8.0 – 9.0 pKi 4-5
pKi 8.0 – 9.0 [4-5]
secretin {Sp: Human} Hs Full agonist 9.7 pEC50 1
pEC50 9.7 (EC50 2x10-10 M) [1]
secretin {Sp: Pig} Rn Agonist 9.0 pIC50 6
pIC50 9.0 (IC50 1x10-9 M) [6]
Description: Inhibition of [125I]Tyr25 secretin binding in membranes from CHO cells expressing recombinant receptor
[Arg16]chicken secretin Rn Agonist 7.7 pIC50 6
pIC50 7.7 (IC50 2x10-8 M) [6]
Description: Inhibition of [125I]Tyr25 secretin binding in membranes from CHO cells expressing recombinant receptor
VIP {Sp: Human, Mouse, Rat} Rn Agonist 6.2 pIC50 6
pIC50 6.2 (IC50 6x10-7 M) [6]
Description: Inhibition of [125I]Tyr25 secretin binding in membranes from CHO cells expressing recombinant receptor
VIP {Sp: Human, Mouse, Rat} Hs Partial agonist 5.4 pIC50 9
pIC50 5.4 [9]
secretin-(5-27) (pig) Rn Full agonist 5.0 pIC50 9
pIC50 5.0 [9]
View species-specific agonist tables
Antagonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[(CH2NH)4,5]secretin Hs Antagonist 5.3 pKi 7
pKi 5.3 [7]
Primary Transduction Mechanisms
Transducer Effector/Response
Adenylate cyclase stimulation
Calcium channel
References: 
Tissue Distribution
Duodenum, jejunum, pancreas, tertiary bronchus, lung parenchyma and pulmonary artery.
Species:  Human
Technique:  RT-PCR.
References:  3
Cerebellum, central amygdala, hippocampus, area postrema and the nucleus of the tractus solitary.
Species:  Rat
Technique:  RT-PCR.
References:  16
Jejunum, pancreas, epididymis.
Species:  Rat
Technique:  RT-PCR.
References:  2
Epididymis: Principle cells of the capus region > initial segement.
Species:  Rat
Technique:  Western blotting.
References:  2
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 cAMP levels in CHO cells transfected with the secretin receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of cAMP accumulation.
References:  14
Measurement of the extracellular acidification rate in CHO cells transfected with the human secretin receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Increase in ectracellular acidification rate.
References:  14
Measurement of short-circuit current (Isc) caused by chloride and bicarbonate secretion in cultured epididymal epithelia.
Species:  Human
Tissue:  Cultured epididymal epithelia.
Response measured:  Stimulation of Isc.
References:  2
Physiological Functions
Secretin activates GABA release both directly and indirectly via glutamate release.
Species:  Rat
Tissue:  Cerebellum.
References:  12
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Sctrtm1Bkcc Sctrtm1Bkcc/Sctrtm1Bkcc
B6.129S7-Sctr
MGI:2441720  MP:0003009 abnormal cytokine secretion PMID: 17283064 
Sctrtm1Bkcc Sctrtm1Bkcc/Sctrtm1Bkcc
B6.129S7-Sctr
MGI:2441720  MP:0000521 abnormal kidney cortex PMID: 17283064 
Sctrtm1Bkcc Sctrtm1Bkcc/Sctrtm1Bkcc
B6.129S7-Sctr
MGI:2441720  MP:0003014 abnormal kidney medulla morphology PMID: 17283064 
Sctrtm1Bkcc Sctrtm1Bkcc/Sctrtm1Bkcc
B6.129S7-Sctr
MGI:2441720  MP:0009643 abnormal urine homeostasis PMID: 17283064 
Sctrtm1Bkcc Sctrtm1Bkcc/Sctrtm1Bkcc
B6.129S7-Sctr
MGI:2441720  MP:0005618 decreased potassium excretion PMID: 17283064 
Sctrtm1Bkcc Sctrtm1Bkcc/Sctrtm1Bkcc
B6.129S7-Sctr
MGI:2441720  MP:0005570 decreased sodium excretion PMID: 17283064 
Sctrtm1Bkcc Sctrtm1Bkcc/Sctrtm1Bkcc
B6.129S7-Sctr
MGI:2441720  MP:0002988 decreased urine osmolality PMID: 17283064 
Sctrtm1Bkcc Sctrtm1Bkcc/Sctrtm1Bkcc
B6.129S7-Sctr
MGI:2441720  MP:0004860 dilated kidney collecting duct PMID: 17283064 
Sctrtm1Bkcc Sctrtm1Bkcc/Sctrtm1Bkcc
B6.129S7-Sctr
MGI:2441720  MP:0005559 increased circulating glucose level PMID: 17283064 
Sctrtm1Bkcc Sctrtm1Bkcc/Sctrtm1Bkcc
B6.129S7-Sctr
MGI:2441720  MP:0005425 increased macrophage cell number PMID: 17283064 
Sctrtm1Bkcc Sctrtm1Bkcc/Sctrtm1Bkcc
B6.129S7-Sctr
MGI:2441720  MP:0001859 kidney inflammation PMID: 17283064 
Sctrtm1Bkcc Sctrtm1Bkcc/Sctrtm1Bkcc
B6.129S7-Sctr
MGI:2441720  MP:0001426 polydipsia PMID: 17283064 
Sctrtm1Bkcc Sctrtm1Bkcc/Sctrtm1Bkcc
B6.129S7-Sctr
MGI:2441720  MP:0001762 polyuria PMID: 17283064 
General Comments
There appear to be important species differences in the cellular and organ distribution of secretin and secretin family receptors. The best example of this is the confusing series of observations in pancreas of guinea-pig, rat, and human[10,15]. There are also differences in the pharmacologic profile of secretin receptors from different species, despite minimal changes in primary structure. Rat and human secretin receptors have very different binding affinities for VIP that have been attributed to a single receptor residue[8].
Available Assays
DiscoveRx PathHunter® CHO-K1 SCTR β-Arrestin Cell Line (Cat no. 93-0237C2)
PathHunter® eXpress SCTR CHO-K1 β-Arrestin GPCR Assay (Cat no. 93-0237E2CP0M)
PathHunter® HEK 293 SCTR β-Arrestin Cell Line (Cat no. 93-0237C1)
more info

REFERENCES

1. Chow BK. (1995) Molecular cloning and functional characterization of a human secretin receptor. Biochem. Biophys. Res. Commun.212: 204-211. [PMID:7612008]

2. Chow BK, Cheung KH, Tsang EM, Leung MC, Lee SM, Wong PY. (2004) Secretin controls anion secretion in the rat epididymis in an autocrine/paracrine fashion. Biol Reprod70: 1594-1599. [PMID:14749298]

3. Davis RJ, Page KJ, Dos Santos Cruz GJ, Harmer DW, Munday PW, Williams SJ, Picot J, Evans TJ, Sheldrick RL, Coleman RA, Clark KL. (2004) Expression and functions of the duodenal peptide secretin and its receptor in human lung. Am J Respir Cell Mol Biol31: 302-308. [PMID:15191914]

4. Dong M, Wang Y, Hadac EM, Pinon DI, Holicky E, Miller LJ. (1999) Identification of an interaction between residue 6 of the natural peptide ligand and a distinct residue within the amino-terminal tail of the secretin receptor. J Biol Chem274: 19161-19167. [PMID:10383421]

5. Ganguli SC, Park CG, Holtmann MH, Hadac EM, Kenakin TP, Miller LJ. (1998) Protean effects of a natural peptide agonist of the G protein-coupled secretin receptor demonstrated by receptor mutagenesis. J Pharmacol Exp Ther286: 593-598. [PMID:9694908]

6. Gourlet P, Vandermeers A, Vertongen P, Rathe J, De Neef P, Cnudde J, Waelbroeck M, Robberecht P. (1997) Development of high affinity selective VIP1 receptor agonists. Peptides18: 1539-1545. [PMID:9437714]

7. Haffar BM, Hocart SJ, Coy DH, Mantey S, Chiang HC, Jensen RT. (1991) Reduced peptide bond pseudopeptide analogues of secretin. A new class of secretin receptor antagonists. J. Biol. Chem.266 (1): 316-22. [PMID:1702423]

8. Holtmann MH, Miller LJ. (1996) Molecular basis and species specificity of high affinity binding of vasoactive intestinal polypeptide by the rat secretin receptor. J. Pharmacol. Exp. Ther.279: 555-560. [PMID:8930157]

9. Ishihara T, Nakamura S, Kaziro Y, Takahashi T, Takahashi K, Nagata S. (1991) Molecular cloning and expression of a cDNA encoding the secretin receptor. EMBO J.10: 1635-1641. [PMID:1646711]

10. Jensen RT, Gardner JD. (1980) Interaction of cholecystokinin with specific membrane receptors on pancreatic acinar cells. Proc. Natl. Acad. Sci. U.S.A.77: 2079-2083. [PMID:6246521]

11. Jiang S, Ulrich C. (1995) Molecular cloning and functional expression of a human pancreatic secretin receptor. Biochem. Biophys. Res. Commun.207: 883-890. [PMID:7864894]

12. Lee SM, Chen L, Chow BK, Yung WH. (2005) Endogenous release and multiple actions of secretin in the rat cerebellum. Neuroscience, : -. [PMID:15963647]

13. Mark HF, Chow BK. (1995) Localization of the gene encoding the secretin receptor, SCTR, on human chromosome 2q14.1 by fluorescencein situhybridization and chromosome morphometry. Genomics29: 817-818. [PMID:8575789]

14. Ng SS, Pang RT, Chow BK, Cheng CH. (1999) Real-time evaluation of human secretin receptor activity using cytosensor microphysiometry. J Cell Biochem72: 517-527. [PMID:10022611]

15. Robberecht P, Christophe J. (1988) Secretin receptors in human pancreatic membranes. Pancreas3: 529-535. [PMID:3186683]

16. Tay J, Goulet M, Rusche J, Boismenu R. (2004) Age-related and regional differences in secretin and secretin receptor mRNA levels in the rat brain. Neurosci Lett366: 176-181. [PMID:15276242]

To cite this database page, please use the following:

Dominique Bataille, Philippe Delagrange, Daniel J. Drucker, Burkhard Göke, Rebecca Hills, Kelly E. Mayo, Laurence J. Miller, Bernard Thorens.
Glucagon receptor family: secretin receptor. Last modified on 06/01/2014. Accessed on 23/07/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=252.

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