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RXFP3
| Previous and Unofficial Names |
| GPCR135 |
| SALPR |
| RLN3R1 |
| Structural Information |
|
class A G protein-coupled receptor |
| Species |
TM |
AA |
Chromosomal Location |
Gene Name |
Reference |
| Human |
7 |
469 |
5p15.1-p14 |
RXFP3
|
45 |
| Rat |
7 |
476 |
2q16 |
Rxfp3
|
|
| Mouse |
7 |
472 |
15 A1 |
Rxfp3
|
46 |
|
|
| Database Links |
|
Ensembl |
ENSG00000182631 (Hs), ENSMUSG00000060735 (Mm), ENSRNOG00000023126 (Rn) |
|
Entrez Gene |
51289 (Hs), 239336 (Mm), 294807 (Rn) |
|
GeneCards |
RXFP3 (Hs) |
|
HomoloGene |
9568 (Hs) |
|
OMIM |
609445 (Hs) |
|
PharmGKB Gene |
PA134868535 (Hs) |
|
Protein Ontology (PRO) |
PRO:000001552 (Hs) |
|
RefSeq Nucleotide |
NM_016568 (Hs), NM_178717 (Mm), NM_001008310 (Rn) |
|
RefSeq Protein |
NP_057652 (Hs), NP_848832 (Mm), NP_001008311 (Rn) |
|
UniGene Hs. |
170146 (Hs) |
|
UniProt |
Q9NSD7 (Hs), Q8BGE9 (Mm), Q5Y986 (Rn) |
|
Wikipedia |
RXFP3 |
| Search for 3D structures on the PDB |
|
Search using keywords: Relaxin family peptide receptors RXFP3
|
Search using accession numbers: Q5Y986 || Q9NSD7 || Q8BGE9
|
| Agonists |
|
Key to terms and symbols
|
|
Click column headers to sort
|
|
|
| Agonist Comments |
H3 relaxin activates RXFP3 but also RXFP4 and RXFP1. Relaxin-3 is highly conserved across species and is believed to be the ancestral relaxin.
Affinity values were determined in COS-7 cells transiently expressing human RXFP3 labelled using [125I]H3 relaxin. |
| Antagonists |
|
Key to terms and symbols
|
|
Click column headers to sort
|
| Ligand |
|
|
|
|
|
INSL5
|
|
|
|
|
Hs |
Antagonist |
6.3 |
pIC50 |
50 |
|
| Antagonist Comments |
Affinity values were determined in COS-7 cells transiently expressing human RXFP3 labelled using [125I] H3 relaxin.
Produces parallel rightward shifts of c/r curve to H3 relaxin induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cells expressing human RXFP3 receptors. |
| Primary Transduction Mechanisms
|
| Transducer |
Effector/Response |
|
Gi/Go family |
Adenylate cyclase inhibition |
| Tissue Distribution
|
| Brain, testis, thymus, adrenal gland. |
| Species: |
Human |
| Technique: |
RT-PCR. |
| References: |
49 |
|
|
| Olfactory bulb, sensory cortex, amygdala, thalamus, paraventricular nucleus, supraoptic nucleus, inferior and superior colliculus. |
| Species: |
Rat |
| Technique: |
Autoradiography. |
| References: |
48,52 |
|
|
| Brain, testis. |
| Species: |
Mouse |
| Technique: |
RT-PCR. |
| References: |
47 |
|
|
| Brain, testis. |
| Species: |
Rat |
| Technique: |
RT-PCR. |
| References: |
47 |
|
|
| Hypothalamus, supraoptic nucleus, periaqueductal gray, nucleus incertus, brainstem, olfactory bulb, sensory cortex, amygdala, thalamus, paraventricular nucleus, inferior and superior colliculus. |
| Species: |
Human |
| Technique: |
in situ hybridisation. |
| References: |
49,52 |
|
|
| Functional Assays
|
| Inhibition of forskolin stimulated cAMP responses in CHO-K1 cells stably transfected with human RXFP3 receptors. |
| Species: |
Human |
| Tissue: |
CHO-K1 cells. |
| Response measured: |
cAMP accumulation. |
| References: |
47-50 |
|
|
| [35S] GTPγS incorporation in CHO-K1 cells stably transfected with human RXFP3 receptors. |
| Species: |
Human |
| Tissue: |
CHO-K1 cells. |
| Response measured: |
[35S] GTPγS incorporation. |
| References: |
47,49 |
|
|
| Reporter gene assay in SK-N-MC/β-gal cells stably transfected with human RXFP3 receptors. |
| Species: |
Human |
| Tissue: |
SK-N-MC cells. |
| Response measured: |
Increased β-galactosidase expression. |
| References: |
48,50 |
|
|
| Ca2+ mobilisation assay in HEK 293 cells transiently expressing human RXFP3 receptors and Gα16. |
| Species: |
Human |
| Tissue: |
HEK 293 cells. |
| Response measured: |
Ca2+ dye Fluo-3 fluorescence. |
| References: |
48,50 |
|
|
| Extracellular acidification rate response of CHO-K1 cells stably expressing human RXFP3 receptors in the cytosensor microphysiometer. |
| Species: |
Human |
| Tissue: |
CHO-K1 cells. |
| Response measured: |
Increased extracellular acidification rate. |
| References: |
51 |
|
|
| Physiological Functions
|
| Sensory processing particularly under stressful conditions. |
| Species: |
Rat |
| Tissue: |
Brain. |
| References: |
52 |
|
|
To cite this receptor data page, please use the following:
Ross Bathgate, Richard Ivell, Barbara Sanborn, David Sherwood, Roger Summers.
Relaxin family peptide receptors: RXFP3. Last modified on 2010-07-01. Accessed on 2010-09-09. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=353.
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