Ghrelin Receptor (GHS-R)

GH secretagogues (GHSs) are synthetic compounds that are potent stimulators of GH release. GHSs, act through a novel orphan G-protein-coupled receptor (GPCR), the GHS receptor (GHS-R). Ghrelin has been purified and identified from rat and human stomach as the endogenous ligand for the GHS-R. The rat and human mature Ghrelin (28-aa) are produced from 117 amino acids precursor. In rat stomach, a 28-aa Ghrelin and des-Gln14-Ghrelin (deletion of Gln14) are produced due to alternative splicing of Ghrelin mRNA. The activity of both Ghrelins is the same. Ghrelin has an unusual modification at Ser3 residue that is n-octanoylated and it is essential for biological activity. Rat Ghrelin is expressed in the stomach, small and large intestines, and brain regions (hypothalamic arcuate nucleus) that are involved the regulation of food intake. Both Ghrelin and GHS-R expression is detected in the heart, suggesting that Ghrelin might have some cardiovascular effects. GHS-R (rat 364aa; human 366aa, ~90% sequence homology) is a receptor for GHRP and non-peptide, low mol wt. secreatgogues. This receptor is coupled to G-a11. Two isoforms of GHS-R have been reported: isoform 1a (human 36aa) and type 1b (289aa and only 5 TM domains) appears not to bind the ghrelin. GHS-R displays the typical structure of GPCR with TM domains, extracellular N-terminus and intracellular C-terminus. It is expressed in not only in the pituitary and hypothalamus but also in the hippocampus, pancreas, and neuroendocrine tumors, including somatotropinomas and rat GH3 cells.\n\nApplications: \nSuitable for use in ELISA and Western Blot. Other applications not tested.\n\nRecommended Dilution:\nWestern Blot:1-10ug/ml using ECL. \nELISA: 1:10,000-1:100,000 using 50-100ng G2033-75N control peptide/well.\nOptimal dilutions to be determined by the researcher.\n\nStorage and Stability:\nMay be stored at 4 degrees C for short-term only. Aliquot to avoid repeated freezing and thawing. Store at -20 degrees C. Aliquots are stable for at least 12 months. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap.

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SPECIFICATIONS

Catalog Number

G2033-75M

Size

50ug

Applications

ELISA, WB

Hosts

Rabbit

Reactivities

Rat

Form

Supplied as a liquid in PBS, pH 7.4, 0.1% BSA.

P Type

Pab

Purity

Purified by immunoaffinity chromatography.

Isotype

IgG

References

1. Howard AD et al Science 273: 974 (1996). 2.Kaji H et al JBC 273: 33885 (1998).]3. Shibasaki SY et al Life Sci. 68: 991(2001). 4. McKee KK et al Mol. Endocrinol. 11: 415 (1997). 5. Smith Rg et al Trends Endocrinol. Metabol. 10:128 (1999). 6. Guan XM et al Brain res. Mol. Brain. Res. 48: 128(1997) 7. Kojima M et al Nature 402: 656(1999).

Additional Info

Recognizes rat ghrelin receptor at ~27kD in rat brain. No crossreactivity with type 1b GHS-R. No significant sequence homology exists with other GPCRs. Species sequence homology: mouse, 100%; human, sheep, porcine, 95%.