(D-Arg1,D-Phe5,D-Trp7.9,Leu11)-Substance P Ghrelin and Obestatin Catalog

CAS	96736-12-8
Sequence	H-D-Arg-Pro-Lys-Pro-D-Phe-Gln-D-Trp-Phe-D-Trp-Leu-Leu-NH2
Sequence Single	rPKPfQwFwLL-NH2
Molecular Formula	C79H109N19O12
Molecular Weight	1516.86
Synonyms	[DArg1, DPhe5, DTrp7,9, Leu11] Substance P
Technology	Synthetic
Storage	-20°C, avoid light, cool and dry place
Application	Obesity Research
Description	(D-Arg1,D-Phe5,D-Trp7.9,Leu11)-Substance P initially described as a low potency ghrelin receptor antagonist has surprisingly been found to be a full inverse agonist (EC50 = 5.2 nM). In COS-7 cells transiently transfected with the ghrelin receptor the substance P analog rPKPfQwFwLL decreased the constitutive signaling down to levels observed in untransfected cells. Assuming that constitutive signaling of the ghrelin receptor is of physiological relevance in the regulation of appetite control, inverse agonists of the ghrelin receptor could be interesting for the treatment of obesity.
References	1. Novel linear antagonists of the antidiuretic (V2) and vasopressor (V1) responses to vasopressin. M.Manning et al., Int. J. Pept. Protein Res., 32, 455 (1988) 2. Antagonism of ghrelin receptor reduces food intake and body weight gain in mice. A.Asakawa et al., Gut, 52, 947 (2003) 3. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]substance P, a potent bombesin antagonist in murine Swiss 3T3 cells, inhibits the growth of human small cell lung cancer cells in vitro. P.J.Woll and E.Rozengurt, Proc. Natl. Acad. Sci. USA, 85, 1859 (1988) 4. Block of the hyoscine-resistant opiate withdrawal contracture of ileum by a new substance P antagonist [D-Arg1,D-Phe5,D- Trp7,9,Leu 11]substance P. K.Tsou et al., Eur. J. Pharmacol., 110, 155 (1985) 5. [D-Arg1, D-Phe5, D-Trp7,9, Leu11] substance P induces apoptosis in lung cancer cell lines in vitro. J.G.Reeve and N.M.Bleehen, Biochem. Biophys. Res. Commun., 199, 1313 (1994) 6. Metabolism of the anticancer peptide H-Arg-D-Trp-NmePhe-D-Trp-Leu-Met-NH2. D.A.Jones et al., Peptides, 16, 777 (1995) 7. Unexpected effects of peptide and nonpeptide substance P receptor antagonists on basal prolactin and growth hormone release in vitro. P.Heinz-Erian et al., Gastroenterology, 90, 1455 (1986) 8. High constitutive signaling of the ghrelin receptor--identification of a potent inverse agonist. H.Houben and C.Denef, Peptides, 14, 109 (1993)

PeptideDB

(D-Arg1,D-Phe5,D-Trp7.9,Leu11)-Substance P

CAS No.: 96736-12-8