Return to Previous Page
Details
(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. So, Asakawa et al. found that peripherally administered H-6395 decreased food intake in lean mice, in mice with diet induced obesity, and in ob/ob obese mice.
Catalog Number
H-6935
APC Number
70-9-18
One Letter Code
rPKPfQwFwLL-NH₂
Synonyms
[DArg1, DPhe5, DTrp7,9, Leu11] Substance P
Molecular Formula
C₇₉H₁₀₉N₁₉O₁₂
Relative Molecular Mass
1516.86
CAS Registry Number
96736-12-8
Source
Synthetic
Storage Conditions
-20 ± 5 °C
Keywords
Inverse agonist of ghrelin
Application
Obesity Research
Links / Documents:
Brochures:
Bachem product citations
Product citations
P.Heinz-Erian et al.,
Gastroenterology,
90,
1455 (1986)