Product Name :
[DArg1, DPhe5, DTrp7, 9, Leu11] Substance P
CAS NO. :
96736-12-8
Formula :
C79H109N19O12
Molecular Weight::
1516.83
Target:
Serial Number:
DArg-Pro-Lys-Pro-DPhe-Gln-DTrp-Phe-DTrp-Leu-Leu-NH2
Short serial number :
rPKPfQwFwLL-NH2
Purity:
95%
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. 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.
References:
[1]. 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. [2]. [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. [3]. Unexpected effects of peptide and nonpeptide substance P receptor antagonists on basal prolactin and growth hormone release in vitro.
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