Biological ActivityTripeptide substance P (SP) antagonist (IC50 = 90 μM). Also inhibits binding of SP to Mas-related GPCR (MRGPR) X2. Inhibits SP-induced IgE-independent degranulation of mast cells in vitro. Inhibits compound 48/80-induced MRGPRX2 activation and scratching in mice in vivo.
(Modifications: Gln-1 = N-terminal Boc, Trp-2 = D-Trp (Formyl), Phe-3 = Phe-OBzl)
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Studies on neurokinin antagonists. 1. The design of novel tripeptides possessing the glutaminyl-D-tryptophylphenylalanine sequence as substance P antagonists.
Hagiwara et al.
Dual action of neurokinin-1 antagonists on Mas-related GPCRs.
Azimi et al.
JCI Insight., 2016;1:e89362
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