[Sar9, Met(O2)11]-Substance P (trifluoroacetate salt)

[Sar9, Met(O2)11]-Substance P (Sar-SP) is a peptide agonist of the neurokinin-1 (NK1) receptor.1 It is selective for NK1 over NK2 and NK3 receptors. Sar-SP induces inositol phosphate formation in U373MG glioblastoma cells with an EC50 value of 3.8 nM, an effect that can be blocked by the NK1 receptor antagonist SR 140333.2 It induces contractions in isolated human bronchi when used at concentrations of 3, 100, and 1,000 nM.3 Sar-SP (10, 25, 65, and 100 pmol/animal, i.c.v.) increases mean arterial pressure and heart rate in conscious rats.4WARNING This product is not for human or veterinary use.

[1] D REGOLI. New selective agonists for neurokinin receptors: pharmacological tools for receptor characterization.[J]. Trends in pharmacological sciences, 1988, 9 8: 290-295. DOI: 10.1016/0165-6147(88)90013-2
[2] F. OURY-DONAT. SR 140333, a Novel, Selective, and Potent Nonpeptide Antagonist of the NK1 Tachykinin Receptor: Characterization on the U373MG Cell Line[J]. Journal of Neurochemistry, 1994, 62 4: 1399-1407. DOI: 10.1046/j.1471-4159.1994.62041399.x
[3] ERIC BARCHASZ . Interleukin-1β-induced hyperresponsiveness to [Sar9,Met(O2)11]substance P in isolated human bronchi[J]. European journal of pharmacology, 1999, 379 1: Pages 87-95. DOI: 10.1016/s0014-2999(99)00484-7
[4] ERIC CELLIER. Characterization of central and peripheral effects of septide with the use of five tachykinin NK1 receptor antagonists in the rat[J]. British Journal of Pharmacology, 2009, 127 3: 717-728. DOI: 10.1038/sj.bjp.0702620