[Sar9,Met(O2)11]-Substance P 是一种选择性的速激肽 NK1 受体激动剂。
[Sar9,Met(O2)11]-Substance P Chemical Structure
CAS No. : 110880-55-2
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[Sar9,Met(O2)11]-Substance P 相关产品
bull;相关化合物库:
Bioactive Compound Library Plus
Peptide Library
生物活性
[Sar9,Met(O2)11]-Substance P is a tachykinin NK1 receptor selective agonist.
IC50 Target
NK1 receptor[1]
体外研究 (In Vitro)
[Sar9,Met(O2)11]-Substance P and septide (10-100 pmol per rat, i.c.v.) are equipotent in increasing mean arterial blood pressure (MAP) and heart rate (HR), yet they have dissimilar time-course. Both agonists increase dose-dependently face washing and sniffing while [Sar9,Met(O2)11]-Substance P is the sole to produce grooming[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
[1]. Cellier E, et al. Characterization of central and peripheral effects of septide with the use of five tachykinin NK1 receptor antagonists in the rat. Br J Pharmacol. 1999 Jun;127(3):717-28.
Kinase Assay [1]
Rats initially receive an i.c.v. injection of artificial cerebrospinal fluid (aCSF; 1 μl) followed 60 min later by a single dose of either [Sar9,Met(O2)11]-Substance P (10 pmol (n=9), 25 pmol (n=9), 65 pmol (n=8) or 100 pmol (n=8)) or septide (10 pmol (n=12), 25 pmol (n=9), 65 pmol (n=6) or 100 pmol (n=6)) to construct a complete dose-response curve. Each rat is selected randomly and injected with only one of the two agonists for the remainder of the protocol. Increasing doses of [Sar9,Met(O2)11]-Substance P or septide are given at 24 h intervals on day 1 (10 pmol), day 2 (25 pmol), day 3 (65 pmol) and day 4 (100 pmol). Control rats (n=18) receive only the vehicle (aCSF) each day of experiment. Peptides are administered in a volume of 1 μL of vehicle followed by 5 μL flush volume of aCSF which corresponds to the void volume of the catheter. Each dose is calculated per rat in 1 μL solution[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Cellier E, et al. Characterization of central and peripheral effects of septide with the use of five tachykinin NK1 receptor antagonists in the rat. Br J Pharmacol. 1999 Jun;127(3):717-28.