neurokinin A (4-10), Tyr(5)-Trp(6,8,9)-Arg(10)-

Product Nameneurokinin A (4-10), Tyr(5)-Trp(6,8,9)-Arg(10)-
CAS126050-12-2
MFC57H68N14O10
MW1109.24
EINECS
MOL File126050-12-2.mol

Chemical Properties

Density	1.477±0.14 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
pka	3.706±0.10(predicted)
form	Solid
color	White to off-white

Usage And Synthesis

Description

MEN 10207 is a tachykinin antagonist.

Uses

MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.

in vivo

but not Substance P in a dose-dependent manner. And MEN 10207 also effectively blocks the long-term reflex facilitation to the gastrocnemius nerve stimulation^[1].

Animal Model:	Decerebrate, spinalized, unanesthetized Female Sprague-Dawley rats (250-280 g)^[1]
Dosage:	7 pmol/10 μL, 70 pmol/10 μL, 700 pmol/10 μL
Administration:	Intrathecal administration; once
Result:	Blocked the reflex facilitation to intrathecal Neurokinin A, but not Substance P in a dose-dependent manner.

IC 50

Tachykinin NK₂ Receptor: 7.9 (pA2); NK1: 5.2 (pA2); NK3: 4.9 (pA2)

References

[1] X J Xu, et al. On the role of NK-2 tachykinin receptors in the mediation of spinal reflex excitability in the rat. Neuroscience. 1991;44(2):483-90. DOI:10.1016/0306-4522(91)90071-u
[2] P Rovero, et al. A highly selective NK-2 tachykinin receptor antagonist containing D-tryptophan. Eur J Pharmacol. 1990 Jan 3;175(1):113-5. DOI:10.1016/0014-2999(90)90161-x
[3] A K Henderson, et al. Demonstration of a neurokinin A receptor subtype in transfected fibroblasts. Eur J Pharmacol. 1992 Feb 13;225(2):175-8. DOI:10.1016/0922-4106(92)90099-h