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

Names

[ Name ]:
neurokinin A (4-10), Tyr(5)-Trp(6,8,9)-Arg(10)-

[Synonym ]:
neurokinin A (4-10), Tyr(5)-Trp(6,8,9)-Arg(10)-
5-Tyr-6,8,9-Trp-10-Arg-NKA (4-10)
5-Tyr-6,8,9-Trp-10-Arg-neurokinin A (4-10)

Biological Activity

[Description]:

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[1][2].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor

[Target]

Tachykinin NK2 Receptor:7.9 (pA2)

NK1:5.2 (pA2)

NK3:4.9 (pA2)

[In Vitro]

In competitive radioligand binding assays, MEN 10207 (the IC50 ranges of 21-54 nM) has high affinity in bovine stomach membranes and SKLKB82#3 cells, a murine fibroblast cell line transfected with a cDNA encoding for the bovine NK2 receptor[3].

[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.

[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.

[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.

[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.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C₅₇H₆₈N₁₄O₁₀

[ Molecular Weight ]:
1109.238

[ Exact Mass ]:
1108.524292

[ LogP ]:
3.11

[ Index of Refraction ]:
1.711

Related Compounds

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