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

Modify Date: 2024-01-06 19:45:47

neurokinin A (4-10), Tyr(5)-Trp(6,8,9)-Arg(10)- Structure
neurokinin A (4-10), Tyr(5)-Trp(6,8,9)-Arg(10)- structure
Common Name neurokinin A (4-10), Tyr(5)-Trp(6,8,9)-Arg(10)-
CAS Number 126050-12-2 Molecular Weight 1109.238
Density 1.5±0.1 g/cm3 Boiling Point N/A
Molecular Formula C57H68N14O10 Melting Point N/A
MSDS N/A Flash Point N/A

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


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].

 Names

Name [TYR5,D-TRP6,8,9, ARG10]-NEUROKININ A(4-10)
Synonym More Synonyms

  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
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

 Synonyms

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)