(Tyr5,D-Trp6.8.9,Lys-NH2¹⁰)-Neurokinin A (4-10)

Names

[ Name ]:
(Tyr5,D-Trp6.8.9,Lys-NH2¹⁰)-Neurokinin A (4-10)

[Synonym ]:
L-Asp-L-Tyr-D-Trp-L-Val-D-Trp-D-Trp-L-Lys-NH2
NK2 TACHYKININ RECEPT
M.W. 1081.24 C57H68N12O10
(TYR5,D-TRP6·8·9,LYS-NH210)-NEUROKININ A (4-10)
Men 10376

Biological Activity

[Description]:

Men 10376 is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor.

[Related Catalog]:

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

Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor

Peptides

Research Areas >> Others

[Target]

Ki: 4.4 μM (NK-2 receptor, rat small intestine)[1]

[In Vitro]

Men 10376 is a selective tachykinin NK-2 receptor, with a Ki of 4.4 μM, and shows low selectivity for NK-1 and NK-3 receptors (Ki, >10 μM)[1]. Men 10376 shows pA2s of 5.66 and 8.08 for NK-1 (guinea-pig ileum) and NK-2 receptors (endothelium-deprived rabbit pulmonary artery). Men 10376 shows no effect on NK-3 receptor (Ki, >10 μM)[2].

[In Vivo]

Men 10376 (1 and 3 μmol/kg) antagonizes increase in bladder motility produced by the NK-2 receptor agonist in rats[2].

[References]

[1]. Quartara L, et al. N-terminal truncated analogs of men 10376 as tachykinin NK-2 receptor antagonists. Life Sci. 1992;51(25):1929-36.

[2]. Maggi CA, et al. In vivo evidence for tachykininergic transmission using a new NK-2 receptor-selective antagonist, MEN 10,376. J Pharmacol Exp Ther. 1991 Jun;257(3):1172-8.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.361 g/cm3

[ Boiling Point ]:
1555.4ºC at 760 mmHg

[ Molecular Formula ]:
C₅₇H₆₈N₁₂O₁₀

[ Molecular Weight ]:
1081.22000

[ Flash Point ]:
894.5ºC

[ Exact Mass ]:
1080.52000

[ PSA ]:
374.63000

[ LogP ]:
6.53410

[ Vapour Pressure ]:
0mmHg at 25°C

[ Index of Refraction ]:
1.672

[ Storage condition ]:
-20°C

[ Water Solubility ]:
Insuluble (2.3E-3 g/L) (25 ºC)

MSDS

Click to get detail MSDS

Safety Information

[ Hazard Codes ]:
N

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3.0

Articles

Effects of substance P on identified neurons of the rat dorsal motor nucleus of the vagus.

Am. J. Physiol. Gastrointest. Liver Physiol. 281(1) , G164-72, (2001)

Previous evidence suggests that substance P (SP) activates subpopulations of neurons within the dorsal motor nucleus of the vagus (DMV). In this study we aimed at identifying these subpopulations in r...

Neurokinin receptors modulate the impact of uncontrollable stimulation on adaptive spinal plasticity.

Behav. Neurosci. 121(5) , 1082-94, (2007)

Previous research has demonstrated that spinally transected rats can acquire a prolonged flexion response to prevent the delivery of shock. However, rats that receive shock irrespective of leg positio...

Intrathecal administration of neurokinin 1 and neurokinin 2 receptor antagonists undermines the savings effect in spinal rats seen in an instrumental learning paradigm.

Behav. Neurosci. 121(1) , 186-99, (2007)

Research has demonstrated that the isolated spinal cord is capable of modifying its behavior in response to changes in environmental stimuli. Previous studies have shown that rats with complete thorac...

Related Compounds

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