MEN 10376
Biological Activity
MEN 10376 is a potent and selective NK2 receptor antagonist (pA2 = 8.08, rabbit pulmonary artery). Displays > 250-fold selectivity over NK1 (pA2 = 5.66, guinea pig ileum) and NK3 (Ki > 10 mM, guinea pig brain). Active in vivo.Technical Data
(Modifications: Trp-3, Trp-5, Trp-6 = D-Trp, Lys-7 = C-terminal amide)
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Tachykininergic transmission to the circular muscle of the guinea-pig ileum: evidence for the involvement of NK2 receptors.
Bartho et al.
Br.J.Pharmacol., 1992;105:805 -
In vivo evidence for tachykininergic transmission using a new NK-2 receptor-selective antagonist, MEN 10,376.
Maggi et al.
J.Pharmacol.Exp.Ther., 1991;257:1172 -
Pharmacological evidence of tachykinin-induced intracellular calcium rise in a human NK2 receptor transfected cell line.
Subramanian et al.
Biochem.Biophys.Res.Commun., 1994;200:1512
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