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 NK
2 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
