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| | neurokinin A (4-10), Tyr(5)-Trp(6,8,9)-Arg(10)- Basic information |
| | neurokinin A (4-10), Tyr(5)-Trp(6,8,9)-Arg(10)- Chemical Properties |
| density | 1.477±0.14 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | | pka | 3.706±0.10(predicted) | | form | Solid | | color | White to off-white |
| | neurokinin A (4-10), Tyr(5)-Trp(6,8,9)-Arg(10)- Usage And Synthesis |
| 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 NK2 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 |
| | neurokinin A (4-10), Tyr(5)-Trp(6,8,9)-Arg(10)- Preparation Products And Raw materials |
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