产品
编 号:F099920
分子式:C57H68N14O10
分子量:1109.24
产品类型
结构图
CAS No: 126050-12-2
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产品详情
生物活性:
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.
体内研究:
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.Animal Model:Decerebrate, spinalized, unanesthetized Female Sprague-Dawley rats (250-280 g)
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.
体外研究:
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.