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MCE 国际站:SR 142948 dihydrochloride
产品活性:SR 142948 dihydrochloride 是一种具有口服活性、选择性的非肽神经降压素受体 (NT) 拮抗剂,在 h-NTR1-CHO 细胞、HT-29 细胞和成年大鼠脑中的 IC50 分别为 1.19 nM、0.32 nM、3.96 nM。SR 142948 dihydrochloride 在 HT-29 细胞中拮抗 NT 诱导的肌醇单磷酸盐形成,IC50 为 3.9 nM。SR 142948 dihydrochloride 在体内阻断 NT 诱导的体温过低、镇痛和转向行为。SR 142948 dihydrochloride 可以透过血脑通透性,可用于精神疾病的研究。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Neurotensin Receptor
In Vitro: SR 142948 (1 µM; 90 min) dihydrochloride inhibits expression of c-fos and krox24 in CHO-hNT1-R cells.
SR 142948 (0-1 µM; 1 h) dihydrochloride exhibits good antagonistic activity by inhibiting [125I-Tyr3]NT binds to h-NTR1-CHO and HT 29 cell membranes, with IC50s of 1.19 and 0.32 nM, respectively.
SR 142948 (0-1 µM; 30 min) dihydrochloride antagonizes production of IP1 stimulated by NT both in h-NTR1-CHO and HT 29 cells, in a concentration-dependent manner.
SR 142948 (1, 10 nM; 60-80 s) dihydrochloride antagonizes intracellular calcium mobilization stimulated by NT in h-NTR1-CHO cells.
In Vivo: SR 142948 (2 µg/kg; p.o.; single) dihydrochloride inhibits the turning behavior induced by NT (10 pg/mouse).
SR 142948 (0.01, 0.03, 0.3 mg/kg; i.p.; single) dihydrochloride prevents the enhancement of ACh release produced by NT (100 nM), in a dose-dependent manner.
SR 142948 (0-10 mg/kg; p.o.; single) dihydrochloride partially but significantly blocks NT-induced hypothermia (53% at 2 mg/kg in rats and 54% at 4 mg/kg in mice).
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