SR 142948 是一种口服有效的选择性非肽神经紧张素 (NT) 受体拮抗剂。SR 142948 能拮抗NT诱导的 HT 29细胞中肌醇单磷酸酯的形成，其IC50值为 3.9 nM。SR 142948 能阻断由NT诱导的低体温，镇痛以及小鼠转向行为。SR 142948 能透过血脑屏障，可用于精神类疾病的研究。
| 生物活性 | SR 142948 is an orally active, potent and selective non-peptideneurotensin receptor(NT1R) antagonist. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT 29 cells with anIC50of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability, can be used in study of psychiatric disorders[1][2]. |
体外研究
(In Vitro) | SR 142948 (1 μM; 90 min) inhibits expression of c-fos and krox24 in CHO-hNT1-R cells[1].
SR 142948 (0-1 μM; 1 h) 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[2].
SR 142948 (0-1 μM; 30 min) antagonizes production of IP1 stimulated by NT both in h-NTR1-CHO and HT 29 cells, in a concentration-dependent manner[2].
SR 142948 (1, 10 nM; 60-80 s) antagonizes intracellular calcium mobilization stimulated by NT in h-NTR1-CHO cells[2].
Cell Viability Assay[1] | Cell Line: | CHO cells (expressing hNT1-R) | | Concentration: | 1 μM | | Incubation Time: | 90 min | | Result: | Inhibited NT-stimulated expression of c-fos and krox24. |
Cell Viability Assay[2] | Cell Line: | CHO cells (expressing hNT1-R), HT 29 cells | | Concentration: | 0-1 μM | | Incubation Time: | 1 h | | Result: | Inhibited the specific binding of [125I-Tyr3]NT to h-NTR1-CHO and HT 29 cell membranes in a dose-dependent manner (IC50=1.19, 0.32 nM, respectively). |
Cell Viability Assay[2] | Cell Line: | h-NTR1-CHO cells, HT 29 cells | | Concentration: | 0-1 μM | | Incubation Time: | 30 min | | Result: | Antagonized the NT-induced IP1 production and intracellular calcium mobilization, with IC50s of 3.9, 11, and 53 nM for 10, 100 and 1000 nM NT, respectively.(in HT 29 cells).
Inhibited IP1 formation induced by 10 nM NT in h-NTR1-CHO cells with an IC50value of 9.7 nM. |
Cell Viability Assay[2] | Cell Line: | h-NTR1-CHO cells | | Concentration: | 1, 10 nM | | Incubation Time: | 60-80 s (Infuse for 40-60 s and incubate for another 20 s). | | Result: | Abolished the ability of NT to increase free Calcium ions when at 10 nM.
Inhibited the second peak of NT by 65% (S2/S1=0.35; S2/S1=1.12 (blank control)) when concentration at 1 nM. |
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体内研究
(In Vivo) | SR 142948 (2 μg/kg; p.o.; single) inhibits the turning behavior induced by NT (10 pg/mouse)[2].
SR 142948 (0.01, 0.03, 0.3 mg/kg; i.p.; single) prevents the enhancement of ACh release produced by NT (100 nM), in a dose-dependent manner[2].
SR 142948 (0-10 mg/kg; p.o.; single) partially but significantly blocks NT-induced hypothermia (53% at 2 mg/kg in rats and 54% at 4 mg/kg in mice)[2].
| Animal Model: | Female Swiss albino CD1 mice (25-30 g; intrastriatal injection of 10 pg/mouse NT)[2]. | | Dosage: | 2 μg/kg | | Administration: | Oral administration; single. | | Result: | Inhibited the turning behavior with maximal and significant antagonism between 1-2 h after administration. |
| Animal Model: | Male Sprague-Dawley rats (270-320 g; stimulation of 100 nM NT)[2]. | | Dosage: | 0.01, 0.03, 0.3 mg/kg | | Administration: | Intraperitoneal injection; single. | | Result: | Inhibited NT-induced release of ACh, in a dose-dependent manner. |
| Animal Model: | Male OFA rats (130-160 g) and male OFA mice (25-30 g)[2]. | | Dosage: | 0-10 mg/kg | | Administration: | Oral administration; single. | | Result: | Partially but significantly blocked NT-induced hypothermia (53% at 2 mg/kg in rats and 54% at 4 mg/kg in mice). The dose-response relationship was bell-shaped, with disappearance of the effect in both species at doses above 4 mg/kg. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
