Talnetant (SB 223412) 是一种选择性、竞争性、脑渗透性的NK3受体拮抗剂，在 hNK-3-CHO 细胞中Ki为 1.4 nM。 相对于 hNK-2 受体，Talnetant 对于 hNK-3 有 100 倍的选择性，对 hNK-1 无亲和性。Talnetant 可用于精神分裂症的相关研究。
| 生物活性 | Talnetant (SB 223412) is a selective, competitive, brain-permeableNK3receptor antagonist with aKiof 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies[1][2][3]. |
体外研究
(In Vitro) | Talnetant (SB 223412) (0.1-1 μM) can reduce the accumulation of NKB-induced IP in U-2OS cells expressing the human NK3 receptor[3].
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体内研究
(In Vivo) | Talnetant (SB 223412) (0.5-2 mg/kg iv, 2min pretreatment) can inhibit the miosis induced by senktide (25μg, iv) in a dose-dependent manner with an ED50of 0.44mg/kg in conscious rabbits[1].
Talnetant (SB 223412) (i.p., 1-100 mg/kg, 1 h) can significantly attenuate senktide-induced "wet dog wagging" behavior in a dose-dependent manner, significantly increase extracellular dopamine and norepinephrine in the medial prefrontal cortex and reduce haloperidol-induced increases in dopamine levels in the vomeronasal nucleus of freely moving guinea pigs[3].
| Animal Model: | Male Dunkin-Hartley guinea pig[3] | | Dosage: | 1, 3, 10, 30 or 100 mg/kg | | Administration: | Intraperitoneal injection; 1 h | | Result: | Showed a significant attenuation of wet dog shake (WDS) behavior from 31.1 to 16.7 at 30 mg/kg.
Significantly increased extracellular DA levels to 238% and NE levels to 227.1%, without affecting 5-HT levels. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(261.47 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.6147 mL | 13.0736 mL | 26.1472 mL | | 5 mM | 0.5229 mL | 2.6147 mL | 5.2294 mL | | 10 mM | 0.2615 mL | 1.3074 mL | 2.6147 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.54 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.54 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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