NNC 05-2090 hydrochloride是一种GABA摄取抑制剂，对BGT-1（mGAT-2）转运体具有选择性。
Cas No.:184845-18-9
Sample solution is provided at 25 µL, 10mM.
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NNC 05-2090 hydrochloride is a GABA uptake inhibitor selective for the BGT-1 (mGAT-2) transporter[1]. NNC 05-2090 hydrochloride can be used for research related to epilepsy and neurological diseases[2-3].
In vitro, NNC 05-2090 hydrochloride (1.25–20μM) treated primary hepatocytes for 15 minutes, followed by stimulation with TNF-α (20ng/ml)/ActD (200ng/ml) for 24 hours. NNC 05-2090 hydrochloride inhibited TNF-α-mediated hepatocyte apoptosis and upregulated the expression of the anti-apoptotic gene c-Met[4]. NNC 05-2090 hydrochloride (50–150μM) treated rat astrocytes and HepG2 cells for 1 hour. NNC 05-2090 hydrochloride inhibited betaine transport through BGT1 and reversed the osmoprotective effect of betaine against cell shrinkage under hypertonic conditions[5].
In vivo, NNC 05-2090 hydrochloride (8mg/kg) was administered intraperitoneally to mice 1 hour after intracerebroventricular injection of Aβ25-35. NNC 05-2090 hydrochloride significantly attenuated the preventive effect of betaine on Aβ25-35-induced cognitive impairment but did not affect betaine's inhibition of brain oxidative stress[6]. NNC 05-2090 hydrochloride (0–242μmol/kg) was administered intraperitoneally to DBA/2 mice 1 hour before acoustic stimulation. NNC 05-2090 hydrochloride dose-dependently antagonized sound-induced tonic and clonic convulsions[7].
References:
[1] Jinzenji A, Sogawa C, Miyawaki T, et al. Antiallodynic action of 1-(3-(9H-Carbazol-9-yl)-1-propyl)-4-(2-methyoxyphenyl)-4-piperidinol (NNC05-2090), a betaine/GABA transporter inhibitor. J Pharmacol Sci. 2014;125(2):217-26.
[2] Thomsen C, Sørensen PO, Egebjerg J. 1-(3-(9H-carbazol-9-yl)-1-propyl)-4-(2-methoxyphenyl)-4-piperidinol, a novel subtype selective inhibitor of the mouse type II GABA-transporter. Br J Pharmacol. 1997 Mar;120(6):983-5.
[3] Kunisawa K, Kido K, Nakashima N, et al. Betaine attenuates memory impairment after water-immersion restraint stress and is regulated by the GABAergic neuronal system in the hippocampus. Eur J Pharmacol. 2017 Feb 5;796:122-130.
[4] Liu Z, Li Q, Shen R, Ci L, et al. Betaine/GABA transporter-1 (BGT-1) deficiency in mouse prevents acute liver failure in vivo and hepatocytes apoptosis in vitro. Biochim Biophys Acta Mol Basis Dis. 2020 Mar 1;1866(3):165634.
[5] Pukale DD, Farrag M, Gudneppanavar R, et al. Osmoregulatory Role of Betaine and Betaine/γ-Aminobutyric Acid Transporter 1 in Post-Traumatic Syringomyelia. ACS Chem Neurosci. 2021 Oct 6;12(19):3567-3578.
[6] Ibi D, Tsuchihashi A, Nomura T, et al. Involvement of GAT2/BGT-1 in the preventive effects of betaine on cognitive impairment and brain oxidative stress in amyloid β peptide-injected mice. Eur J Pharmacol. 2019 Jan 5;842:57-63.
[7] Dalby NO, Thomsen C, Fink-Jensen A, et al. Anticonvulsant properties of two GABA uptake inhibitors NNC 05-2045 and NNC 05-2090, not acting preferentially on GAT-1. Epilepsy Res. 1997 Jul;28(1):51-61.
NNC 05-2090 hydrochloride是一种GABA摄取抑制剂，对BGT-1（mGAT-2）转运体具有选择性[1]。NNC 05-2090 hydrochloride可用于癫痫和神经系统疾病的相关研究[2-3]。
在体外，NNC 05-2090 hydrochloride（1.25–20μM））处理原代肝细胞15分钟，随后以TNF-α（20ng/ml）/ActD（200ng/ml）刺激24小时。NNC 05-2090 hydrochloride可抑制TNF-α介导的肝细胞凋亡，并上调抗凋亡基因c-Met的表达[4]。NNC 05-2090 hydrochloride（50–150μM）处理大鼠星形胶质细胞及HepG2细胞1小时。NNC 05-2090 hydrochloride可抑制甜菜碱通过BGT1的转运，同时逆转甜菜碱在高渗条件下对细胞皱缩的保护作用[5]。
在体内，NNC 05-2090 hydrochloride（8mg/kg）在Aβ25-35侧脑室注射后1小时腹腔注射处理小鼠。NNC 05-2090 hydrochloride显著减弱了甜菜碱对Aβ25-35诱导的认知障碍的预防作用，但不影响甜菜碱对大脑氧化应激的抑制作用[6]。NNC 05-2090 hydrochloride（0–242μmol/kg）在声刺激前1小时腹腔注射于DBA/2小鼠。NNC 05-2090 hydrochloride以剂量依赖性地拮抗了声音诱发的强直性和阵挛性惊厥[7]。
| Cell experiment [1]: | |
Cell lines | Rat astrocytes (DI TNC1) and HepG2 cells (human liver hepatocellular carcinoma cell line) |
Preparation Method | Cells were cultured and then pre-incubated with hypertonic media overnight. Cells were then treated with different concentrations of the BGT1 inhibitor NNC 05-2090 (50–150µM) for 1 hour, followed by the addition of betaine (100µM). |
Reaction Conditions | 50–150µM; 1h. |
Applications | NNC 05-2090 hydrochloride significantly inhibited betaine transport through BGT1 in a concentration-dependent manner, showing the highest activity against BGT1. NNC 05-2090 hydrochloride also reversed the osmoprotective effect of betaine, abrogating betaine-mediated reduction in cell shrinkage under hypertonic conditions. |
| Animal experiment [2]: | |
Animal models | DBA/2 mice, NMRI mice, Amygdala-kindled rats |
Preparation Method | Animals received intraperitoneal (i.p.) administration of NNC 05-2090 hydrochloride (0-242μmol/kg). Seizure tests (sound-induced seizures or maximal electroshock) were conducted at specified times (1 hour) after drug injection. |
Dosage form | 19-242μmol/kg; i.p.; single injection. |
Applications | NNC 05-2090 hydrochloride dose-dependently antagonized sound-induced tonic and clonic convulsions in DBA/2 mice and tonic hindlimb extension in the maximal electroshock (MES) test in mice. In amygdala-kindled rats, NNC 05-2090 hydrochloride significantly reduced generalized seizure severity at the highest tested doses. |
References: | |
| Cas No. | 184845-18-9 | SDF | |
| 化学名 | 1-(3-(9H-carbazol-9-yl)propyl)-4-(2-methoxyphenyl)piperidin-4-ol hydrochloride | ||
| Canonical SMILES | COC1=CC=CC=C1C(CC2)(O)CCN2CCCN3C4=CC=CC=C4C5=CC=CC=C53.Cl | ||
| 分子式 | C27H30N2O2.HCl | 分子量 | 451.01 |
| 溶解度 | <5.64mg/ml in ethanol; <45.1mg/ml in DMSO | 储存条件 | Desiccate at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2172 mL | 11.0862 mL | 22.1725 mL |
| 5 mM | 443.4 μL | 2.2172 mL | 4.4345 mL |
| 10 mM | 221.7 μL | 1.1086 mL | 2.2172 mL |
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