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Cebranopadol

Cebranopadol

产品编号 T5167   CAS 863513-91-1
别名: 西博帕多, GRT6005

Cebranopadol (GRT6005) 是镇痛 NOP 和阿片受体激动剂,对人 NOP、μ-阿片 (MOP)、κ-阿片 (KOP) 和 δ-阿片 (DOP) 受体的 Ki 值分别为 0.9、0.7、2.6 和 18 nM。

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Cebranopadol Chemical Structure
Cebranopadol, CAS 863513-91-1
规格 价格/CNY 货期 数量
1 mg ¥ 473 现货
2 mg ¥ 692 现货
5 mg ¥ 1,160 现货
10 mg ¥ 1,870 现货
25 mg ¥ 3,460 现货
50 mg ¥ 5,180 现货
100 mg ¥ 7,130 现货
200 mg ¥ 9,630 现货
1 mL * 10 mM (in DMSO) ¥ 1,280 现货
其他形式的 Cebranopadol:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: Cebranopadol (T5167)
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纯度: 99.86%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Cebranopadol (GRT6005) is an analgesic NOP and opioid receptor agonist with Kis of 0.9 nM, 0.7 nM, 2.6 nM, 18 nM for human NOP, μ-opioid (MOP), κ-opioid (KOP) and δ-opioid (DOP) receptor, respectively.
靶点活性 μ opioid receptor:1.2 nM (EC50, cell free), NOP:13 nM (EC50, cell free), δ opioid receptor:110 nM (EC50, cell free), κ opioid receptor:17 nM (EC50, cell free)
体外活性 Cebranopadol showed full agonistic efficacy at the human MOP and DOP receptors, almost full efficacy at the human NOP receptor, and partial efficacy at the human KOP receptor. In a functional [35S]GTPgS binding assay with membranes expressing the human 5-HT5A receptor, cebranopadol did not show agonistic or signirficant antagonistic effects at concentrations up to 10.0 μM [1].
体内活性 Cebranopadol exhibits highly potent and efficacious antinociceptive and antihypersensitive effects in several rat models of acute and chronic pain with ED50 values of 0.5-5.6 μg/kg after intravenous and 25.1 μg/kg after oral administration. Cebranopadol's duration of action is long (up to 7 hours after intravenous 12 μg/kg; >9 hours after oral 55 μg/kg in the rat tail-flick test) [1]. In streptozotocin (STZ)-treated rats, cebranopadol (i.pl.) reduced mechanical hypersensitivity in the ipsilateral paw but had no effect at the contralateral paw. In CCI rats, cebranopadol (i.pl.) showed antiallodynic activity at the ipsilateral paw. After administration to the contralateral paw, cebranopadol also showed ipsilateral antiallodynic activity, but with reduced potency and delayed onset. In diabetic mice, cebranopadol i.th. and i.c.v. decreased heat hyperalgesia with full efficacy and similar potency for both routes [2]. In NOP(-/-) mice morphine treatment produced the same signs of withdrawal as in NOP(+/+) animals, while cebranopadol treatment elicited a stronger withdrawal syndrome in NOP(-/-) than of NOP(+/+) mice [3].
激酶实验 Rat MOP, KOP, and NOP receptor binding assays were run using membrane suspensions from rat brain without the cerebellum for MOP receptors; without the pons, medulla oblongata, and cerebellum for NOP receptors; and without the pons, medulla oblongata, cerebellum, and cortex for KOP receptors and the following tritium-labeled radioligands: [3H]DAMGO in the MOP receptor assay, [3H]nociceptin in the NOP receptor assay, and [3H]Ci-977 in the KOP receptor assay. The assay buffer used for the binding studies was 50 mM Tris-HCl (pH 7.4) supplemented with 0.05% sodium azide. The final assay volume of 250 μl/well included 2 nM [3H]DAMGO, 1 nM [3H]nociceptin, or 1 nM [3H]Ci-977 as a ligand in the MOP, NOP, or KOP receptor assays, respectively, and cebranopadol in dilution series. Cebranopadol was diluted with 25% DMSO in water to yield a final 0.5% DMSO concentration, which also served as a respective vehicle control. The assays were started by the addition of the membrane suspensions and, after short mixing, the assays were run for 90 minutes at room temperature. All incubations were run in triplicate and terminated by rapid filtration under mild vacuum and two washes of 5 ml of buffer using FP-100 Whatman GF/B filter mats. The radioactivity of the samples was counted after a stabilization and extraction period of at least 15 hours by use of the scintillation fluid Ready Protein; the complete competition curves for cebranopadol were recorded [1].
动物实验 The pharmacokinetic properties of cebranopadol in rats were investigated after a single intravenous dose of 160 μg/kg cebranopadol. The intravenous dose was administered as a bolus in a volume of 2 ml/kg with a catheter in the vena femoralis. Blood samples (200 μl/sample) were withdrawn via an implanted arterial catheter (arteria carotis) by an automated blood sampling system at the following sampling times: 0 (predose), 5, 15, 30, 60, 180, 360, 720, and 1440 minutes after administration. Blood samples were centrifuged, and plasma was separated. Plasma concentrations of cebranopadol were determined using a validated liquid chromatography-tandem mass spectrometry method. The lower limit of quantification for cebranopadol in this method was 0.05 ng/ml using a sample volume of 50 μl of plasma [1].
别名 西博帕多, GRT6005
分子量 378.48
分子式 C24H27FN2O
CAS No. 863513-91-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 6 mg/mL

H2O: Insoluble

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TargetMol Library Books参考文献

1. Linz K, et al. Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist. J Pharmacol Exp Ther. 2014 Jun;349(3):535-48. 2. Tzschentke TM, et al. Antihyperalgesic, Antiallodynic, and Antinociceptive Effects of Cebranopadol, a Novel Potent Nociceptin/Orphanin FQ and Opioid Receptor Agonist, after Peripheral and Central Administration in Rodent Models of Neuropathic Pain. Pain Pract. 2017 Nov;17(8):1032-1041. 3. Ruzza C, et al. NOP agonist action of cebranopadol counteracts its liability to promote physical dependence. Peptides. 2019 Feb;112:101-105.
Amentoflavone Deltorphin 2 μ opioid receptor agonist 3 beta-Neoendorphin acetate(77739-21-0 free base) ZT 52656A hydrochloride Mu opioid receptor antagonist 7 Ac-RYYRIK-NH2 acetate GSK1521498 free base

相关化合物库

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药物功能重定位化合物库 抗癌临床化合物库 抗癌药物库 GPCR靶点分子库 神经退行性疾病化合物库 ReFRAME 相关化合物库 临床前化合物库 神经信号分子库 神经递质受体化合物库 临床期小分子药物库

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Keywords

Cebranopadol 863513-91-1 Endocrinology/Hormones GPCR/G Protein Neuroscience Opioid Receptor Inhibitor inhibit 西博帕多 GRT-6005 GRT 6005 GRT6005 inhibitor

 

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