2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. Rivanicline oxalate

Rivanicline oxalate  (Synonyms: RJR-2403 oxalate; (E)-Metanicotine oxalate)

目录号: HY-13225
产品使用指南 技术支持

Rivanicline (RJR-2403) oxalate 是一种神经元型烟碱受体(neuronal nicotinic receptor) 激动剂。Rivanicline oxalate 对大鼠大脑皮层的 nAChR (Ki = 26 nM，EC50 为 732 nM) 和 α4β2 亚型(Ki = 26 nM，EC50 为 16 μM) 具有高度选择性。Rivanicline oxalate 能够显著恢复学习障碍和认知功能障碍。Rivanicline oxalate 可用于研究神经退行性疾病 (如精神分裂症或阿尔茨海默病)。

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Rivanicline oxalate

Rivanicline oxalate Chemical Structure

CAS No. : 220662-95-3

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Rivanicline oxalate 的其他形式现货产品:

Other Forms of Rivanicline oxalate:

Rivanicline oxalate 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Rivanicline (RJR-2403) oxalate is a neuronal nicotinic receptor agonist. Rivanicline oxalate is highly selective for the rat brain cortex nAChRs (Ki = 26 nM, EC50 of 732 nM) and α4β2 subtype (Ki = 26 nM, EC50 = 16 μM). Rivanicline oxalate can significantly restore the learning impairment and cognitive dysfunction. Rivanicline oxalate can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease)[1][2][3][4][5].

IC50 & Target[3]

α4β2

16 μM (EC50)

α4β4

50 μM (EC50)

α3β2

150 μM (EC50)

α7

240 μM (EC50)

α3β2α5

360 μM (EC50)

α3β4

NA μM (EC50)

体内研究
(In Vivo)

Rivanicline oxalate (75-125 µmol/kg, s.c., 单次给药) 能在小鼠生理测试组合模型中引起体温、呼吸频率、Y迷宫活动和听觉惊吓反应的下降，但效力显著低于尼古丁[2]。
Rivanicline oxalate (0-1.2 µmol/kg, s.c., 单次给药) 显著改善了东莨菪碱 (HY-N0296) 所致遗忘后的被动回避记忆保持，并增强了前脑胆碱能投射系统受损大鼠在八臂放射状迷宫模型中的工作记忆和参考记忆[2]。
Rivanicline oxalate (2 mg/kg, i.p., 单次给药) 在眨眼条件反射功能受损的模型中，恢复了小鼠的学习能力[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Scopolamine (1.3 μmol/kg)-induced passive amnesia model established in male wistar rats (200-220 g)[2]
Dosage: 0.06, 0.6, 6 µmol/kg
Administration: Subcutaneous Injections (s.c.), 30 min before testing
Result: Reversed scopolamine-induced amnesia, increasing step-through latency at 0.6 µmol/kg.
No effect at 0.06 or 6 µmol/kg.
Animal Model: Ibotenic acid lesion radial arm maze model established in male Sprague-Dawley rats (250–270 g) [2]
Dosage: 0, 0.3, 0.6, 0.9, 1.2 µmol/kg
Administration: Subcutaneous Injections (s.c.), 20 min before testing
Result: Improved working memory (place task) in lesioned rats.
Animal Model: Physiological test battery model established in C57BL/6 mice[2]
Dosage: 75, 100 and 125 µmol/kg
Administration: Subcutaneous Injections (s.c.), single dose
Result: Was 15-50x less potent than nicotine in reducing body temperature, respiration, and locomotor activity.
Animal Model: MK-801 (0.02 mg/kg)-induced impairment of eyeblink conditioning model established in C57Bl/6 mice (3-5 months)[4]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Rescues learning by activating presynaptic nAChRs to enhance glutamate release.
分子量

252.27

Formula

C12H16N2O4
CAS 号
中文名称

(E)-位变异烟碱草酸盐
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.
纯度 & 产品资料
参考文献

Rivanicline oxalate 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rivanicline220662-95-3RJR-2403(E)-Metanicotine(E)-位变异烟碱草酸盐RJR2403RJR 2403nAChRNicotinic acetylcholine receptorsHippocampusEyeblinkClassical conditioningNMDA receptorsNicotinic receptorsPaired-pulse facilitationMiceInhibitorinhibitorinhibit

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