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Submit ReviewABT 089 dihydrochloride is a high affinity and selective α4β2 partial agonist (Ki = 16 nM). Exhibits >1000-fold and >10,000-fold selectivity for α4β2 over α1β1γ1 and α7 receptors respectively. Neuroprotective against glutamate-induced toxicity in rat cortical neurons in vitro. Enhances cognitive performance in vivo. Orally bioavailable and brain penetrant.
分子量 | 265.18 |
公式 | C11H16N2O.2HCl |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 161416-61-1 |
PubChem ID | 23729426 |
InChI Key | UGVSESCRKJTJAK-XRIOVQLTSA-N |
Smiles | CC1=NC=CC=C1OC[C@H]2NCCC2.Cl.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 26.52 | 100 | |
DMSO | 5.3 | 20 |
以下数据基于产品分子量 265.18。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.77 mL | 18.86 mL | 37.71 mL |
5 mM | 0.75 mL | 3.77 mL | 7.54 mL |
10 mM | 0.38 mL | 1.89 mL | 3.77 mL |
50 mM | 0.08 mL | 0.38 mL | 0.75 mL |
参考文献是支持产品生物活性的出版物。
Rueter et al (2004) ABT-089: pharmacological properties of a neuronal nicotinic acetylcholine receptor agonist for the potential treatment of cognitive disorders. CNS Drug Rev. 10 167 PMID: 15179445
Sullivan et al (1997) ABT-089 [2-methyl-3-(2-(S)-pyrrolidinylmethoxy)pyridine]: I. A potent and selective cholinergic channel modulator with neuroprotective properties. J.Pharmacol.Exp.Ther. 283 235 PMID: 9336329
Decker et al (1997) ABT-089 [2-methyl-3-(2-(S)-pyrrolidinylmethoxy)pyridine dihydrochloride]: II. A novel cholinergic channel modulator with effects on cognitive performance in rats and monkeys. J.Pharmacol.Exp.Ther. 283 247 PMID: 9336330
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