Pozanicline
Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [3H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction.
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- CAS 番号: 161417-03-4
- 分子式: C11H16N2O
- 分子量:192.26
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
Ki: 16 nM (α4β2* nAChR)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| IMR-32 | EC50 |
150 μM
Compound: S-4 (ABT-089)
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Concentration required to elicit ganglionic receptors measured using [86Rb+] flux functional assay in a human neuroblastoma-derived IMR-32 cell line
Concentration required to elicit ganglionic receptors measured using [86Rb+] flux functional assay in a human neuroblastoma-derived IMR-32 cell line
|
[PMID: 9022806] |
化学情報
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CAS 番号 161417-03-4
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分子量 192.26
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分子式 C11H16N2O
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SMILES
CC1=C(OC[C@H]2NCCC2)C=CC=N1
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別名
ABT-089
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Sullivan JP, et al. ABT-089 [2-methyl-3-(2-(S)-pyrrolidinylmethoxy)pyridine]: I. A potent and selective cholinergic channel modulator with neuroprotective properties. J Pharmacol Exp Ther. 1997 Oct;283(1):235-46. [Content Brief]
[2]. Yildirim E, et al. ABT-089, but not ABT-107, ameliorates nicotine withdrawal-induced cognitive deficits in C57BL6/J mice. Behav Pharmacol. 2015 Apr;26(3):241-8. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)