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Xanthoplanine

目录号: PC-42912

Xanthoplanine fully inhibits the EC(50) ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC(50) values of 9+/-3 microM (alpha7) and 5+/-0.8 microM (alpha4beta2).

CAS NO.:6872-88-4

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规格 价格 库存
2mg 4500.00 10-20工作日
5mg 7800.00 10-20工作日

基本信息

Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers.[Pubmed: 17391965]

METHODS AND RESULTS:
(S)-Aporphine metho salts with the 1,2,9,10 oxygenation pattern displaced radioligands from recombinant human alpha7 and alpha4beta2 neuronal nicotinic acetylcholine receptors (nAChR) at low micromolar concentrations. The affinity of the nonphenolic glaucine methiodide (4) (vs [(3)H]cytisine) was the lowest at alpha4beta2 nAChR (K(i)=10 microM), and predicentrine methiodide (2) and Xanthoplanine iodide (3), with free hydroxyl groups at C-2 or C-9, respectively, had the highest affinity at these receptors (K(i) approximately 1 microM), while the affinity of the diphenolic boldine methiodide (1) was intermediate between these values. At homomeric alpha7 nAChR, Xanthoplanine had the highest affinity (K(i)=10 microM) vs [(125)I]alpha-bungarotoxin while the other three compounds displaced the radioligand with K(i) values between 15 and 21 microM. At 100 microM, all four compounds inhibited the responses of these receptors to EC(50) concentrations of ACh.
CONCLUSIONS:
The effects of Xanthoplanine iodide (3) were studied in more detail. Xanthoplanine fully inhibited the EC(50) ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC(50) values of 9+/-3 microM (alpha7) and 5+/-0.8 microM (alpha4beta2).

CAS 6872-88-4
分子量 356.43
分子式

C21H26NO4

溶剂

DMSO

纯度 95%
存储温度 -20℃

相关说明文档

储备液配置

浓度 体积 质量
1mg 5mg 10mg
1 mM 2.8056 mL 14.0280 mL 28.0560 mL
5 mM 0.5611 mL 2.8056 mL 5.6112 mL
10 mM 0.2806 mL 1.4028 mL 2.8056 mL
注:请根据所选浓度进行配置储备液,配置好储备液后进行分装低温保存,避免反复冻融!PCM提供多种溶剂,如:DMSO(PC-57930);玉米油(PC-86094);棉籽油(PC-30875)等

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