Xanthoplanine_植物提取-PlantChemMed

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℃