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Submit ReviewDihydroergotoxine mesylate is a complex of closely related alkaloid salts. Binds with high affinity to the GABAA receptor Cl- channel, producing an allosteric interaction with the benzodiazepine site. Also interacts with central dopaminergic, serotonergic and adrenergic (α1) receptors. Displays antiproliferative activity in vitro (IC50 = 18 - 38 μM in prostate cancer cells) and exhibits cognition-enhancing, anticonvulsant and sedative activity in vivo. Orally active.
储存 | Store at RT |
CAS Number | 8067-24-1 |
PubChem ID | 92044435 |
InChI Key | HMMYROQEJAZVGJ-CTOOOFERSA-N |
Smiles | [H][C@]4([C@@]([H])3C[C@@H]([C@@](N[C@@]5([C@H](C)C)C(N([C@@]([H])([C@@H](C)C)C(N7[C@]([H])6CCC7)=O)[C@@]6(O)O5)=O)=O)CN4C)CC1=CNC2=C1C3=CC=C2.[H][C@]%11([C@@]([H])%10C[C@@H]([C@@](N[C@@]%12([C@H](C)C)C(N([C@@]([H])(CC%15=CC=CC=C%15)C(N%14[C@]([H])%13CCC%14)=O)[C@@]%13(O)O%12)=O)=O)CN%11C)CC8=CNC9=C8C%10=CC=C9.[H][C@]%19([C@@]([H])%18C[C@@H]([C@@](N[C@@]%20([C@H](C)C)C(N([C@@]([H])(CC(C)C)C(N%22[C@]([H])%21CCC%22)=O)[C@@]%21(O)O%20)=O)=O)CN%19C)CC%16=CNC%17=C%16C%18=CC=C%17.[H][C@]%26([C@@]([H])%25C[C@@H]([C@@](N[C@@]%27([C@H](C)C)C(N([C@@]([H])([C@@H](CC)C)C(N%29[C@]([H])%28CCC%29)=O)[C@@]%28(O)O%27)=O)=O)CN%26C)CC%23=CNC%24=C%23C%25=CC=C%24.CS(=O)(O)=O.CS(=O)(O)=O.CS(=O)(O)=O.CS(=O)(O)=O |
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参考文献是支持产品生物活性的出版物。
Abdul et al (2008) Expression of gamma-aminobutyric acid receptor (subtype A) in prostate cancer Acta Oncol. 47 1546 PMID: 18607852
Tvrdeic and Perici (1991) Dihydrogenated ergot compounds bind with high affinity to GABAA receptor-associated Cl- ionophore. Eur.J.Pharmacol. 202 109 PMID: 1664802
Tvrdeic and Perici (1992) Dihydroergotoxine modulation of the GABAA receptor-associated Cl- ionophore in mouse brain. Eur.J. Pharmacol. 221 139 PMID: 1333969
Tvredic and Perici (2003) Effects of ergot alkaloids on 3H-flunitrazepam binding to mouse brain GABAA receptors. Coll.Antropol. 27 S175 PMID: 12955907
关键词: Dihydroergotoxine mesylate, Dihydroergotoxine mesylate supplier, Binds, GABAA, receptor, Cl-, channel, allosteric, modulators, benzodiazepine, site, Receptors, 0505, Tocris Bioscience
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