ajmalan-17(R),21alpha-diol hydrochloride
ajmalan-17(R),21alpha-diol hydrochloride Basic information
- Product Name:
- ajmalan-17(R),21alpha-diol hydrochloride
- Synonyms:
-
- ajmalan-17(R),21alpha-diol hydrochloride
- ajmaline hydrochloride
- CAS:
- 4410-48-4
- MF:
- C20H27ClN2O2
- MW:
- 362.89358
- EINECS:
- 224-562-3
- Mol File:
- 4410-48-4.mol
ajmalan-17(R),21alpha-diol hydrochloride Usage And Synthesis
Uses
Ajmaline hydrochloride is a Class Ia antiarrhythmic agent. It inhibits HERG potassium channels with IC50s of 1.0 μmol/l and 42.3 μmol/l in HEK cells and moth spider oocytes respectively. The inhibitory effect of Ajmaline hydrochloride is rapid, reversible, and positive frequency dependent. It acts primarily on the open state of the HERG channel and may also be combined with the inactivated state. The inhibitory effect of ajmaline hydrochloride is dependent on aromatic residues in the S6 domain, and the sensitivity is significantly reduced in the inactivation-deficient HERG S620T channel. It can also slightly affect the activation voltage of HERG channels. Ajmaline hydrochloride's inhibitory effect on HERG channels may contribute to both its potent antiarrhythmic effects and its potential proarrhythmic risk.
Purification Methods
It crystallises from water as the dihydrate m 140o, and the anhydrous salt has m 252-255o, and [] D +84.6o (c 1, H2O). The dihydrochloride crystallises from EtOH/Et2O with m 305-306o. [Beilstein 23 III/IV 3212.]
References
[1] Class Ia anti-arrhythmic drug ajmaline blocks HERG potassium channels: mode of action