Key result
(-)-Propafenone binds beta-adrenergic receptors more potently than the (+) isomer in rat membranes.
Why the study?
Does propafenone interact stereoselectively with beta-adrenergic receptors?
Does propafenone interact stereoselectively with beta-adrenergic receptors?
Propafenone interacts stereoselectively with beta-adrenergic receptors, with the (-) isomer being significantly more potent, which may explain some of its clinical adverse effects.
No takes yet. Share an insight, caveat, or question.
May contribute to adverse effects; hypothesis-generating and should not change practice without human data.
Burnett et al. (1988) studied this question. (-)-Propafenone and (+)-Propafenone was evaluated on Binding affinity (Ki values) to beta-adrenergic receptors. (-)-Propafenone interacted stereoselectively with beta-adrenergic receptors, showing greater potency than the (+) isomer in rat cerebral cortical and cerebellar membranes (Ki 32 and 77 nM, respectively).
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