Cinchona-derived ammonium salts give long-lasting, sensory-selective nerve block
- Ammonium salts built on natural cinchona alkaloids were explored as local anesthetics; the bicyclic quincoridine skeleton beat acyclic and monocyclic analogues.
- Lead CLA-1-3 blocked the rat sciatic nerve for more than 50 hours and potently inhibited voltage-gated sodium channels.
- A second compound, CLA-3-5, gave a sensory-selective block lasting up to about 3 hours at 0.30–0.60% concentration.
💡 Points
Duration is the headline, but the permanently charged ammonium is the more interesting design choice: it should slow washout from the injection site, which probably explains the long action. For anything that lasts over 50 hours, though, I'd look at local neurotoxicity and myotoxicity data before the efficacy curves.
Cinchona Alkaloids-Derived Ammonium Salts for Long-Acting and Sensory-Selective Nerve Blockades ↗