Peer-reviewed veterinary case report
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2009
- Authors:
- Zamponi, Gerald W et al.
- Affiliation:
- Department of Physiology and Pharmacology · Canada
Abstract
The therapeutic agents flunarizine and lomerizine exhibit inhibitory activities against a variety of ion channels and neurotransmitter receptors. We have optimized their scaffolds to obtain more selective N-type calcium channel blockers. During this optimization, we discovered NP118809 and NP078585, two potent N-type calcium channel blockers which have good selectivity over L-type calcium channels. Upon intraperitoneal administration both compounds exhibit analgesic activity in a rodent model of inflammatory pain. NP118809 further exhibits a number of favorable preclinical characteristics as they relate to overall pharmacokinetics and minimal off-target activity including the hERG potassium channel.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/19815411/