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- Title
Molecular Modeling and Potential Ca 2+ Channel Blocker Activity of Diphenylmethoxypiperidine Derivatives.
- Authors
Pulgar, Victor M.; Harp, Jill; Reeves, Tony E.
- Abstract
Molecular interactions of 4-diphenylmethoxy-1-methylpiperidine derivatives with the calcium channel CaV1.1 (pdb:6JP5) are described. All the compounds tested, previously shown to inhibit adrenergic vascular contractions, display similar binding energetics and interactions with the trans-membrane domain of 6JP5 on the opposite side relative to the channel pore, where nifedipine, a known dihydropyridine Ca2+ channel blocker binds. Additionally, the compounds tested inhibit Ca2+-dependent contractions in isolated mouse mesenteric arteries. Thus, diphenylpyraline analogs may exert their anticontractile effects, at least partially, by blocking vascular Ca2+ channels.
- Subjects
CALCIUM ions; CALCIUM channels; MESENTERIC artery; MOLECULAR interactions; DIHYDROPYRIDINE
- Publication
Chemistry (2624-8549), 2023, Vol 5, Issue 2, p713
- ISSN
2624-8549
- Publication type
Article
- DOI
10.3390/chemistry5020050