Molecular Modeling and Potential Ca2+ Channel Blocker Activity of Diphenylmethoxypiperidine Derivatives

Author:

Pulgar Victor M.123ORCID,Harp Jill2456ORCID,Reeves Tony E.7ORCID

Affiliation:

1. Department of Pharmaceutical & Clinical Sciences, College of Pharmacy & Health Sciences, Campbell University, Buies Creek, NC 27506, USA

2. Biomedical Research Infrastructure Center, Winston-Salem State University, Winston-Salem, NC 27101, USA

3. Department of Obstetrics and Gynecology, Wake Forest School of Medicine, Winston-Salem, NC 27157, USA

4. Department of Biological Sciences, Winston-Salem State University, Winston-Salem, NC 27101, USA

5. Department of Chemistry, Winston-Salem State University, Winston-Salem, NC 27101, USA

6. Department of Physiology and Pharmacology, Wake Forest School of Medicine, Winston-Salem, NC 27157, USA

7. Department of Internal Medicine, Wake Forest School of Medicine, Winston-Salem, NC 27157, USA

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.

Funder

Department of Pharmaceutical & Clinical Sciences, Campbell University and MD00232 from the National Institutes of Health

Biomedical Research Infrastructure Center (BRIC) Winston-Salem State University

Publisher

MDPI AG

Subject

Organic Chemistry,Inorganic Chemistry,Electrochemistry,Chemistry (miscellaneous)

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