Journal article
Inhibition of calmodulin by phenothiazines and related drugs: Structure-activity relationships
The Journal of pharmacology and experimental therapeutics, v 222(3), pp 509-516
01 Jan 1982
PMID: 6286920
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
Phenothiazine antipsychotics and several structurally related drugs have been shown to inhibit the actions of calmodulin by binding directly to it in a Ca super(++)-dependent manner. Although both hydrophobic and ionic bonding seem to be involved, the structural factors influencing this interaction are poorly under stood. Accordingly, the abilities of selected phenothiazine derivatives to inhibit the calmodulin-induced activation of phosphodiesterase in vitro was examined. Results show that varying either the phenothiazine nucleus or the amino side chain influenced anticalmodulin potency, suggesting that both of these regions are involved in the binding of drugs to calmodulin.
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Details
- Title
- Inhibition of calmodulin by phenothiazines and related drugs: Structure-activity relationships
- Creators
- W ProzialeckB Weiss
- Publication Details
- The Journal of pharmacology and experimental therapeutics, v 222(3), pp 509-516
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Pharmacology and Physiology
- Web of Science ID
- WOS:A1982PH03000001
- Scopus ID
- 2-s2.0-0019980821
- Other Identifier
- 991019184051504721
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- Collaboration types
- Domestic collaboration
- Web of Science research areas
- Pharmacology & Pharmacy