| Structural features and protective activity of dexamethasone and pregnenolone-16 alpha-carbonitrile. | |
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MedLine Citation:
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PMID: 957124 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Pretreatment with dexamethasone acetate or pregnenolone-16 alpha-carbonitrile markedly diminished the pharmacological effect of zoxazolamine in rats. This prophylactic action was associated with significantly decreased plasma drug levels, which, in turn, were correlated with enhanced hepatic drug biotransformation, induced by the steroids. Dexamethasone proved to be more active than pregnenolone-16 alpha-carbonitrile in this respect. The A-ring conformation as well as the distances of O-3-O-11, O-11-O-17, and the O-3-mean plane C-5-C-17 may be key factors in glucocorticoid activity, and the longer the distances, the greater the potency. These characteristics have no bearing on catatoxic activity for which the 16 alpha-substituent appears to be a structural prerequisite. |
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Authors:
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A Terzis; P Kourounakis; T Theophanides |
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Publication Detail:
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Type: In Vitro; Journal Article |
Journal Detail:
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Title: Journal of pharmaceutical sciences Volume: 65 ISSN: 0022-3549 ISO Abbreviation: J Pharm Sci Publication Date: 1976 Jul |
Date Detail:
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Created Date: 1976-11-01 Completed Date: 1976-11-01 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 2985195R Medline TA: J Pharm Sci Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 1092-4 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Dexamethasone / pharmacology* Female Glucocorticoids / pharmacology Hydroxylation Microsomes, Liver / drug effects Molecular Conformation Paralysis / chemically induced Pregnenolone Carbonitrile / pharmacology* Rats Structure-Activity Relationship Time Factors Zoxazolamine / antagonists & inhibitors |
| Chemical | |
Reg. No./Substance:
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0/Glucocorticoids; 1434-54-4/Pregnenolone Carbonitrile; 50-02-2/Dexamethasone; 61-80-3/Zoxazolamine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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