Abstract：
:Some geminal bisphosphonates are used clinically for a number of important bone/calcium related diseases; however, side effects and lack of selectivity impede their wide use. This work reports the synthesis and evaluation of bisacylphosphonates (e.g., adipoyl- and suberoylbisphosphonate). These compounds were found to inhibit significantly hydroxyapatite formation and dissolution in vitro and the calcification of bioprosthetic tissue implanted subdermally in rats. These are the first instances of nongeminal bisphosphonates [P-(C)n-P, n greater than or equal to 2] that have been reported to be active in calcium-related disorders. The reported bisacylphosphonates possess apparent lower toxicity, and their calcium complexes/salts have improved solubility properties. Therefore, they are of potential importance for clinical applications.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Golomb G,Schlossman A,Saadeh H,Levi M,Van Gelder JM,Breuer Edoi
10.1023/a:1018956516640subject
Has Abstractpub_date
1992-01-01 00:00:00pages
143-8issue
1eissn
0724-8741issn
1573-904Xjournal_volume
9pub_type
杂志文章abstract：:Intraocular enzymes convert the ketoxime analogues of some beta-adrenergic blockers via a sequential bioactivation process involving hydrolysis to the corresponding ketones followed by reduction to the aryloxyaminoalcohols, which then exert known and predictable physiological and pharmacological effects only at the si...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015863521513
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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journal_title：Pharmaceutical research
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doi：10.1023/a:1011973409022
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-0992-9
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journal_title：Pharmaceutical research
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journal_title：Pharmaceutical research
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-8498-8
更新日期：2006-01-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：1984-05-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018902404036
更新日期：1993-07-01 00:00:00
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pub_type： 杂志文章
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更新日期：2005-02-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2013-08-01 00:00:00
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pub_type： 杂志文章
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更新日期：2019-07-31 00:00:00
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doi：10.1007/s11095-006-9175-2
更新日期：2007-03-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018873702411
更新日期：1999-03-01 00:00:00
abstract：:The new generation of nanotechnology-based drug formulations is challenging the accepted ways of cancer treatment. Multi-functional nanomaterial constructs have the capability to be delivered directly to the tumor site and eradicate cancer cells selectively, while sparing healthy cells. Tailoring of the nano-construct...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0214-7
更新日期：2011-02-01 00:00:00
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journal_title：Pharmaceutical research
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更新日期：2015-04-01 00:00:00
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更新日期：2013-03-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000026444.67883.83
更新日期：2004-05-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
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更新日期：2008-05-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015882323677
更新日期：1991-01-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1021437306990
更新日期：2002-12-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016237216352
更新日期：1995-12-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
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更新日期：1995-04-01 00:00:00
abstract：PURPOSE:The aim of this work was to develop a quantitative, flow cytometric method for tracking the endolysosomal escape of a fluorescently labelled saporin toxin. METHODS:Flow cytometric measurements of fluorescent pulse width and height were used to track the endocytic uptake into Daudi cells of a fluorescently labe...
journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2019-12-23 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2020-07-13 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2006-11-01 00:00:00
abstract：PURPOSE:The objective of this investigation is to develop a rational design of Osteotropic Drug Delivery System (ODDS), which we have proposed as a novel method for drug delivery to the skeleton via bisphosphonic prodrug, based on the relationship between physicochemical and pharmacokinetic properties of bisphosphonate...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011033326980
更新日期：2001-05-01 00:00:00
abstract：:The influence of varying protein and fat content in milk of New Zealand White rabbits on the milk-to-plasma drug concentration (M/P) ratio of diazepam was studied. At various time points after littering, a bolus dose (1.5 mg/kg) followed by a 26-hr infusion (1.8 mg/h) of diazepam was administered to freely moving rabb...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015809418284
更新日期：1992-10-01 00:00:00
