Abstract：
:Substance P (SP) was degraded by synaptic membranes of rat spinal cord. Cleavage products were separated by reversed phase high performance liquid chromatography and identified by amino acid composition analyses. Major products of SP were phenylalanine, SP(1-4), SP(1-6), SP(1-7), SP(10-11), and SP(8-9). Both the degradation of SP and the accumulation of the major cleavage products were strongly inhibited by a metal chelator, o-phenanthroline, and also by specific inhibitors of endopeptidase-24.11, thiorphan, and phosphoramidon. Thus, endopeptidase-24.11 plays a major role in SP degradation in the rat spinal cord. N-Terminal fragments, SP(1-7) and SP(1-4), detected after incubation with spinal synaptic membranes were examined in vivo for antagonism against the scratching, biting, and licking response induced by intrathecal (IT) injection of SP (3.0 nmol) in rats. When IT coadministered with SP, SP(1-7) and SP(1-4) produced a significant inhibition of behavioral response to SP with ED50 of 135.0 pmol and 6.2 nmol, respectively. These results suggest that the degradation of SP in the spinal cord is not only responsible for inactivation of parent peptide, but may also lead to the formation of N-terminal SP-fragments which are shown to display a novel physiological function.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Sakurada C,Watanabe C,Sakurada S,Tan-No K,Sakurada Tdoi
10.1021/js990149csubject
Has Abstractpub_date
1999-11-01 00:00:00pages
1127-32issue
11eissn
0022-3549issn
1520-6017pii
S0022-3549(15)50899-Xjournal_volume
88pub_type
杂志文章abstract：:Nanocrystals have emerged as a potential formulation strategy to eliminate the bioavailability-related problems by enhancing the initial dissolution rate and moderately super-saturating the thermodynamic solubility. This review contains an in-depth knowledge of, the processing method for formulation, an accurate quant...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
doi：10.1002/jps.24694
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abstract：:Sonication process is regularly adopted for dispersing single-walled carbon nanotubes (SWCNTs) in an aqueous medium. This can be achieved by either covalent functionalization of SWCNTs with strong acid or by noncovalent functionalization using dispersants that adsorb onto the surface of SWCNTs during dispersion. Becau...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.24483
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abstract：:Sugars and polyols have been used routinely with lyophilized proteins and peptides as bulking agents, cryoprotectants, and lyoprotectants. However, reducing sugars may present a problem as excipients since they are potentially reactive with proteins. In this stability study of recombinant human relaxin (Rix) with vari...
journal_title：Journal of pharmaceutical sciences
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doi：10.1021/js950456s
更新日期：1996-08-01 00:00:00
abstract：:We extend and modify the Noyes-Whitney equation and the Hixon-Crowell cube root law to include surface roughness effects on the dissolution rate of drugs. The problem is treated theoretically in terms of the fractal reaction dimension, DR, of the effective surface which undergoes dissolution. Effects of changes in DR ...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600810111
更新日期：1992-01-01 00:00:00
abstract：:The aminoxyl (nitroxyl) labeled (2-chloroethyl)nitrosocarbamoyl (CNC) derivatives of amino acids, i.e., N-[[N'-(2-chloroethyl)-N'-nitrosoamino]carbonyl]-A-(1-oxy-2,2,6,6- tetramethylpiperidin-4-yl)amides, A = glycyl (10a), A = L-alanyl (10b), A = L-valyl (10c), A = L-phenylalanyl (10d), were synthesized and evaluated ...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600830715
更新日期：1994-07-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600651218
更新日期：1976-12-01 00:00:00
abstract：:The melting behavior of paracetamol and polyethylene glycol (PEG) 4000, both individually and as binary systems, has been studied using differential scanning calorimetry. The appearance of the PEG peaks was shown to be highly dependent on scanning rate, with evidence for the existence of once-folded and extended chain...
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更新日期：1997-09-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600790704
更新日期：1990-07-01 00:00:00
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更新日期：2016-09-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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更新日期：2021-01-05 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.20679
更新日期：2006-11-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
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更新日期：2008-11-01 00:00:00
abstract：:The crystallization tendency of 2 crystalline polymorphs of indomethacin (Iα, Iγ) in the undercooled melt has been investigated using molecular dynamics simulations. The main thermodynamical and dynamical physical parameters involved in the nucleation and growth processes have been determined. A careful attention has ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2019.10.054
更新日期：2020-02-01 00:00:00
abstract：:The deamidation of asparagine into aspartate and isoaspartate moieties is a major pathway for the chemical degradation of monoclonal antibodies (mAbs). It can affect the shelf life of a therapeutic antibody that is not formulated or stored appropriately. A new approach to detect deamidation using ion exchange chromato...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23529
更新日期：2013-06-01 00:00:00
abstract：:Citric acid anhydrate (CAA) and paracetamol (PARA), prepared as crystalline physical mixtures and as amorphous blends, were studied using (13)C solid-state cross polarization magic angle spinning (CPMAS) NMR. Amorphous blends showed significant line broadening from the conformational distribution as compared to the cr...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21559
更新日期：2009-05-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/1520-6017(200007)89:7<892::AID-JPS6>3.0.CO
更新日期：2000-07-01 00:00:00
abstract：:Hydrolytic degradation products of cefdinir were studied in acidic (pH 1), neutral (pH 6), and basic (pH 9) solutions. Seven major degradation products were isolated by preparative and/or high-performance liquid chromatography and characterized by UV, IR, 1H-NMR, and mass spectra. To clarify degradation pathways in ea...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js950446r
更新日期：1996-09-01 00:00:00
abstract：:One manifestation of cystic fibrosis (CF) is the presence of a viscid mucus secretion in the lungs. The clearance of this mucus is significantly slower than in "normals" due to uncoordinated beating of the cilia and the increased viscosity of the mucus. In these studies, the permeabilities of p-aminosalicylic acid, is...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js950381s
更新日期：1996-06-01 00:00:00
abstract：:The potential binding interaction(s) of the anti-thyroid drug methimazole (MMZ) with the protein bovine serum albumin (BSA) has been studied using isothermal titration calorimetry (ITC) and UV-Visible, fluorescence and circular dichroism (CD) spectroscopic techniques. The binding of MMZ to BSA has been studied in both...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.21140
更新日期：2008-06-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600661113
更新日期：1977-11-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
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更新日期：2010-12-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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更新日期：2019-06-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600680123
更新日期：1979-01-01 00:00:00
abstract：:In this study, the influence of the preparation technique (ball milling, spray drying, and film casting) of a supersaturated amorphous dispersion on the quality of solubility determinations of indomethacin in polyvinylpyrrolidone was investigated by means of statistical analysis. After annealing of the amorphous dispe...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24207
更新日期：2015-01-01 00:00:00
abstract：:Oxidative-reductive interconversion of the methylthiomethyl ester of aspirin and the corresponding sulfoxide and sulfone derivatives can be detected in rat liver homogenate, in addition to the extremely facile hydrolysis of these esters. The methylthiomethyl and methylsulfinylmethyl 2-acetoxybenzoates penetrate freshl...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600700710
更新日期：1981-07-01 00:00:00
abstract：:Role of water in chemical (in)stability is revisited, with focus on deamidation in freeze-dried amorphous proteins and peptides. Two distinct patterns for deamidation versus water have been reported, that is, a consistent increase in rate constant with water, and a "hockey stick"-type behavior. For the latter, deamida...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2017.09.003
更新日期：2018-01-01 00:00:00
abstract：:The poor aqueous solubility of carbamazepine was dramatically increased via complexation with various chemically modified beta-cyclodextrins and gamma-cyclodextrins. A preparation of carbamazepine and 2-hydroxypropyl-beta-cyclodextrin was found to be stable to steam sterilization and to storage under a variety of cond...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600800420
更新日期：1991-04-01 00:00:00
abstract：:The aim of this study was to characterize the metabolic pathways of 2-methoxyestradiol (2ME2), an investigational anticancer drug. In vitro metabolism studies were performed by incubation of 2ME2 with human liver microsomes under various conditions and metabolite identification was performed using liquid chromatograph...
journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章
doi：10.1002/jps.20837
更新日期：2007-07-01 00:00:00
abstract：:The aim was to study a new method of dissolution in vitro, the "Bio-Dis" apparatus, and to compare it with the classical rotating bottle method. Several theophylline controlled-release drug dosage forms were studied. Dissolution testing was performed in increasing pH in standard conditions and after treatment with pea...
journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1002/jps.2600801017
更新日期：1991-10-01 00:00:00
