Abstract：
:In this study the relationships between previously reported connectivity indices described by Kier and Hall and steric contributions to the rate constants for several series of reactions are examined. Rate data were examined for four different series of reactions, which were chosen to represent a range of different reaction mechanisms and transition-state structures. For sterically controlled reactions, the relative rates of series of substrates can be correlated either with the connectivity indices of the substrates themselves or with the changes in the indices that accompany formation of transition states. As expected, the significant indices in the correlations are of the cluster and path-cluster types. The connectivity indices should be useful descriptors in helping relate equilibrium properties, chemical reactivities, and pharmacological data to one another.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Schug JC,Viers JW,Seeman JIdoi
10.1002/jps.2600731038subject
Has Abstractpub_date
1984-10-01 00:00:00pages
1472-7issue
10eissn
0022-3549issn
1520-6017pii
S0022-3549(15)46392-0journal_volume
73pub_type
杂志文章abstract：:Comparability studies used to assess a proposed manufacturing change for a biological product include sensitive analytical studies to confirm there are no significant differences in structural or functional attributes that may contribute to clinically meaningful changes in efficacy or safety. When a proposed change is...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,多中心研究,随机对照试验
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更新日期：2018-06-01 00:00:00
abstract：:There is a growing clinical interest in developing and commercializing pharmaceutical-grade cannabinoid products, containing primarily tetrahydrocannabinol (THC) and cannabidiol (CBD). The oral bioavailability of THC and CBD is very low due to extensive "first-pass" metabolism. A novel oral THC and CBD formulation, PT...
journal_title：Journal of pharmaceutical sciences
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600670235
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abstract：:The hydrolysis of acetylcholine and acetylcholine mustard by acetylcholinesterase was compared over a substrate concentration range of 1-10 mM. Reactions were allowed to proceed for 2 min at 25 degrees. Results of these experiments reveal that the substrates have similar affinities for the enzyme, whereas the maximum ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600640839
更新日期：1975-08-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2019.02.002
更新日期：2019-07-01 00:00:00
abstract：:The pharmacokinetics of tamsulosin (TAM) was investigated using male Sprague-Dawley rats in which plasma alpha(1)-acid glycoprotein (alpha(1)-AGP) levels were elevated by the subcutaneous injection of 0.2 mL/kg of turpentine oil. alpha(1)-AGP levels increased about eight times after turpentine oil treatment, causing a...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/(SICI)1520-6017(200004)89:4<490::AID-JPS6>
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abstract：:We characterized a glucose-sensitive, controlled-release insulin delivery system. Insulin release rates increased when glucose was perfused in the release media surrounding the matrix. The system was composed of solid, particulate insulin, incorporated into an ethylene-vinyl acetate copolymer (EVAc) matrix. Feedback c...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js9600686
更新日期：1996-12-01 00:00:00
abstract：:Twelve 6,8-disubstituted-1-ethyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid derivatives were prepared and evaluated for their antibacterial activity. Among these, only the 6,8-difluoroquinolinone-3-carboxylic acid showed moderate activity. ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600751214
更新日期：1986-12-01 00:00:00
abstract：:N-linked glycosylation is an important post translational modification that occurs on Asparagine 297 residue or a homologous position on the Fc portion of monoclonal antibodies (mAbs). mAb Fc glycans play important roles in antibody structure, stability, and function including effector function and pharmacokinetics. T...
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doi：10.1016/j.xphs.2020.09.056
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600810320
更新日期：1992-03-01 00:00:00
abstract：:A new three-step synthesis of 4-amino-3-hydroxybutyric acid from an inexpensive starting material and under mild reaction conditions is described. Crotonic acid was brominated by the Wohl-Ziegler reaction to 4-bromocrotonic acid, which, in turn, was converted with ammonium hydroxide into 4-aminocrotonic acid. This com...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670133
更新日期：1978-01-01 00:00:00
abstract：:The intracellular delivery of small interfering RNA (siRNA) is a therapeutic strategy to transiently block gene expression. Two silencing RNA strategies utilize either synthetic double stranded RNA or plasmid DNA encoding a short hairpin RNA (shRNA). In the present study, we have quantitatively compared the potency of...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20968
更新日期：2007-11-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600840310
更新日期：1995-03-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21958
更新日期：2010-04-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600721216
更新日期：1983-12-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600620809
更新日期：1973-08-01 00:00:00
abstract：:NF-kappaB activation is clearly linked to the pathogenesis of multiple inflammatory diseases including arthritis. The prominent role of IkappaB kinase-2 (IKK-2) in regulating NF-kappaB signaling in response to proinflammatory stimuli has made IKK-2 a primary anti-inflammation therapeutic target. PHA-408, a potent and ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
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更新日期：2010-03-01 00:00:00
abstract：:Bilateral adrenalectomy (10 days) increased the monoamine oxidase activity of the rat heart, vas deferens, spleen, superior cervical ganglion, and hypothalamus but not that of the rest of the brain, kidney, and liver. Experiments were made to determine whether the increased activity was due to neurogenic influences an...
journal_title：Journal of pharmaceutical sciences
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更新日期：1976-01-01 00:00:00
abstract：:Aqueous solubilities for some guanine derivatives were estimated by semiempirical equations developed by Yalkowsky and Valvani1 using the data for partition coefficient and melting temperature. It was shown that in the case of guanine derivatives examined in this study, the solubility values could not be estimated ade...
journal_title：Journal of pharmaceutical sciences
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更新日期：1999-01-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600661023
更新日期：1977-10-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600680743
更新日期：1979-07-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600690934
更新日期：1980-09-01 00:00:00
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doi：10.1002/jps.1059
更新日期：2001-08-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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更新日期：1996-02-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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更新日期：1977-11-01 00:00:00
abstract：:Insulin-degrading enzyme (IDE) has been implicated in the intracellular degradation of insulin in insulin target cells. Knowledge of the existence of this enzyme in the intestine will be beneficial to the achievement of clinical oral efficacy of insulin. A comparative study was conducted with rat intestine, human colo...
journal_title：Journal of pharmaceutical sciences
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更新日期：1997-01-01 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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更新日期：2002-10-01 00:00:00
abstract：:Pelrinone HCl is essentially nonhygroscopic. The pH-solubility profile exhibits a U-shaped curve, while the octanol-water partition coefficient-pH profile shows a bell-shaped curve. Two ionizable functions, with a pKa1 value of 4.71 and a pKa2 value of 8.94, produce the cationic and anionic forms, respectively. A weak...
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pub_type： 杂志文章
doi：10.1002/jps.2600771104
更新日期：1988-11-01 00:00:00
