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The tachykinin NK1 receptor antagonist PD 154075 blocks cisplatin-induced delayed emesis in the ferret.
TLDR
PD 154075 is a selective and specific high affinity NK1 receptor antagonist with good oral bioavailability which is effective against both acute and delayed emesis induced by cisplatin in the ferret.
Absorption of Cam-2445, and NK1 neurokinin receptor antagonist: in vivo, in situ, and in vitro evaluations.
TLDR
Results indicated that neither stability in the GI tract nor membrane transport were major obstacles to the absorption of Cam-2445, and strongly support GI dissolution and/or precipitation as the limiting factor for the oral bioavailability of the compound.
Investigations on plasma activity of low molecular weight heparin after intravenous and oral administrations.
TLDR
The results of this investigation indicate that LMWH does not have detectable plasma activity after oral administration, and that after i.v. administration it has significant anti-IIa and APTT activities in addition to its anti-Xa activity.
Role of polyamines in the stimulation of synthesis and secretion of plasminogen activator from bovine aortic endothelial cells
TLDR
The results of the present study suggest that polyamines may play a role in the regulation of PA synthesis and secretion and that this function can be modified under pathophysiological conditions affecting cellular and tissue levels of polyamines.
Sample pooling to expedite bioanalysis and pharmacokinetic research.
TLDR
It is demonstrated that sample pooling following One-in-One dosing can be utilized to enhance the throughput rate in PK screening in discovery phase and is likely to be useful in enhancing the throughput of PK characterization in development phase.
The discovery of [1-(4-dimethylamino-benzyl)-piperidin-4-yl]-[4-(3,3-dimethylbutyl)-phen yl]-(3-methyl-but-2-enyl)-amine, an N-type Ca+2 channel blocker with oral activity for analgesia.
TLDR
The rationale for the design, synthesis, biological evaluation, and pharmacokinetics of the 4-piperidinylaniline series of blockers is described.
Effects of sulfonylureas on the synthesis and secretion of plasminogen activator from bovine aortic endothelial cells.
TLDR
The results suggest that, in addition to their beneficial effects in the treatment of diabetes mellitus, some sulfonylurea compounds may also have significant thrombolytic effects and suggest that pharmacological enhancement of PA production by vascular endothelial cells may be a promising antithrombotic mechanism.
Sample pooling to enhance throughput of brain penetration study.
TLDR
By employing sample pooling approach, pharmacokinetic parameters and brain penetration of all six compounds were obtained in a fraction of the time required by conventional single compound dosing and analysis.
Pharmacokinetic evaluation of two human epidermal growth factors (hEGF51 and hEGF53) in rats.
TLDR
The results indicate that the pharmacokinetic behavior of human epidermal growth factor is not altered by deletion of two amino acids from the carboxyl terminus, and suggests that about 23% of the exogenous peptides were associated with red blood cells.
Influence of nicotine and cotinine on the expression of plasminogen activator activity in bovine aortic endothelial cells.
TLDR
It is suggested that nicotine and cotinine may have fibrinolytic activity in vivo and these compounds had no significant effects on the release of PAI.
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