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Mississauga, Canada

Webster L.R.,Lifetree Clinical Research | Bath B.,Lifetree Clinical Research | Medve R.A.,Nektar Therapeutics | Medve R.A.,NeurAxon Inc. | And 2 more authors.
Pain Medicine (United States) | Year: 2012

Objective. The objective of this study was to evaluate the pharmacokinetics and abuse potential of different formulations of oxycodone. Design. The participants completed an 8-day, placebo-controlled trial with four phases: naloxone challenge, double-blind drug discrimination, double-blind abuse liability, and discontinuation. Subjects. Nineteen healthy, male, recreational drug abusers participated in this study. Interventions. The participants were administered different doses and formulations of oxycodone (40mg immediate release [IR], 40mg controlled release [CR], crushed 40mg CR, and 80mg CR) to evaluate pharmacokinetic parameters and ratings of drug liking and high. Outcome Measures. Pharmacokinetic parameters were determined over a 12-hour dosing interval. The primary pharmacodynamic endpoints were two questions from the Drug Effects Questionnaire ("Do you like the drug?" and "How high are you now?"). Results. Maximal plasma concentrations and area under the curve determinations were similar for 40mg IR, crushed 40mg CR, and 80mg CR, which were all greater than 40mg CR. For drug liking and high, the maximal effect and area under the effect curve were similar for the three formulations, which were all greater than 40mg CR. The dose required to produce comparable reports of drug liking and high was approximately twofold greater for the CR vs IR formulation. When the 40mg CR tablet was crushed, the pharmacokinetic and pharmacodynamic profile was similar to the 40mg IR formulation. Adverse events were consistent with opioid administration. Conclusions. Intact, orally administered oxycodone CR produced less drug liking and high than IR oxycodone, and required approximately twofold greater doses to produce subjective effects comparable to IR oxycodone. © Wiley Periodicals, Inc. Source


Hanessian S.,University of Montreal | Stoffman E.,University of Montreal | Mi X.,University of Montreal | Renton P.,NeurAxon Inc.
Organic Letters | Year: 2011

The scope of MacMillan's organocatalytic asymmetric conjugate addition reaction of indoles and electron-rich aromatics to α,β-unsaturated aldehydes has been extended to the use of 3-amino crotonaldehydes as substrates. The aromatics used include indoles as well as an aniline and a furan. The scope and effect of the groups on nitrogen (R, R′) has also been studied. The method has been applied to the concise synthesis of an advanced precursor to S-(+)-1, a drug prototype for the treatment of migraine headaches.(Figure Presented) © 2011 American Chemical Society. Source


The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.


The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.


Patent
NeurAxon Inc. | Date: 2011-05-06

The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.

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