Sharon C. Stratton

article

Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors

Martin E. Swarbrick, Paul J. Beswick, Robert J. Gleave, Richard H. Green, more

Bioorganic & Medicinal Chemistry Letters > 2009 > 19 > 15 > 4504-4508

A novel series of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidine-based cyclooxygenase-2 (COX-2) inhibitors, which have a different arrangement of substituents compared to the more common 1,2-diarylheterocycle based molecules, have been discovered. For example, 2-(butyloxy)-4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)pyrimidine (47), a member of the 2-pyrimidinyl ether series, has...

article

The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor

Susan M. Westaway, Samantha L. Brown, Elizabeth Conway, Tom D. Heightman, more

Bioorganic & Medicinal Chemistry Letters > 2008 > 18 > 24 > 6429-6436

Optimisation of urea (5), identified from high throughput screening and subsequent array chemistry, has resulted in the identification of pyridine carboxamide (33) which is a potent motilin receptor agonist possessing favourable physicochemical and ADME profiles. Compound (33) has demonstrated prokinetic-like activity both in vitro and in vivo in the rabbit and therefore represents a promising novel...

article

In vivo pharmacological effects of JZP-4, a novel anticonvulsant, in models for anticonvulsant, antimania and antidepressant activity

Mark M. Foreman, Taleen Hanania, Sharon C. Stratton, Karen S. Wilcox, more

Pharmacology, Biochemistry and Behavior > 2008 > 89 > 4 > 523-534

JZP-4 is a potent calcium and sodium channel blocker, which is currently being evaluated in patients as an anticonvulsant and mood stabilizer. In the current studies, JZP-4 was evaluated in a variety of animal models for anticonvulsant, antimania and antidepressant activity. In the mouse and rat maximal electroshock models, JZP-4 was slightly more potent than LTG. In the mouse pentylenetetrazole induced...

article

Effect of lamotrigine on the activities of monoamine oxidases A and B in vitro and on monoamine disposition in vivo

Eric Southam, Rui Pereira, Sharon C. Stratton, Rebecca Sargent, more

European Journal of Pharmacology > 2005 > 519 > 3 > 237-245

Recent clinical evidence indicates that the broad spectrum anticonvulsant drug lamotrigine is effective against the depressive phase of bipolar illness and the difficult to treat rapid cycling form of the disorder. However, the molecular mechanism underlying this therapeutic action remains uncertain. Given that inhibition of the A-type of monoamine oxidase (MAO) is a proven antidepressant mechanism,...

article

Effect of lamotrigine treatment on epileptogenesis: an experimental study in rat

Jari Nissinen, Charles H. Large, Sharon C. Stratton, Asla Pitkänen

Epilepsy Research > 2004 > 58 > 2-3 > 119-132

Prevention of epileptogenesis in patients with acute brain damaging insults like status epilepticus (SE) is a major challenge. We investigated whether lamotrigine (LTG) treatment started during SE is antiepileptogenic or disease-modifying. To mimic a clinical study design, LTG treatment (20mg/kg) was started 2h after the beginning of electrically induced SE in 14 rats and continued for 11 weeks (20mg/kg...

article

LABORAS(TM): Initial pharmacological validation of a system allowing continuous monitoring of laboratory rodent behaviour

Leann P. Quinn, Tania O. Stean, Brenda Trail, Mark S. Duxon, more

Journal of Neuroscience Methods > 2003 > 130 > 1 > 83 - 92

A newly developed apparatus for automated behavioural analysis, Laboratory Animal Behaviour Observation, Registration and Analysis System (LABORAS(TM)), has been further validated with respect to the ability of the system to detect the pharmacodynamic effects of standard pharmacological tools. Data were obtained from rats administered with mCPP (reversal with SB242084), 8-OH-DPAT (reversal with WAY100635),...

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The design of 8,8-Dimethyl[1,6]naphthyridines as potential anticonvulsant agents

Nigel E. Austin, Michael S. Hadley, John D. Harling, Frank P. Harrington, more

Bioorganic & Medicinal Chemistry Letters > 2003 > 13 > 10 > 1627-1629

Starting from a series of 7-linked tetrahydroisoquinoline derivatives, as exemplified by SB-270664, a new series of 8,8-dimethylnaphthyridine compounds has been identified. SAR studies around these attractive leads have provided compounds such as 12 which display excellent anticonvulsant activity and an encouraging pharmacokinetic profile in vivo.

article

Effects of lamotrigine and levetiracetam on seizure development in a rat amygdala kindling model

Sharon C. Stratton, Charles H. Large, Brian Cox, Gary Davies, more

Epilepsy Research > 2003 > 53 > 1-2 > 95-106

In kindling models of epilepsy, the period during which repeated stimulation evokes intensifying seizures is attributed to an underlying epileptogenic process, and the point at which class 5 kindled seizures occur is considered the established epileptic state. Previous studies have indicated that a separation can occur between drug effects on these two components. For example, carbamazepine and phenytoin...

article

Broad spectrum anticonvulsant activity of BW534U87: possible role of an adenosine-dependent mechanism

Eric Southam, Sharon C. Stratton, Rebecca S. Sargent, Kim T. Brackenborough, more

Pharmacology, Biochemistry and Behavior > 2002 > 74 > 1 > 111-118

The novel putative anticonvulsant drug 1-[2,6-difluorophenyl)-methyl]-1H-1,2,3-triazolo[4,5-c]) pyridine-4-amine monohydrochloride (BW534U87) effectively reduced seizures induced in rodents by threshold maximal and supramaximal electroshock, electrical kindling, pentylenetetrazole (PTZ) infusion and by vestibular stimulation in the genetically seizure-prone epilepsy-like (EL) mouse. The range of animal...

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Search results for: Sharon C. Stratton

Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors

The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor

In vivo pharmacological effects of JZP-4, a novel anticonvulsant, in models for anticonvulsant, antimania and antidepressant activity

Effect of lamotrigine on the activities of monoamine oxidases A and B in vitro and on monoamine disposition in vivo

Effect of lamotrigine treatment on epileptogenesis: an experimental study in rat

LABORAS(TM): Initial pharmacological validation of a system allowing continuous monitoring of laboratory rodent behaviour

The design of 8,8-Dimethyl[1,6]naphthyridines as potential anticonvulsant agents

Effects of lamotrigine and levetiracetam on seizure development in a rat amygdala kindling model

Broad spectrum anticonvulsant activity of BW534U87: possible role of an adenosine-dependent mechanism

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