Christopher S Crean

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BACKGROUND Perivascular adipose tissue secretes an adipocyte-derived relaxing factor (ADRF) that opens voltage-dependent K (Kv) channels in peripheral arteries. We studied the role of KCNQ-type Kv channels and tested the hypothesis that hydrogen sulfide (H2S) could be an ADRF. METHODS We performed isometric contraction studies on systemic arteries of rats(More)
Retigabine [RTG (international nonproprietary name); ezogabine (EZG; U.S. adopted name)] is a first-in-class antiepileptic drug (AED) that reduces neuronal excitability by enhancing the activity of KCNQ (K(v)7) potassium (K(+)) channels. RTG/EZG has recently been approved by the European Medicines Agency and the U.S. Food and Drug Administration as(More)
Openers or activators of neuronal KCNQ2/Q3 potassium channels decrease neuronal excitability and may provide benefit in the treatment of disorders of neuronal excitability such as epilepsy. In the present study, we evaluate the effects of ICA-27243 [N-(6-chloro-pyridin-3-yl)-3,4-difluoro-benzamide], an orally bioavailable, potent, and selective KCNQ2/Q3(More)
The seaweed fly mating system is characterized by pre-mating struggles during which females exhibit a mate rejection response involving kicking, shaking and abdominal curling. Males must resist rejection until females become passive and allow copulation to take place. However, despite the vigorous nature of the struggle males frequently dismount passive(More)
BACKGROUND Retigabine (international nonproprietary name)/ezogabine (United States adopted name) is an antiepileptic drug (AED) that enhances KCNQ (Kv7) potassium channel activity. OBJECTIVES The aim of this study was to explore the relationship between retigabine/ezogabine systemic exposure and efficacy and adverse events (AEs) of retigabine/ezogabine(More)
Sexual selection is thought to be responsible for the evolution of exaggerated male characters and of female mate preferences. Evolutionary mechanisms driven by an advantage to the progeny are only effective if the preferred character has a large genetic component of variance; in most systems in which sexual selection operates, little is known of the(More)
PURPOSE To investigate the ocular distribution of 1% azithromycin ophthalmic solution and the effect of polycarbophil-based mucoadhesive formulation on ocular tissue levels of azithromycin after single and multiple topical administrations in the rabbit eye. METHODS Rabbits were treated with either a single administration of 1% azithromycin solution with(More)
OBJECTIVES Ezogabine (EZG) is a potassium-channel opener that has been approved as adjunctive treatment for partial-onset seizures in adults with epilepsy. This Phase I clinical study evaluated the pharmacokinetics (PK), safety, and tolerability of coadministration of EZG and a combined oral contraceptive (OC). METHODS An open-label drug-interaction study(More)
P2Y(12) receptors participate in ADP-induced activation and aggregation of human platelets. INS50589, a selective P2Y(12) receptor antagonist, is being developed for use where controlled, reversible modulation of the platelet hemostatic function is needed. The tolerability, pharmacokinetics, and pharmacodynamics of INS50589 were tested in healthy human(More)
PURPOSE To evaluate the ocular pharmacokinetics of azithromycin and moxifloxacin in human conjunctiva and aqueous humor in subjects undergoing cataract surgery. DESIGN Multicenter, open-label, randomized study. METHODS Subjects scheduled for routine cataract surgery and with normal-appearing conjunctiva were eligible. One conjunctival biopsy sample and(More)