April 2009
Volume 50, Issue 13
Free
ARVO Annual Meeting Abstract  |   April 2009
Direct Activation of BKca Channels by NS1619 Increases Outflow Facility and Decreases TM Cell Volume
Author Affiliations & Notes
  • W. M. Dismuke
    Pharmacodynamics, University of Florida, Gainesville, Florida
  • D. Z. Ellis
    Pharmacodynamics, University of Florida, Gainesville, Florida
  • Footnotes
    Commercial Relationships  W.M. Dismuke, None; D.Z. Ellis, None.
  • Footnotes
    Support  American Health Assistance Foundation, National Glaucoma Research
Investigative Ophthalmology & Visual Science April 2009, Vol.50, 2035. doi:
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    • Get Citation

      W. M. Dismuke, D. Z. Ellis; Direct Activation of BKca Channels by NS1619 Increases Outflow Facility and Decreases TM Cell Volume. Invest. Ophthalmol. Vis. Sci. 2009;50(13):2035.

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      © ARVO (1962-2015); The Authors (2016-present)

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Abstract

Purpose: : The large-conductance calcium-activated potassium (BKca) channels mediate the nitric oxide (NO)-induced increase in outflow facility and decrease in trabecular meshwork (TM) cell volume. This NO-induced reduction in TM cell volume is mediated through a signal transduction pathway involving soluble guanylate cyclase (sGC), cGMP generation and protein kinase G (PKG). In this study we investigate the ability of a direct activator of the BKca channel, NS1619, to increase outflow facility and decrease TM cell volume.

Methods: : Outflow facility was measured using an anterior segment organ perfusion system. Low passage TM cells were loaded with Calcein AM and visualized using a confocal microscope. Images were taken of TM cells that were treated with or without: DETA-NO, NS1619, hypotonic medium (30% water). Cell volumes were quantified from confocal image stacks using NIH ImageJ software.

Results: : Following a steady basal outflow facility (0.4199+0.0071 ul/min/mmHg) (mean+SEM) a bolus administration of NS1619 (30uM) resulted in a significant increase in outflow facility (0.7816+0.0528 ul/min/mmHg). Outflow facility remained elevated for 3 hours post drug administration before returning to baseline values. Additionally, NS1619 dose-dependently decreased TM cell volume and prevented a hypotonic-induced TM cell volume increase. Finally, exposure to either the NO donor DETA-NO or NS1619 resulted in decreases in TM cell volume, but when administered in combination, produced no additional cell volume decrease.

Conclusions: : These data demonstrate the ability of NS1619, a direct activator of the BKca channel, to increase outflow facility and decrease TM cell volume in a dose-dependent manner. Additionally, NS1619 when administered with a hypotonic shock, attenuated the hypotonic-induced increases in TM cell volume, further implicating the BKca channel in TM cell regulatory volume decrease. The inability of DETA-NO and NS1619 to cause greater decreases in TM cell volume when compared with NS1619 or with DETA-NO alone, suggest that their combined effects are not additive. Taken together, our data suggest that activators of the BKca channel, like NS1619, may have ocular hypotensive properties.

Keywords: trabecular meshwork • outflow: trabecular meshwork • ion channels 
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