Biological Activity:
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AA92593 is a potent and selective small molecule antagonist of melanopsin-mediated photo-transduction (IC50?~160 nM). It inhibits melanopsin (opsinamides) by competing with retinal binding to melanopsin, and inhibits its function without affecting rod- and cone-mediated responses. In vivo administration of AA92593 to mice specifically and reversibly modified melanopsin-dependent light responses, including the pupillary light reflex and light aversion. Melanopsin, expressed in a subset of retinal ganglion cells, mediates behavioral adaptation to ambient light and other non-image-forming photic responses. The discovery of AA92593 raises the prospect of therapeutic control of the melanopsin photo-transduction system to regulate light-dependent behavior and remediate pathological conditions.
How to Use:
In vitro:??AA92593 was used at 10 μM final concentration in various in vitro assays.
In vivo:?AA92593 was dosed intraperitoneally 30 mg/kg 20 min before PLR measurement attenuated pupil constriction in response to light (1013?ph cm-2?s-1) by ~50% in ***** rd mice.?
Reference:
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