LML134 |
| カタログ番号GC38450 |
LML134 (化合物 18b) は、hH3R cAMP および hH3R bdg に対して 0.3 nM および 12 nM の Kis を有する、経口的に活性で選択性の高いヒスタミン 3 受容体 (H3R) インバース アゴニストです。
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Cas No.: 1542135-76-1
Sample solution is provided at 25 µL, 10mM.
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LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 is for the treatment of excessive sleep disorders[1].
LML134 (compound 18b) (oral; 10 mg/kg) indicates rapid oral absorption, with a Tmax of 0.5 hours, t1/2 of 1.54 hours and a fraction absorbed of 44%, as well as a rapid clearance in male Sprague-Dawley rats[1]. LML134 (i.v.; 1 mg/kg) has t1/2 of 0.44 hours, CL of 28 mL/min/kg and the low plasma protein binding in male Sprague-Dawley rat (Fu =39.0%)[1].
[1]. Troxler T, et al. The Discovery of LML134, a Histamine H3 Receptor Inverse Agonist for the Clinical Treatment of Excessive Sleep Disorders. ChemMedChem. 2019 Jul 3;14(13):1238-1247.
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