LML134

1542135-76-1

375.47

DMSO : 12.5 mg/mL (33.29 mM; Need ultrasonic)

Immunology/Inflammation; GPCR/G Protein; Neuronal Signaling

LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with K_is 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 has the potential for excessive sleep disorders^[1]. IC50 & Target: Ki: 0.3 nM (hH3R cAMP) and 12 nM (hH3R bdg)^[1] In Vivo: LML134 (compound 18b) (oral; 10 mg/kg) indicates rapid oral absorption, with a T_max of 0.5 hours, t_1/2 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 t_1/2 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].