rwj 52353

α2D adrenergic receptor agonist

RWJ-52353 hydrochloride is a potent oral agonist of the α2D adrenergic receptor (Ki: 1.5 nM) with potential analgesic properties. It exhibits pain-relief activity in abdominal tests on rats and mice and reduces agitation in mice during the hot plate and tail flick tests. Furthermore, RWJ-52353 hydrochloride modulates the organic cation transporter (OCT) subtypes by inhibiting rOCT1 and rOCT2 with IC50 values of 100 μM and 20 μM, respectively, and activating rOCT3, influencing the transport of [3H]-1-methyl-4-phenylpyridinium ([3H]MPP) in cells [1] [2].