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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].
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10 mg | Inquiry | Inquiry | |
50 mg | Inquiry | Inquiry |
Description | 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]. |
In vivo | RWJ-52353 (30 mg/kg; po) hydrochloride exhibits complete inhibition (100%) in a mouse model of induced abdominal pain [1]. The ED50 values of RWJ-52353 in induced abdominal pain models for rats and mice are 15.1 mg/kg (po) and 11.6 mg/kg (po), respectively [1]. Additionally, RWJ-52353 alleviates pain in the mouse hot plate test (48°C) and tail-flick test, with ED50 values of 25.9 mg/kg (po) and 100.2 mg/kg (po), respectively [1]. |
Formula | C11H11ClN2S |
Cas No. | 245744-13-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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