| Bioactivity | RWJ-52353 hydrochloride is an orally potent, highly selective α2D adrenergic receptor agonist (Ki: 1.5 nM) with potential analgesic effects. RWJ-52353 hydrochloride demonstrated analgesic activity in abdominal tests in rats and mice, and improved agitation in mice in the hot plate test and tail flick test. RWJ-52353 hydrochloride also regulates the organic cation transporter (OCT) subtype, inhibiting rOCT1 and rOCT2 with IC50s of 100 μM and 20 μM respectively; it also activates rOCT3, affecting [3H]-1- in cells. Methyl-4-phenylpyridinium ([3H]MPP| Target |
Ki: 1.5 nM (α2D AR), 254 nM (α2A AR), 621 nM (α2B AR), 443 nM (α1 AR)IC50: 100 μM (rOCT1), 20 μM (rOCT2) |
In Vivo |
RWJ-52353 (30 mg/kg; po; 单剂量) hydrochloride 在诱导引起的小鼠腹部疼痛模型具有抑制作用，抑制率达到 100%[1]。RWJ-52353 在诱导引起的大鼠和小鼠的腹部疼痛模型中的 ED50s 分别为 15.1 mg/kg (po) 和 11.6 mg/kg (po)[1]。RWJ-52353 还能够减轻小鼠在热板实验 (48°C) 和甩尾实验中的痛苦程度，ED50s 分别为 25.9 mg/kg (po) 和 100.2 mg/kg (po)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
CAS |
245744-13-2 |
Formula |
C11H11ClN2S |
Molar Mass |
238.74 |
Transport |
Room temperature in continental US; may vary elsewhere. |
Storage |
Please store the product under the recommended conditions in the Certificate of Analysis. Reference |
[1]. Ross T M, et al. α2 Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1, 3-dimethyl-6, 7-dihydrothianaphthene as a high-affinity ligand for the α2D adrenergic receptor[J]. Journal of medicinal chemistry, 2000, 43(7): 1423-1426. [2]. Amphoux A, et al. Inhibitory and facilitory actions of isocyanine derivatives at human and rat organic cation transporters 1, 2 and 3: a comparison to human alpha 1- and alpha 2-adrenoceptor subtypes. Eur J Pharmacol. 2010 May 25;634(1-3):1-9. |
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RWJ52353 hydrochloride
CAS: 245744-13-2 F: C11H11ClN2S W: 238.74
RWJ-52353 hydrochloride is an orally potent, highly selective α2D adrenergic receptor agonist (Ki: 1.5 nM) with potenti
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