245744-13-2
Chemical Structure
RWJ52353 hydrochloride
- CAS No.: 245744-13-2
- Formula:C11H11ClN2S
- Molecular Weight:238.74
IUPAC Name: 5-(6,7-dihydrobenzo[b]thiophen-4-yl)-1H-imidazole hydrochloride
InChIKey: LIHWQUZNTRDJFW-UHFFFAOYSA-N
SMILES: C1(C2=CCCC3=C2C=CS3)=CN=CN1.Cl
Biological Activity:
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
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RWJ52353 hydrochloride | 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 |
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References
- [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. [Content Brief]
