ARC 239 dihydrochloride (CAS 67339-62-2)
See product citations (4)
QUICK LINKS
ARC 239 dihydrochloride hydrate is a selective α2B-AR adrenoceptor antagonist with a pKD value of 8.8. This antagonist is known to display inhibitory effects on α2A-AR (α2A) and α2D receptors with pKD values of 6.7 and 6.4 respectively. Studies indicate that ARC 239 dihydrochloride is 100-fold more selective towards the α2B-AR (α2B adrenoceptor) than chlorpromazine (sc-357313) and 7-hydroxychlorpromazine. Studies conducted on pentobarbital-treated dogs and rats show that ARC 239 dihydrochloride competitively antagonizes pressor responses to adrenaline, while inhibiting these pressor responses to noradrenaline, phenylephrine, tyramine, and dimethylphenylpiperazinium. ARC 239 dihydrochloride hydrate is an inhibitor of α2B-AR.
ARC 239 dihydrochloride (CAS 67339-62-2) References
- Development of scintillation-proximity assays for alpha adrenoceptors. | Gobel, J., et al. 1999. J Pharmacol Toxicol Methods. 42: 237-44. PMID: 11033439
- Both α2B- and α2C-adrenoceptor subtypes are involved in the mediation of centrally induced gastroprotection in mice. | Zádori, ZS., et al. 2011. Eur J Pharmacol. 669: 115-20. PMID: 21816147
- Yohimbine antagonises α1A- and α1D-adrenoceptor mediated components in addition to the α2A-adrenoceptor component to pressor responses in the pithed rat. | Docherty, JR. 2012. Eur J Pharmacol. 679: 90-4. PMID: 22290390
- Blockade of platelet alpha2B-adrenergic receptors: a novel antiaggregant mechanism. | Marketou, ME., et al. 2013. Int J Cardiol. 168: 2561-6. PMID: 23582690
- Dual Alpha2C/5HT1A Receptor Agonist Allyphenyline Induces Gastroprotection and Inhibits Fundic and Colonic Contractility. | Zádori, ZS., et al. 2016. Dig Dis Sci. 61: 1512-23. PMID: 26860509
- Alpha-2A and alpha-2B adrenergic receptor subtypes: antagonist binding in tissues and cell lines containing only one subtype. | Bylund, DB., et al. 1988. J Pharmacol Exp Ther. 245: 600-7. PMID: 2835476
- Anti-aggregation effect of aroxyalkyl derivatives of 2-methoxyphenylpiperazine is due to their 5-HT2A and α2-adrenoceptor antagonistic properties. A comparison with ketanserin, sarpogrelate, prazosin, yohimbine and ARC239. | Kubacka, M., et al. 2018. Eur J Pharmacol. 818: 263-270. PMID: 29111111
- Regioselective synthesis of isoquinolinonediones through remote unactivated C(sp3)-H bonds. | Huang, L., et al. 2024. Chem Commun (Camb). 60: 4818-4821. PMID: 38616709
- Pharmacological properties of AR-C239, 2-[2-[4(o-methoxyphenyl)-piperazine-1-Yl]-ethyl]4,4-dimethyl-1,3(2H-4H) isoquinolinedione, a new alpha-adrenoceptor blocking drug. | Mouillé, P., et al. 1980. J Cardiovasc Pharmacol. 2: 175-91. PMID: 6171685
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
ARC 239 dihydrochloride, 5 mg | sc-203518 | 5 mg | $125.00 |